International Journal of
Drug Delivery Technology
ISSN: 0975 4415
Peer Review Journal
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This journal is member of Crossref.
1. Anisotropic Gold Nanoparticles Synthesized using Litchi chinensis Leaf Extract and their Effect on Breast Cancer
Ramanjeet Kaur, Jitender Singh, Pramod K Avti, Vivek Kumar, Rajesh Kumar
Ramanjeet Kaur, Jitender Singh, Pramod K Avti, Vivek Kumar, Rajesh Kumar
Abstract
For its medicinal potential, especially in cancer therapy, eco-friendly gold nanoparticles (GNPs) have gained a lot of interest. This investigation used Litchi chinensis leaf extract (LLE) as a reducing agent for the one-step synthesis of regulated-size GNPs. FTIR spectrum shows that the bio-molecules act as capping and reducing agents. The formation of GNPs has been confirmed using UV-vis absorption spectra. Effect of various synthesized parameters, i.e., reaction time (5–120 minutes), temperature (25–100°C), solvent quantity (5–45 μL), metal ion concentration (0.25–2 mM) and pH (2–10) has been studied. The size, distribution, and morphology (anisotropic) have been studied using FESEM and DLS techniques in the range of 10 to 70 nm. X-Ray diffraction (XRD) reveals that the particles were crystalline and had face-centered cubic (FCC) structure, and Transmission electron microscopy (TEM) images revealed anisotropic morphology (spherical, hexagonal, and triangular). In-vitro studies of GNPs on breast cancer cell lines show cytotoxicity with cellular structural alterations and caused DNA damage without the micronuclei formation.
2. The Development of Tablets containing Vinpocetine and Ginkgo biloba L. Extract
NV Slovesnova, A Yu Petrov, S А Glavatskih, АV Bolotova, DS Kopchuk
NV Slovesnova, A Yu Petrov, S А Glavatskih, АV Bolotova, DS Kopchuk
Abstract
The release rate of active pharmaceutical ingredients (APIs) from tablet dosage forms is significantly influenced by the composition of the formulation, in particular filler composition. In this work, we analyzed the impact of the ratio of excipients on the release rate of vinpocetine from a tablet containing Ginkgo biloba L. extract as the second API. Microcrystalline cellulose (MCC), hydroxypropyl cellulose (L-HPC) mixed with MCC (up to 16% of HPC), and partially pregelatinized starch were used in different ratios as excipients. Moreover, tween-80 was used to study the effect of introduction of emulsifiers on the APIs’ release rates. According to our findings, optimal APIs’ release rates are achieved when using the combination of MCC with HPC at a ratio of 2:3.
3. Effect of Annurca Apple Extract on Anti-hyper Cholesterol Action of a RYR based Formulation
Simone Pepi, Luigi Talarico, Gemma Leone, Claudia Bonechi, Gabriella Tamasi, Marco Consumi, Flavia Bisozzi, Agnese Magnani
Simone Pepi, Luigi Talarico, Gemma Leone, Claudia Bonechi, Gabriella Tamasi, Marco Consumi, Flavia Bisozzi, Agnese Magnani
Abstract
Recently, European Authorities imposed that any product for daily consumption shall provide less than 3 mg of monacolins from red yeast rice (RYR). This obliges to find new formulations able to guarantee an effect on cholesterol levels close to that performed by 10 mg of monacolin K. Two different formulations based on chitosan and xanthan gum containing 10 mg of lovastatin from RYR and a combination of lovastatin (3 mg) from RYR and annurca apple extract (AC), respectively, were compared to verify their anti-hyper cholesterol action in terms of inhibition of HMG-CoA reductase enzyme, protection of high-density lipoprotein (HDL) and low-density lipoprotein (LDL) from oxidation and total free cholesterol depletion. Results highlighted that the combination of RYR and AC represents a valid alternative to the use of high dose of monacolin K. Indeed, formulations containing both nutraceuticals showed a significantly higher activity in terms of inhibition of HMG-CoA reductase, antioxidant activity towards both HDL and LDL and depletion of free cholesterol.
4. Solubility and Taste Masked Behaviour of Cyclodextrin Molecular Inclusion Complex of Lumefantrin
Rahul Bijwar, Harshal Tare
Rahul Bijwar, Harshal Tare
Abstract
Lumefantrine is an antimalarial drugs used especially for pediatric persons. β-Cyclodextrine is used to improve the taste of lumefantrine by forming complexes with them by the solvent evaporation method, respectively. β-Cyclodextrine prevent the release of drug in the saliva. Lumefantrine is a bitter drug. So masking of bitter taste in the formulation is a prerequisite as it improves the compliance of the patient and product value. Lumefantrine with β-cyclodextrin in a drug-polymer ratio 1:1 gave complete taste masking with a satisfactory result obtained in term of in-vivo and in-vitro evaluation visual inspection revealed that lumefantrine was yellow-crystalline. The melting point of lumefantrine was found to be 127℃, respectively. The standard calibration curve of Lumefantrine shows a slope 0.0108 and a correlation coefficient of 0.9997. Compatibility studies show that drugs are compatible with polymers. Solubility study show that the solubility of both drugs are increased in phosphate buffer 6.8 by successfully forming a complex with β-cyclodextrin. The solubility of lumefantrine in saliva (pH 6.8) is 0.408 mg/mL, after complex forming with β-cyclodextrine the solubility of (Lumefantrine complex) is 0.526 mg/mL. In an in-vitro drug release investigation, taste masking occurs when the amount of drug substance in dissolved media is either below the detection threshold for recognizing its taste or is undetectable in the early time points (between 0 and 5 minutes). Taste masking (Taste perception test) 11 volunteers are selected for this test, results show that complex is taste masked successfully. Lumefantrine with β-Cyclodextrine complex is a hopeful approach to enhance solubility, dissolution and drug taste.
5. Catechins as Catalase Modulators: A Comprehensive In-silico Analysis Unveiling their Potential Antioxidant Effects
Harshal Tare, Ujjwala Thube, Ramanlal Kachave, Vijay Wagh , Babaso Udugade
Harshal Tare, Ujjwala Thube, Ramanlal Kachave, Vijay Wagh , Babaso Udugade
Abstract
This research explores the potential of carefully selected catechins as catalase modulators, leveraging their documented antioxidant effects. The catalase protein’s structural quality was rigorously evaluated, revealing an overall high-quality 3D structure. Ligand-based virtual screening identified ten novel catechin hits with promising interactions, presenting candidates designed for new validation. Molecular docking simulations demonstrated robust binding empathies between selected catechins and catalase, with CHEMBL223855 exhibiting the highest affinity. ADMET analysis highlighted CHEMBL223855 as a promising candidate for drug development, boasting favorable properties, including high gastrointestinal absorption and absence of blood-brain barrier permeation. Despite medicinal chemistry alerts and lead likeness violations, this comprehensive analysis guides future experimental validation efforts, supporting the potential of these catechins as effective catalase modulators.
6. Eriodictyol Flavanones Based Virtual Screening of Bioactive Compounds from ChEMBL 2D Database with Classic 3-point Pharmacophore Screening Method for HER2 Inhibitors for Breast Cancer
Harshal Tare, Anjali Bedse, Ujjwala Thube, Ramanlal Kachave, Vijay Wagh
Harshal Tare, Anjali Bedse, Ujjwala Thube, Ramanlal Kachave, Vijay Wagh
Abstract
Understanding binding interactions between flavanones and human epidermal growth factor receptor 2 (HER2) is an important step in developing effective treatments for breast cancer, and this study applies computational methods to do just that. This research presents a comprehensive computational methodology for identifying potential HER2 inhibitors with a focus on breast cancer treatment. The study leverages a combination of structural and pharmacophore-based approaches, starting with bioactive compound selection from the ChEMBL 2D database. The PDB-REDO refined crystal structure of Kinase domain of Human HER2 (erbB2) was used to conduct molecular docking simulations with the identified drugs. The Kleywegt-like plot analysis demonstrates the improved structural quality of the HER2 kinase domain after refinement, showing enhanced agreement with experimental data. Molecular docking simulations, conducted using the AutoDock tool, reveal the binding affinity and interaction patterns of selected compounds with the HER2 receptor. Virtual screening results highlight compounds with high binding affinity, favorable interaction patterns, and structural compatibility as potential lead candidates. To ensure safety and efficacy, ADMETox filtering was employed, providing insights into the compound’s toxicity profile and pharmacokinetic attributes. The selected compound, Eriodictyol (C20H20O6), exhibits a generally favorable safety profile, with predicted inactivity across multiple toxicity classifications and endpoints. While immunotoxicity is predicted, the overall low probabilities suggest a relatively low risk. Physicochemical and pharmacokinetic assessments indicate Eriodictyol’s potential for drug development. With a molecular weight of 356.37 g/mol, balanced lipophilicity, and high gastrointestinal absorption, the compound aligns with drug-likeness criteria. However, careful consideration is warranted due to its inhibitory effects on certain enzymes and alerts for catechol_A and isolated_alkene.
In conclusion, this integrated computational approach streamlines the identification of potential HER2 inhibitors, offering a systematic strategy for drug discovery. Eriodictyol emerges as a promising candidate, demonstrating a favorable safety profile and pharmacokinetic attributes, paving the way for further in-depth studies and development as a potential therapeutic agent for breast cancer.
7. Efficiency of Phenazine Compound Produced by Rhizospheric Pseudomonas fluorescens against Few Pathogenic Bacteria Isolated from Ear Infections
Oras Kadhim, Jehan Y Al-demirchi, Mohammed K Al-Hussainawy, Mais M Al-Hamdani, Abed J Kadhim
Oras Kadhim, Jehan Y Al-demirchi, Mohammed K Al-Hussainawy, Mais M Al-Hamdani, Abed J Kadhim
Abstract
The most typical bacterial infection in children of pediatric age is acute otitis media. Because resistance to these microorganisms grows, management expenses for each pathogen must be specifically adapted to that pathogen. Pseudomonas fluorescens isolated from the rhizosphere rice soil revealed a higher level of antibacterial activity against ear infection pathogenic bacteria than other species of Pseudomonas. Phenazine was extracted P. fluorescens by using organic solvents such as benzene with3.76 μg/ml then characterized with thin layer chromatography and gave a band with a retardation factor (RF) of 0.64 based on the compound’s mobility on the silica plate. In comparison to the antibacterial activity of crude phenazine, the purified phenazine revealed the highest activity against Staphylococcus aureus at 32 mm, and the lowest activity was recorded on bacteria P. aeruginosa with an 18 mm diameter of inhibition. This leads to the encouragement of the use of phenazine compound for the treatment of the increased ear infections due to multi-resistance by causing pathogens.
8. Repurposing FDA-Approved Anastrozole-based Drugs for Breast Cancer through Drug-Drug Transcriptomic Similarity and Cavity Detection guided Blind Docking
Tabjez Mujawar, Harshal Tare, Nitin Deshmukh, Babaso Udugade, Ujjwala Thube
Abstract
Breast cancer remains a significant global health concern, necessitating innovative strategies for drug discovery and development. Repurposing existing drugs offers a promising avenue, leveraging the wealth of information available on food and drug administration (FDA) approved compounds. This study investigates the repurposing potential of anastrozole-based drugs, already established for their efficacy in certain conditions, for breast cancer treatment.
This research presents a multifaceted investigation into the identification, structural refinement, and virtual screening of potential therapeutics targeting the aromatase CYP19A enzyme, a crucial player in hormone-related conditions such as breast cancer. The study commences with the identification of anastrozole-based drugs exhibiting transcriptomic profiles closely resembling known breast cancer therapeutics. Through a comprehensive analysis, a subset of compounds demonstrates high transcriptomic similarity, suggesting shared molecular pathways and target interactions. Notably, anastrozole, a well-known aromatase inhibitor, emerges as a top candidate, highlighting its potential in breast cancer treatment. The crystallographic structure of aromatase CYP19A is subjected to meticulous preprocessing using the PDB-REDO server, resulting in significant improvements in various validation metrics. Structural changes, including alterations in rotamers, removal of water molecules, and peptide flips, indicate the success of the refinement process in enhancing the accuracy of the protein model. The refined structure serves as a reliable foundation for subsequent studies. Further, structure-based cavity detection unveils potential binding sites on the aromatase enzyme. Docking studies employing the cb-dock server elucidate the interaction patterns and binding affinities of selected compounds within these cavities. Anastrozole, along with other candidates like dolasetron and stiripentol, exhibits promising binding scores and interacts with specific residues crucial for enzyme activity.
This integrative approach, combining transcriptomic similarity analysis, structural refinement, and virtual screening, provides valuable insights into potential lead compounds for the inhibition of aromatase in breast cancer therapy. The identified compounds offer a starting point for further experimental validation and drug development. The most promising compound that can be repurposed for as an aromatase inhibitor is dolasetron. Overall, this research contributes to the ongoing efforts to leverage computational methodologies for the rational design of targeted therapeutics against hormone-related disorders.
This research presents a multifaceted investigation into the identification, structural refinement, and virtual screening of potential therapeutics targeting the aromatase CYP19A enzyme, a crucial player in hormone-related conditions such as breast cancer. The study commences with the identification of anastrozole-based drugs exhibiting transcriptomic profiles closely resembling known breast cancer therapeutics. Through a comprehensive analysis, a subset of compounds demonstrates high transcriptomic similarity, suggesting shared molecular pathways and target interactions. Notably, anastrozole, a well-known aromatase inhibitor, emerges as a top candidate, highlighting its potential in breast cancer treatment. The crystallographic structure of aromatase CYP19A is subjected to meticulous preprocessing using the PDB-REDO server, resulting in significant improvements in various validation metrics. Structural changes, including alterations in rotamers, removal of water molecules, and peptide flips, indicate the success of the refinement process in enhancing the accuracy of the protein model. The refined structure serves as a reliable foundation for subsequent studies. Further, structure-based cavity detection unveils potential binding sites on the aromatase enzyme. Docking studies employing the cb-dock server elucidate the interaction patterns and binding affinities of selected compounds within these cavities. Anastrozole, along with other candidates like dolasetron and stiripentol, exhibits promising binding scores and interacts with specific residues crucial for enzyme activity.
This integrative approach, combining transcriptomic similarity analysis, structural refinement, and virtual screening, provides valuable insights into potential lead compounds for the inhibition of aromatase in breast cancer therapy. The identified compounds offer a starting point for further experimental validation and drug development. The most promising compound that can be repurposed for as an aromatase inhibitor is dolasetron. Overall, this research contributes to the ongoing efforts to leverage computational methodologies for the rational design of targeted therapeutics against hormone-related disorders.
9. Ecotoxicological Effects of Lead Exposed Cyprinus carpio and HSP70-Induced Antioxidants against ROS
Sherin Mathew, Sankarganesh P, Baby Joseph
Sherin Mathew, Sankarganesh P, Baby Joseph
Abstract
Lead (Pb) is one of the leading heavy metal pollutions in freshwater sources. This study summarises lead accumulation in freshwater fish Cyprus carpio and its toxicological effects. Pb is known to induce neuro, nephro, and hepatotoxicity in C. carpio and, finally, humans. The effect of Pb leads to the generation of reactive oxygen species (ROS) and antioxidants in the tissues of C. carpio. Antioxidant assays revealed the extent of free radical scavenging activity of the infected tissues. LC50 at a time interval of 24 hours showed a concentration of 7.919 ppm. ROS analysis revealed that the highest concentration of Pb toxicity was observed in the kidneys, liver, and brain of C. carpio. Not only free radicals but also Pb toxicity have been known to activate heat shock proteins as a result of oxidative stress management. This study has raised alarming responses to freshwater aquaculture to initiate control measures against the toxicity and prevent its further entry into the food chain.
10. Standardization of Babbularishta – A Marketed Ayurvedic Formulation as per WHO Guidelines
Seema Gosavi, Pooja Jadhav, Aditi Kulkarni, Supriya Jagtap, Sanket Joshi
Seema Gosavi, Pooja Jadhav, Aditi Kulkarni, Supriya Jagtap, Sanket Joshi
Abstract
Ayurveda is the world’s oldest continuous medicinal tradition. Ayurveda’s discovery of the long-lasting single-dose forms of Asava and Arishta is a boon to modern medicine. Diarrhea, colitis, chronic cough, asthma, tuberculosis, and improved digestive function are only a few of the conditions for which the ayurvedic formulation Babbularishta is utilized. Gallic acid is one of the active ingredients in Babbularishta, a commercially available ayurvedic medicine. The purpose of this study was to develop a standard for the quality of commercially available Babbularishta by measuring its alcohol content and pH. To meet World Health Organisation (WHO) standards, an HPLC and UV method was devised for quantifying the main component, gallic acid, in Babbularishta. Gas chromatography and redox titrimetry were used to confirm the accuracy of the formulation determined during the development process. The formulation was further tested for pharmacological activity, elemental makeup, pesticide traces, and heavy metal concentration.
11. Application of Box-Behnken Design in Optimization of Clobetasol-loaded Nanostructured Lipid Carrier for Topical Use
Devkant Sharma, Anjali Sharma, Niladry Ghosh, Ranjit Singh, Prabhjot Singh, Dinesh K Mishra
Devkant Sharma, Anjali Sharma, Niladry Ghosh, Ranjit Singh, Prabhjot Singh, Dinesh K Mishra
Abstract
The objective of this study was to optimize nanostructured lipid carriers (NLC) for clobetasol propionate using Box-Behnken design (BBD). The formulation was developed by incorporating oleic acid, compritol ATO-888, and tween 80, using the hot homogenization method. The BBD, which employed a 3-level, 3-factor design, investigated the impact of lipid ratio, surfactant concentration, and sonication time on particle size, polydispersity index, and entrapment efficiency (EE). By analyzing the models through ANOVA and diagnostic plots, the optimized formulation composition was selected using the desirability function. The results indicated that a drug-lipid ratio of 1:7.5 was optimal for all formulations. The spherical-shaped Nanostructured lipid carriers had a size of 168.3 ± 0.367 μm, a polydispersity index of 0.248183 ± 0.2847, an EE of 85.4 ± 0.384%, and a desirability value of 0.979. Overall, the use of BBD proved to be a valuable tool in developing optimized NLC with desired properties.
12. Unlocking Therapeutic Potential: A Comprehensive Exploration of FDA-Approved Sirolimus similars for Perivascular Epithelioid Cell Tumor Treatment through Transcriptomic Insight, Structural Integration, and Drug-Drug Similarity Analysis with Cavity-Guided Blind Docking
Tabrej Mujawar, Nandu Kayande, Ujjwala Thube, Santosh Belhekar,Nitin Deshmukh, Harshal Tare
Tabrej Mujawar, Nandu Kayande, Ujjwala Thube, Santosh Belhekar,Nitin Deshmukh, Harshal Tare
Abstract
This research delves into precision medicine for Perivascular epithelioid cell tumors (PEComa), focusing on the repositioning potential of FDA-approved sirolimus similars. Integrating transcriptomic insights and structural analyses, the study identifies analogs with notable similarities to established PEComa treatments. Structural refinement enhances our understanding of drug-target interactions, revealing potential binding sites through cavity detection. Blind docking elucidates interaction patterns and affinities, highlighting sirolimus similars as promising candidates for precision therapy in PEComa. This comprehensive approach contributes crucial knowledge for the effective use of these heliomycins in PEComa treatment, opening avenues for further experimental and clinical exploration.
13. Larvicidal Activity of Ethanol Extract of Cinnamomum sintoc Blume Bark against Aedes aegypti: Role of the Extract as an Acetylcholinesterase Enzyme Inhibitor
Lisda Hayatie, Joharman, Erida Wydiamala, Shabrina N Halisha, Indica Andamari
Lisda Hayatie, Joharman, Erida Wydiamala, Shabrina N Halisha, Indica Andamari
Abstract
The display ponders evaluated the larvicidal exercises of ethanol bark extricates of Cinnamomum sintoc BI against the third instar hatchlings of Aedes aegypti. For superior understanding, this show ponders moreover examined the instrument of plant extricates against the hatchlings through in silico examination. Larvicidal exercises of plant extricate were considered within the extent of 0.01 to 0.1% and two control bunch with aquades and temephos within the research facility bioassays against early third instar hatchlings of A. aegypti. The mortality was checked and subjected to probit investigation to decide the deadly concentrations (LC50 and LC90) to murder 50 and 90% of the treated hatchlings of the particular species. Also, to examine the instrument, four dynamic compounds within the plant extricate with the most noteworthy substance analyzed in silico with the acetylcholinesterase protein in A. aegypti. The appears about appear expanding the concentration will increment the passing of the hatchlings and the viability of the extricate is found to be superior to temephos. The comes about of in silico investigation appeared that the two dynamic compounds in plant extricates, specifically α-copaene and γ-muurolene have a component of activity comparable to temephos. Both of these compounds work as inhibitors of acetylcholinesterase chemicals. Our information recommends that the bark ethanol extricate of C. sintoc BI have the potential to be utilized as a larvicidal operator for the control of the A. aegypti.
14. Removal of Amoxicillin Drug from Aqueous Solution by using Marble Powder Surface Activated by Several Acids
Majeed M Abid, Zainab AA Alhassan, Saad K Mohammed, Mahdi K Ali, Alaa A Omran
Majeed M Abid, Zainab AA Alhassan, Saad K Mohammed, Mahdi K Ali, Alaa A Omran
Abstract
In recent years, the problem of the removal drug from wastewater has become one of the most important global problems due to the accumulation of large quantities of drugs on the surface of the water, which causes a lack of penetration of sunlight into water contaminated with drug, and this leads to a reduction in aquatic life forms for all living organisms and also leads to problems large environmental impacts and many dangerous diseases for humans. An attempt was made to prepare an environmentally friendly, economical and available surface that has a high absorption capacity to remove the contaminants of pharmaceuticals such as amoxicillin (AMX) drug. In this study, waste material such as white marble was used as an absorbent material, and its adsorption properties were enhanced and activated by treating it with several acids (HCL, H2SO4, and HNO3). The prepared white marble before and after adsorption were characterized by field emission scanning electron microscopy (FESEM) and transmission electron microscopy (TEM). The influence of several parameters like contact time (5–120 minutes), initial concentration of drug (10–50 mg/L), adsorbent dosage (0.02–0.2 g), solution temperature (10–40℃), and pH (2–10) was estimated for adsorption method optimization. The equilibrium adsorption result was examined utilizing the isotherm Langmuir, and isotherm Freundlich models. The attained data indicated that, sorption was found to be fast, 84.44% within 1 hour.
15. Design and Characterization of Mangiferin Sustained-Release Tablets
B Nagarani, G V Radha
B Nagarani, G V Radha
Abstract
Background: Mangiferin is a natural bioactive compound used for various pharmacological activities like antidiabetic, anticancer, and anti-inflammatory.
Objective: The development of unique sustained-release matrix tablets of mangiferin is the purpose of the work that is being presented here.
Method: In this study, an effort is made to formulate mangiferin sustained-release matrix tablets by combining the sustained-release polymers HPMC K100M, Kollidone@SR, Keltone LVCR. Mangiferin matrix tablets have been synthesized by wet granulation utilizing the lactose works as the diluent. Systems were developed with different polymer percentages.
Results: Refine the design based on observed differences in weight, hardness, thickness, percent friability, percent drug content, and in-vitro drug release. In-vitro release trials conducted by utilizing a USP type II device utilizing a 6.8 pH phosphate buffer as the separation medium revealed that the most successful F2 formulation, which included 20% polymer, was capable of supporting the mangiferin release for a time of 12 hours period. This sample showed the greatest coefficient (R) value in the Hixson-Crowell model, and release kinetics studies showed that this sample exhibited an erosion process and followed zero-order kinetics.
Conclusion: We can conclude that Kollidone@Sr can be used to prepare sustained-release mangiferin.
Objective: The development of unique sustained-release matrix tablets of mangiferin is the purpose of the work that is being presented here.
Method: In this study, an effort is made to formulate mangiferin sustained-release matrix tablets by combining the sustained-release polymers HPMC K100M, Kollidone@SR, Keltone LVCR. Mangiferin matrix tablets have been synthesized by wet granulation utilizing the lactose works as the diluent. Systems were developed with different polymer percentages.
Results: Refine the design based on observed differences in weight, hardness, thickness, percent friability, percent drug content, and in-vitro drug release. In-vitro release trials conducted by utilizing a USP type II device utilizing a 6.8 pH phosphate buffer as the separation medium revealed that the most successful F2 formulation, which included 20% polymer, was capable of supporting the mangiferin release for a time of 12 hours period. This sample showed the greatest coefficient (R) value in the Hixson-Crowell model, and release kinetics studies showed that this sample exhibited an erosion process and followed zero-order kinetics.
Conclusion: We can conclude that Kollidone@Sr can be used to prepare sustained-release mangiferin.
16. In-vitro and In-vivo Evaluation of Cevimeline HCl Fast Dissolving Films
Vemuri Akash, P Shailaja
Vemuri Akash, P Shailaja
Abstract
The primary aim and objective of the present work was to formulate the cevimeline HCl fast-dissolving films and assess the films, a pharmaceutical compound utilized for the management of xerostomia symptoms linked to Sjogren’s disease. Fast-dissolving films of cevimeline HCl were formulated by utilizing the solvent casting technique and the sodium carboxy methyl cellulose, HPMC E5, polyvinyl alcohol, and polyvinyl pyrrolidone were used as film-forming agents. Additionally, polyethylene glycol 600 and sodium starch glycolate were used as a super disintegrant and plasticizers. The formulation contains citric acid and stevia powder, which serve the purpose of stimulating saliva and providing sweetness, respectively. This study focused mainly on the development and assessment of cevimeline HCl fast-dissolving films, specifically examining parameters such as film thickness, folding resistance, drug content, air bubble entrapment, and film curling. The obtained results were found to be consistent with the preset ranges established for these parameters. The drug release from the fast-dissolving films formulated with PVP K30 was 99.91% released within 5 minutes timeframe. The results indicates that the films prepared with PVP K30 show enhanced solubility, rate of dissolution, flexibility, and tensile strength in comparison to the films formulated with sodium carboxy methyl cellulose, HPMC E5 and Polyvinyl alcohol. Fourier transform infrared (FTIR) and differential scanning calorimetry (DSC) studies were done to characterize the pure drug, polymers and to C11 the optimized formulation. These findings indicated, no observed incompatibilities among the drug and polymers utilized in this study. Moreover, in-vivo investigations were conducted on optimized formulation C11, which demonstrated its notable stability.
17. Microemulgel Delivery of Ciprofloxacin Hydrochloride
Pooja V Torambe, Anuruddha R Chabukswar, Suchita P Dhamane, Swati C Jagdale
Pooja V Torambe, Anuruddha R Chabukswar, Suchita P Dhamane, Swati C Jagdale
Abstract
Background: Ciprofloxacin hydrochloride is broad spectrum carboxyfluoroquinolone antibiotic from BCS class IV. The oral dosage form exhibits gastric irritation whereas the topical cream has demonstrated poor penetration and low bioavailability.
Objective: To optimize microemulsion-based gel of ciprofloxacin hydrochloride to increase its solubility and permeability through the cutaneous layer for targeting bacterial skin infections.
Methods: To develop microemulsion, oil (soya oil, castor oil, oleic acid, isopropyl myristate and vegetable oil), surfactant (cremophore, span 80, tween 80) and cosurfactant (PEG 600 and PEG 400, propylene glycol) were evaluated. To depict the microemulsion formulation pseudo ternary phase diagram was employed. %Transmittance, zeta potential, dissolution study and size analysis were carried out for evaluation of microemulsion. 32 factorial design was used. Two variables i.e concentration of Sepineo P600 and Carbopol 934 effect on microemulgel was evaluated. Evaluation of gel was carried for physical parameters, antimicrobial, in-vitro and ex-vivo release study.
Results: Solubility analysis suggested tween 80, oleic acid and propylene glycol for the formulation of microemulsion. Zeta potential for microemulsion batch F1 was -11.3 mV. This indicated good stability. In-vitro release study showed 91.98% percentage cumulative drug release for batch F1 at 8 hours. Microemulsion-based gel (F1) showed 22.96% inhibition against bacteria which proved its antibacterial activity.
Conclusion: The obtained results exhibited that the permeability and bioavailability of the drug was increased when given through a topical route.
Objective: To optimize microemulsion-based gel of ciprofloxacin hydrochloride to increase its solubility and permeability through the cutaneous layer for targeting bacterial skin infections.
Methods: To develop microemulsion, oil (soya oil, castor oil, oleic acid, isopropyl myristate and vegetable oil), surfactant (cremophore, span 80, tween 80) and cosurfactant (PEG 600 and PEG 400, propylene glycol) were evaluated. To depict the microemulsion formulation pseudo ternary phase diagram was employed. %Transmittance, zeta potential, dissolution study and size analysis were carried out for evaluation of microemulsion. 32 factorial design was used. Two variables i.e concentration of Sepineo P600 and Carbopol 934 effect on microemulgel was evaluated. Evaluation of gel was carried for physical parameters, antimicrobial, in-vitro and ex-vivo release study.
Results: Solubility analysis suggested tween 80, oleic acid and propylene glycol for the formulation of microemulsion. Zeta potential for microemulsion batch F1 was -11.3 mV. This indicated good stability. In-vitro release study showed 91.98% percentage cumulative drug release for batch F1 at 8 hours. Microemulsion-based gel (F1) showed 22.96% inhibition against bacteria which proved its antibacterial activity.
Conclusion: The obtained results exhibited that the permeability and bioavailability of the drug was increased when given through a topical route.
18. Formulation Development and Evaluation of Herbal Antifungal Cream by using Psidium guajava Leaf Extract
Nilima A Thombre, Umesh D Laddha, Eknath D Ahire, Anjali B Tajanpure, Sunita N Surse, Smita P Kakad, Amit V Kakad, Diya Anumone, Rajas Sonawani
Nilima A Thombre, Umesh D Laddha, Eknath D Ahire, Anjali B Tajanpure, Sunita N Surse, Smita P Kakad, Amit V Kakad, Diya Anumone, Rajas Sonawani
Abstract
Fungal infection is one of the major health concerns globally and varies from superficial to systemic infections. Psidium guajava Linn. leaf extract showed antifungal activity against wide range of fungi. The present research focuses on the development and investigation of cream with guava leaf extract. Ethanolic, methanolic and hydroalcoholic leaf extract was evaluated for total flavonoid content, thin layer chromatography (TLC), high-performance thin layer chromatography (HPTLC) and antifungal activity against Candida albicans. Further cream-based extract was optimized using 32 factorial designs. Beeswax and tween 80 were selected as the independent variables whose impact was studied on viscosity and %cumulative drug diffusion. Optimized cream was characterized by appearance, pH, washability, spreadability, in-vitro drug diffusion study, antifungal test and skin irritation test on wistar rats. The hydroalcoholic extract showed the highest content of flavonoids and a better zone of inhibition (27 ± 1 mm). HPTLC results confirmed the presence of essential flavonoids. Cream with 6% beeswax and 5% tween 80 with a viscosity 10420 cP and 70% drug diffusion was considered as optimized batch. The prepared cream showed satisfactory results for all evaluated parameters. The antifungal test showed the highest zone of inhibition for cream (25 mm) in comparison to standard formulation (23 mm). No any sign of skin irritation was observed. The prepared formulation is the best suitable alternative for the available topical antifungal formulation.
19. Microemulgel-based Hydrogel of Diclofenac Sodium using Lipidium sativum as a Gelling Agent
Minal Sonule, Lalchand D Devhare, M Niranjan Babu, Sachinkumar D Gunjal, S Varalaxmi
Minal Sonule, Lalchand D Devhare, M Niranjan Babu, Sachinkumar D Gunjal, S Varalaxmi
Abstract
Aim was to prepare hydrogel containing diclofenac sodium using Lipidium sativum as a gelling agent within a micro emulsion-based system. The oil phase consisted of soybean oil, while surfactants, namely Span 80 and Tween 20, were employed in the formulation. Absolute ethanol was used as a co-surfactant and were characterized by a phase diagram. The in-vitro permeation information is derived from the Franz diffusion. Different microemulsion was designed by screening of various components by performing pseudo-ternary phase diagram and then a solubility study. From this psudo-ternary phase diagram was constructed. In-vitro permeation data was screened from these results the topical delivery of diclofenac sodium microemulsion was clearly confirmed as being by means of w/o microemulsion systems. The optimized formulation of the microemulsion consist of soya bean oil 1.25 mL, span:Tween 20 : 2.5 mL, ethanol 1-mL, water 0.2 mL, L. sativum mucilage and it is compared with the marketed preparation. So, the micro emulsion-based hydrogel of diclofenac using L. sativum mucilage can be used as a gelling agent for a topical drug delivery system.
20. Physicochemical Characterization and Reverse Engineering of Reference Market Product for Generic Formulation Development
Jailani S, CK Dhanapal, Noohu A Khan
Jailani S, CK Dhanapal, Noohu A Khan
Abstract
The present study aimed to carry out reverse engineering of reference innovator product (Xarelto® 20 mg film-coated tablets) to decode the critical scientific information that is needed for successfully develop a stable and bio-equivalent generic formulation of rivaroxaban 20 mg film-coated tablets. The innovator product characterization was done followed by deformulation of the reference product (Xarelto® 20 mg film-coated tablets) to quantity critical excipients to decode the innovator product’s quantitative composition and to identify the manufacturing process used to manufacture the innovator product. The particle size distribution and particle size distribution of rivaroxaban API used in the innovator product were performed using hot-stage microscopy. The polymorphic form of rivaroxaban API used was identified using DSC and XRD methods. Visual, tactile and microscopic evaluation of granules obtained from crushed tablets of the innovator product revealed that the granulation process was used in the manufacturing of the innovator product. It was further concluded that the manufacturing process is wet granulation process due to the presence of organic solvent in the innovator core tablet. Physical evaluation was done to know the tablet weight, shape, size, coating appearance, tablet hardness and disintegration time. Chemical analysis was performed to record the drug content, percentage impurity and dissolution profile. The decoded information can serve as a reference for a faster and bioequivalent generic formulation development with reduced cost, time, effort, and a higher success rate.
21. Development, Optimization and Characterization of Glimepiride Nanosuspension with Improved Solubility and Dissolution
Padmnabh, DC Bhatt
Padmnabh, DC Bhatt
Abstract
Current work describes the development of nanoparticulate suspension (NPs) of glimeperide (GLMP) with enhanced solubility and bioavailability. Using the ultrasonication-assisted precipitation method, GLMP-NP was developed and optimized through the use of a three-factor two-level full factorial design methodology. Drug release, size of a particle, and encapsulation efficiency from nanoparticles were considered as dependent variables while the concentration of Hydroxy propyl cellulose (HPC SSL), Kollicoat IR, and sonication time were considered as independent variables. According to the study, every independent variable significantly affected the dependent variables (p <0.05). The size of the particle GLMP-NP ranged between 159 (F2) to505 nm (F8) while EE varied from 32 (F8) to 75% (F2). The DR of the GLMP-NP observed at 10 min ranged between 35 (F8) to 100% (F2). A significant enhancement in dissolution rate was observed in GLMP-NPs (F1-F8) in comparison to pure GLMP. It was discovered that pure GLMP dissolved in 27.25 ± 6.8 μg/mL of double-distilled water, while GLMP-NP exhibited 3.50 to 6.58-fold enhancement in saturation solubility. FTIR and DSC analysis revealed excellent compatibility between GLMP and excipients. XRD study confirmed the amorphous nature of the nanoparticles while SEM analysis revealed a smooth surface. In conclusion, this study demonstrates the substantial improvement in dissolution rate and solubility of pure GLMP when formulated as nanoparticles.
22. Formulation, Characterization, Optimization, and In-vitro Evaluation of Rosuvastatin as Nanofiber
Ihsan A Mohammed, Fatima J Al-Gawhari
Ihsan A Mohammed, Fatima J Al-Gawhari
Abstract
Bioavailability is the objective for an optimum formulation. The target of the analysis is to maximize both the fluidity and disintegration profile of class II weakly compounds that are water-soluble. Anti-dyslipidemia drug rosuvastatin calcium (RC) (bioavailability 20%) through formulating as nanofibers (NFs) using electrospinning (ES) technology. Twenty formulas were prepared, and different polymers and polymer combinations with various concentrations were used such as polyethylene oxide (PEO) polyvinyl pyrrolidine (PVPK-30), and hydroxypropyl methylcellulose (HPMC). Three distinct groups of maximum parameters, including polymeric solution, electrospinning method, and ambient parameter, are capable of influencing the creation along with the shape of those ultimate NFs. The prepared formulas of rosuvastatin calcium nanofibers (RC-NFs) were evaluated for nanofibers diameter, dissolution profiles, free standing microscopy with electrons and fourier transformation infrared (FTIR)spectroscopy are also available. As a consequence, the velocity of dissolution increases as the particle’s surrounding area increases because of the its small size decrease to the nano level. The optimum ES parameters of polymeric solution (polymer type, concentration, combination, and effect of solvent type), ES process (injection flow rate, voltage, needle gauge, collector round per minute, needle to collector distance and collector type) and ambient parameter are tested and determined. Results show that four selected formulas of NFs are (F12, F14, F15 and F19) with an average diameter of (95, 120, 100 and 80 nm) respectively. The best ultrafine, smooth and beadless NFs is (F19) determined the fact that the narrower the circumference of the RC-NFs, the quicker its breakdown and the shorter the period of this medicinal component’s liberation.
23. Potential of Nitrofurantoin Cyclodextrin Nanosponge Complex to Enhance Solubility and Masking Bitter Taste
Adil Khan, Jaiprakash N Sangshetti, Kamran Mukarram
Abstract
This study aimed to produce b-cyclodextrin (β-CD) based nanosponges (NS) loaded with nitrofurantoin (NFN) to improve oral bioavailability, solubility, and dissolution rate while concealing bitter tastes. The cross-linker diphenyl carbonate and β-CD were reacted in various ratios (1:1, 1:2, 1:4, 1:6, and 1:8) to produce NFN-loaded NS. The developed NS were evaluated for phase solubility study, particle size, drug loading, polydispersity index, scanning electron microscope (SEM), zeta potential, fourier transform infrared (FTIR), differential scanning calorimetry (DSC), a study of phosphate buffer at pH 7.2 for in-vitro release and taste masking ability in human volunteers. Pure NFN showed nearly 100 mcg/mL solubility in ditilled water while at 1:8 (β-CD: DPC) ratio the solubility was found to be 250 mcg/mL, i.e., nearly 2.5 fold enhancement in solubility was observed. The SEM of the NFN-loaded NS (1:8 β-CD: DPC ratio) showed highly spherical surface morphology. For formulation containing a 1:8 proportion of β-CD to DPC, the average particle size was measured at 324.78 ± 10.45 nm, possessing a low polydispersity index of 0.196 ± 0.054. It was found that the zeta potential’s value was -20.59 ± 0.4 mV, indicating sufficient electrostatic repulsion to maintain particle dispersion. FTIR, DSC study reveled excellent drug and excipient compatability. As compared to pure NFN, NFN-loaded NS showed faster release in pH 7.2 phosphate buffer. Research conducted in-vitro showed a gradual release of NFN from pure NFN throughout a two-hour period. The plain NFN suspension was found to have a pronounced bitterness. With 3.95 ± 0.57 as the average score, while the NFN nanosponges (1:8 ratio) had a mean bitterness score of only 0.10 ± 0.00. These findings suggest that the NFN (1:8 ratio) has the capacity to thoroughly cover up the bitter taste of NFN.
24. Formulation and In-vivo Assessment of Topical Polyherbal Hair Serum to Promote Hair Growth
Himani Singh, M A Naidu
Abstract
Male pattern baldness, or androgenic alopecia, is a term used to describe hair loss that results from the underlying sensitivity of hair follicles to androgenic shrinkage. Alopecia is caused by environmental factors, hormone imbalances, and/or inherited factors, according to research studies, however, many etiologies are still unclear. The purpose of treating androgenic alopecia is to slow down the thinning of hair and promote hair growth. A small number of natural treatments, along from allopathic medicines, have demonstrated effectiveness in the decades-long combat over alopecia. The main object of the present study was to develop and in-vivo evaluation of hair growth serum. Crude herbs extract of Hibiscus rosa-sinesis, Glycyrrhizza glabra, Eclipta alba, Withania somnifera and Bacopa monnieria were specifically weighed to make polyherbal serum and animal models are rats with induced androgen test to access for hair growth promoting activity. To assess the serum’s potential against alopecia, it was applied topically. Testosterone had been administered subcutaneously for 20 days to cause alopecia in albino rats. Serums made of herbal extracts were administered concurrently to prevent androgen from having the ability to cause baldness. A positive control was provided with finasteride. At the conclusion hair growth activity was assessed visually, follicular density was measured using an ocular micrometer, and the anagen/telogen ratio was measured using an animal skin sample.
25. Design, Development and Evaluation of Nanosponges Loaded Topical Gel for Rejuvenation of Skin
V Chauhan, N Malviya
V Chauhan, N Malviya
Abstract
The study aimed the development of nanosponges was the choice due to the numerous advantages of this novel technology over the others. Rutin was chosen as it has excellent antioxidant potential. The compatibility study was performed using Fourier transform infrared (FTIR) and there was no interaction found. The optimization study was brought off by Design expert software (version.13). Nanosponges were prepared by emulsion solvent diffusion method. The prepared sponges were brimmed in a night gel formulation for their suitable delivery to the skin. The prepared nanosponges were evaluated for various parameters such as particle size analysis, entrapment efficiency and zeta potential which were found in the acceptable limit. In-vitro permeation study was carried out using Franz-diffusion cell and the cumulative percent drug permeation was found to be 69 to 84.5% in 30 hours. A gel formulation was prepared using rutin-loaded nanosponges and studied for various parameters such as pH, viscosity, and extrudability for various combinations using NS-4. Ex-vivo drug diffusion study reveals that the night gel took 300 minutes for 78.26 to 94.16% permeation. The IC50 values of the flavonoid combination, NS-4 was found to be 54.70, 52.76, and 51.65 μg/mL in the different in-vitro models viz. DPPH, when compared to that of the standard ascorbic acid. Conclusively, the objective of delivery of rutin using nanosponges as carriers for the target delivery was achieved by NS-4 formulation and successfully delivered as night gel for skin rejuvenation.
26. Formulation and Evaluation of Mosquito Repellent Stick
Bobde K Shriram, Lalchand D Devhare, Archana Mehrotra, Savita S Deokar, Surya P Singh
Bobde K Shriram, Lalchand D Devhare, Archana Mehrotra, Savita S Deokar, Surya P Singh
Abstract
Most of mosquito-repellent products and devices are made up of synthetic materials presenting market which causes various harmful effects on human beings. The resistance can be developed by the mosquito due to continuous exposure at high doses. Hence, the present research work represents the development and evaluation of mosquito repellent sticks with the help of various herbal products such as starch powder, wood powder, charcoal powder, eucalyptus oil, coconut oil, lavender oil, lemongrass and cinnamon oil, peppermint and citronella, neem oil making them ozone-friendly, financial effective, non-harmful.
27. Formulation Development and Characterization of Leonotis nepetaefolia Extract Niosomal Gel for Anti-inflammatory Activity
Pravin K Sharma, Rupali Sonntakke, Sujit A Jadhav, Gurmeet Chabra, Rupali Bhavsar Sumeet Dwivedi
Pravin K Sharma, Rupali Sonntakke, Sujit A Jadhav, Gurmeet Chabra, Rupali Bhavsar Sumeet Dwivedi
Abstract
Inflammation is caused when the microorganism enters in our body and settles at specific tissue or sometimes may circulate into the bloodstream. Leonotis nepetaefolia (LN) flower extract contains various phytochemicals out of which saponins and flavonoids are main constituents. As such the phytochemicals have less permeability in the skin, therefore to enhance them these are loaded in niosomes. In the present work, the extract obtained from flowers of LN was taken to develop niosomal gel. The prepared niosomal gel was evaluated for to determine particle size, EE and zeta potential. Also, the anti-inflammatory activity was reported in the present paper. The study indicates that the niosomal gel possesses significant anti-inflammatory activity.
28. Development of Face Pack Powder of Arabica Coffee (Coffea arabica L.) Using Variations of Binders with D-Optimal Mixture Design
Liza Pratiwi, Bambang Wijianto
Liza Pratiwi, Bambang Wijianto
Abstract
Cosmetics like face pack powder are popular preparations used by men and women. Hydroxypropyl methylcellulose (HPMC), sodium carboxymethyl cellulose (CMC-Na) and carbopol are commonly used binders and are suited to dispersal by water. Many natural ingredients such as arabica coffee (Coffea arabica L.) are useful for cosmetics. Chlorogenic acid and α-tocopherol is a bioactive compound for antioxidant activity and is important in its application in face pack powder. This study aimed to determine the ratio comparison of the composition of the three polymers used as the binders for preparations of the coffee face pack powder using a D-optimal mixture design, analyze the evaluation results of the optimum face pack powder formula, and determine its antioxidant activity. The study began with coffee extraction with 70% ethanol as solvent, wet granulation process with binders and other excipients, evaluation of organoleptic properties, pH, and water content, stability observation for28 days, and in-vitro measurement of antioxidant activity. One-sample t-test was applied to analyze the results. The obtained optimum formula was with the ratio of HPMC (8.43): carbopol (1.16): CMC-Na (5.41). The evaluation results of the optimum formula showed that the face pack powder has ash brown color, weak aromatic typical coffee fragrance, homogeneous texture, pH value of 5.93 ± 0.06, and water content of 0.89 ± 0.15%. The resulting study shows the coffee face pack powder and crude extract have antioxidant activity (34.94 ppm ± 0.75 and 15.78 ppm ± 2.53). The analysis with the one-sample t-test showed that the experimental results were not significantly different from the software predictions, so the Design-Expert® software using the D-optimal mixture design is applicable to predict the optimum formula of coffee face pack powder.
29. Formulation and Evaluation of Antiaging Ointment Containing Microencapsulated Turmeric and Jojoba Oil
Abhijit Gholap, Amit Tapkir, Anuradha More, Padmaja Kore, Priyanka Bagade, Prathmesh Nale, Ankita Patil, Abhishek Nagure, Akash Dadas, Krishna Khamkar
Abhijit Gholap, Amit Tapkir, Anuradha More, Padmaja Kore, Priyanka Bagade, Prathmesh Nale, Ankita Patil, Abhishek Nagure, Akash Dadas, Krishna Khamkar
Abstract
Introduction: Skin health and beauty is essential for maintaining the overall well-being of human life. In the current fast-paced world, factors like busy schedules, unhealthy diets, and harsh environmental conditions can lead to noticeable signs of aging. Therefore, it is crucial to find effective solutions to address these concerns and maintain healthy, youthful-looking skin. To address this problem, we prepaid anti-aging ointment. And the beauty of the formulation is it contains microencapsulated turmeric and jojoba oil.
Material and Methods: Microcapsules were synthesized through the utilization of the ionic gelation method. In this method, sodium alginate is used as polymer and calcium chloride as cross-linker. These microcapsules were then incorporated into the ointment base to formulate the anti-aging ointment. Turmeric and jojoba oil were incorporated into the ointment to provide anti-aging benefits.
Results: After the assessment of the microcapsules, it was determined that the prepared microcapsules fall within the range of 400 to 1000 μm. From FTIR spectra revealed successful microencapsulation of oil by sodium alginate. TGA analysis indicates that the prepared microcapsules exhibited thermal stability. The physical properties, spreadability, viscosity, and pH of the ointment were observed within the specified range. Formulation shows sustained release of turmeric oil 68.81% and jojoba oil 74.81% over 6 hours and DPPH assay shows with increase in concentration of oil the free radical scavenging activity also increases.
Conclusion: The oils incorporation of microcapsules has significantly improved the antiaging properties of the ointment. The microencapsulation of these oils enables a sustained release of the active ingredients within the ointment formulation. The DPPH assay results confirm that the formulated ointment possesses robust antioxidant properties.
Material and Methods: Microcapsules were synthesized through the utilization of the ionic gelation method. In this method, sodium alginate is used as polymer and calcium chloride as cross-linker. These microcapsules were then incorporated into the ointment base to formulate the anti-aging ointment. Turmeric and jojoba oil were incorporated into the ointment to provide anti-aging benefits.
Results: After the assessment of the microcapsules, it was determined that the prepared microcapsules fall within the range of 400 to 1000 μm. From FTIR spectra revealed successful microencapsulation of oil by sodium alginate. TGA analysis indicates that the prepared microcapsules exhibited thermal stability. The physical properties, spreadability, viscosity, and pH of the ointment were observed within the specified range. Formulation shows sustained release of turmeric oil 68.81% and jojoba oil 74.81% over 6 hours and DPPH assay shows with increase in concentration of oil the free radical scavenging activity also increases.
Conclusion: The oils incorporation of microcapsules has significantly improved the antiaging properties of the ointment. The microencapsulation of these oils enables a sustained release of the active ingredients within the ointment formulation. The DPPH assay results confirm that the formulated ointment possesses robust antioxidant properties.
30. A Comparative Study of Influence of Different Polymers on Lumefantrine: Piperine Solid Dispersion
Rajendra R Khade, S R Butle
Rajendra R Khade, S R Butle
Abstract
To improve the oral delivery of biopharmaceutical classification system (BCS) class II drugs, solid dispersions techniques are generally adopted in drug product develooment in pharmaceuticals. The choice of polymer in these designs significantly affects a drug’s solubility and dissolution properties. The crystalline nature and the involvement of P-glycoprotein in active ingredient efflux further hinder drug absorption and bioavailability. In this study, solid dispersion (SD) of an antimalarial drug (lumefantrine) combined with piperine (a P-gp and CYP3A4 inhibitor), was created using different polymeric carriers: Soluplus, Klucel, Poloxamer, Povidone/PVP K30 (PVP), and Copovidone/Kollidon® VA64 (KOL). Among these, LUMF-PIP solid dispersion with SOL exhibited the maximum water solvency and fastest release across various media. These findings indicate that the choice of polymeric carrier significantly impacts LUMF’s solubility and dissolution behavior in solid dispersion. SOL emerges as the most promising polymer for enhancing LUMF’s solubility and dissolution, ultimately leading to improved bioavailability upon oral administration.
31. Development of Fast Release Aminated Tamarind Gum Carrier-based Solid Dispersion containing Tablets of Ketoconazole for Solubility and Dissolution Rate Enhancement
Atish B. Velhal, Vijay R. Salunkhe
Atish B. Velhal, Vijay R. Salunkhe
Abstract
This work enhances the solubility as well as dissolution of the biopharmaceutical classification system (BCS) II drug ketoconazole (KTZ) using fast-dissolving tablets that contain solid aminated tamarind gum (ATG). In the first stage amination of the tamarind gum was done to form ATG and which was confirmed by the presence of characteristic peaks using Fourier-transform infrared spectroscopy (FTIR). DSC-TGA analysis showed a weight loss with 3.91% at 100℃, 54.42% loss at 235 to 425℃ and 90% at 485℃. The proton nuclear magnetic resonance (1H-NMR) showed all resonance peaks observed in ATG. The XRD analysis of ATG confirmed the amorphous nature of the material. The second phase involved developing KTZ-loaded solid dispersion (SD) using the kneading process. KTZ SD showed drug content of 94.55 to 97.21%. SD of KTZ manufactured with TG showed 2.55 to 23.82-fold solubility enhancement in water while in case of SD with ATG showed 28.51 to 33.19-fold solubility enhancement. KTZ had a 32% dissolution rate in the pure drug sample, but the SD5 formulation showed a complete release of solid dispersion in 120 minutes. In FTIR, the disappearance of the peak signifies the production of solid dispersion and the drug’s transformation from a crystalline to an amorphous state. Powder X-ray diffraction (PXRD) analysis of solid dispersions reveals a notable decline in crystallinity, as shown by the removal of strong, distinguishing peaks. The scanning electron microscope (SEM) analysis confirmed the successful development of the SD in which KTZ was observed to be dispersed in a polymeric carrier. Optimized KTZ-loaded SD were utilized in fast-dissolving tablets as the third phase. When compared to the drug release achieved from solid dispersions, it was discovered that the dissolving characteristics of all formulation batches were improved.
32. Development and Evaluation of Emulgel Formulation of Diclofenac Sodium utilizing Lipidium sativum as a Gelling Agent
Minal Sonule, Sachinkumar D Gunjal, Prasanthi Samathoti, Badmanaban. R, Bharath Raj K C
Abstract
Emulgels have gained recognition as an effective method for delivering non-polar drugs. The primary goal of our current research is to investigate the potential of Lepidium sativum seed mucilage as a gelling agent in this context. To enhance drug penetration, we have incorporated clove oil, oleic acid, and methyl salicylate. An emulsion was formulated and subsequently integrated into the gel base.
Our research encompassed a series of studies, including rheological assessments, spreading coefficient evaluations, investigations into skin irritancy, and other relevant tests. Furthermore, we conducted drug content analysis, in-vitro release and permeation studies, and stability assessments.
In our in-vitro investigations, it was observed that formulation E6 exhibited the highest drug release within a span of180 minutes. Comparative analyses were conducted, pitting formulations E4, E5, and E6 against a commercially available emulgel preparation.
As a result of our findings, it is evident that an emulgel employing L. sativum mucilage can effectively function as a gelling agent in a topical drug delivery system.
Our research encompassed a series of studies, including rheological assessments, spreading coefficient evaluations, investigations into skin irritancy, and other relevant tests. Furthermore, we conducted drug content analysis, in-vitro release and permeation studies, and stability assessments.
In our in-vitro investigations, it was observed that formulation E6 exhibited the highest drug release within a span of180 minutes. Comparative analyses were conducted, pitting formulations E4, E5, and E6 against a commercially available emulgel preparation.
As a result of our findings, it is evident that an emulgel employing L. sativum mucilage can effectively function as a gelling agent in a topical drug delivery system.
33. Wound Healing Potential of Polyherbal Dusting Powder for the Treatment of Bedsores
Sunita N Surse, Shweta I Sonawane, Priyanka P Sananse, Rani S Kankate, Moreshwar P Patil, Sanjay J Kshirsagar
Sunita N Surse, Shweta I Sonawane, Priyanka P Sananse, Rani S Kankate, Moreshwar P Patil, Sanjay J Kshirsagar
Abstract
A bed sore is also known as a pressure sore and is an open ulcer on the skin. Bedsores are mostly found on the skin that covers bony areas. The primary objective of this research project was to develop and test the polyherbal dusting powder containing an aqueous extract of Azhadirachta indica, Curcuma longa L., Aloe vera, and Tagetes erecta. The preliminary phytochemical investigation of aqueous extract was carried out. Selected herbs have anti-inflammatory, antimicrobial and wound-healing action needed for the treatment of bedsores. The powder was then tested for physical parameters like color, texture, smell, form, and pH), and micrometric parameters like size of particles, angle of repose, Hausner’s ratio, surface area, and other flow properties.
The dosage form has been screened for antimicrobial activity against Escherichia coli, Bacillus subtilis and Staphylococcus aureus. The formulation showed significant antimicrobial activity as compared to the standard povidone iodine drug. In the skin irritation and wound healing studies performed on albino wistar rats, significant effects were observed with 200 mg of powder. According to the in-vivo study, polyherbal dusting powder has been shown to be effective in the treatment of bedsores and can be further investigated.
The dosage form has been screened for antimicrobial activity against Escherichia coli, Bacillus subtilis and Staphylococcus aureus. The formulation showed significant antimicrobial activity as compared to the standard povidone iodine drug. In the skin irritation and wound healing studies performed on albino wistar rats, significant effects were observed with 200 mg of powder. According to the in-vivo study, polyherbal dusting powder has been shown to be effective in the treatment of bedsores and can be further investigated.
34. Design and Characterization of Calcipotriol Proniosomal Gel: In-vivo Exploration against Imiquimod-induced Psoriasis in Experimental Animals
Bhushan R Gudalwar, Tarkeshwar P Shukla
Bhushan R Gudalwar, Tarkeshwar P Shukla
Abstract
The present work focuses on the preparation and evaluation of calcipotriol proniosomal gel (CPG) and find out if the antipsoriatic formulation could prevent imiquimod (IMQ) induced psoriasis in experimental animals. CPG was designed and developed by the coacervation phase separation method. Cholesterol and soya lecithin was used as membrane modifiers and tween 80 and span 60 as non-ionic surfactants. The developed proniosomal gels were characterized which revealed that the optimized batch CPG3 presented excellent formulation characteristics like viscosity of 9690 ± 1.43 cps, rate of spontaneity as 14 ± 1.37, %entrapment efficiency of 82.71 ± 0.48, the average hydrodynamic diameter of niosomes as 739.1 nm, polydispersibility index as 0.360 and ZP of -2.8 mV. In-vivo animal study of the optimized batch CPG3 was performed along with biochemical estimations of oxidative parameters such as glutathione (GSH), Superoxide dismutase (SOD), Malondialdehyde (MDA) and catalase; also, tumor necrosis factor-alpha (TNF-alpha), interleukin-6 (IL-6) were estimated using enzyme-linked immunoassay (ELISA) sandwiched. Histopathological estimation along with psoriasis area severity index (PASI) scores in the IMQ-induced psoriatic model revealed a significant decline in the scoring after treatment with CPG3 compared with a psoriatic group. Primary dermal irritation scoring was also evaluated on Sprague Dawley rats. The results revealed a considerable decrease in skin irritation score compared with a psoriatic group. Also, the levels of GSH, SOD and catalase were raised in CPG3 treated group as compared with a psoriatic group. While MDA level was declined after topical treatment with CPG3 compared with a psoriatic group. In conclusion, the optimized CPG3 showed promising pharmacological effects in the treatment of psoriasis.
35. Solubility Enhancement and Formulation Development of an Oral Film of Ondansetron Hydrochloride Monohydrate using Mix-solvency Concept
Kirti Tomer, Saurav Kumar, Swapnil Goyal, Akanksha Dwivedi, Rakhi Khabiya, Sumeet Dwivedi
Abstract
This research paper presents the formulation and evaluation of ondansetron hydrochloride monohydrate oral film using the mix-solvency concept. Ondansetron hydrochloride monohydrate a selective serotonin receptor antagonist is commonly prescribed to prevent chemotherapy or surgery-induced nausea and vomiting. The aim of the study was to enhance the solubility of ondansetron hydrochloride monohydrate which has been enhanced by the blend of varying aqueous solubilizers poly ethylene glycol, niacinamide, and caffeine. The oral film formulation was prepared using a solvent casting method, incorporating polymers, plasticizers and different solvents. Various formulation variables, including solvent type and concentration, polymer-to-plasticizer ratios, and drug loading, were optimized systematically the resulting oral film was investigated for various parameters such as thickness, drug content, disintegration time, folding endurance and surface pH. The % in-vitro release of drug of the best two formulations F3 and F5 was 99.70 and 96.62%, respectively.
36. Preparation, Characterization and In-vitro Evaluation of Nano Encapsulated 1-Octacosanol for Solubility Enhancing by using Various Polymers through Spray Drying Approach
A K Singh, R Kharb, J B Kandpal
Abstract
This research aimed to develop a nano-encapsulated free-flow powder of 1-octacosanol for functional food application. We had prepared stable green nano-emulsion oil in water by Dyno Mill and spray dryer for free flow powder by using different polymers (Hydroxypropyl methylcellulose, polyvinylpyrrolidone, octenyl succinate starches) as hydrophilic polymers in different ratios for enhancing the solubility. Zeta potential, X-ray diffraction (XRD), fourier transform infrared spectroscopy (FTIR), encapsulation efficiency, particle size distribution, surface morphology, differential scanning calorimetry spectroscopy and in-vitro dissolution research were used to analyze 1-octacosanol.
The optimized nano-emulsion preparation F15 consists of an average particle size 720.9 nm, zeta potential -24.5 mV shows stable nano-emulsion oil in water type, and encapsulation efficiency was found to be 96.76%, FTIR studies did not show any evidence of interaction between the herbal extract and the polymers. XRD shows the conversion of crystalline to amorphous nature of powder. In differential scanning calorimetry (DSC), spectroscopy studies found three major peaks in standard herbal extract peaks is 60.21, 67.16, 81.27°C and nano-encapsulated spray dried powder peaks are 58.18, 66.44, 79.25°C with minor moisture absorbed by the polymer in formulation.
This evaluation shows significant improvement between normal herbal extract of 1-octacosanol and encapsulated spray-dried powder of 1-octacosanol for functional food application successfully improving the water solubility without changing a structural and chemical properties of the 1-octacosanol crystal.
The optimized nano-emulsion preparation F15 consists of an average particle size 720.9 nm, zeta potential -24.5 mV shows stable nano-emulsion oil in water type, and encapsulation efficiency was found to be 96.76%, FTIR studies did not show any evidence of interaction between the herbal extract and the polymers. XRD shows the conversion of crystalline to amorphous nature of powder. In differential scanning calorimetry (DSC), spectroscopy studies found three major peaks in standard herbal extract peaks is 60.21, 67.16, 81.27°C and nano-encapsulated spray dried powder peaks are 58.18, 66.44, 79.25°C with minor moisture absorbed by the polymer in formulation.
This evaluation shows significant improvement between normal herbal extract of 1-octacosanol and encapsulated spray-dried powder of 1-octacosanol for functional food application successfully improving the water solubility without changing a structural and chemical properties of the 1-octacosanol crystal.
37. Solubility Enhancement of Poorly Water-Soluble Drug Ritonavir using Polyvinylpyrrolidone and Chitosan-based Platform Technique
Khakal Nilima N, Aloorkar Nagesh H
Abstract
The antiviral medication ritonavir (RTV) belongs to the biopharmaceutics classification system (BCS) class II drug category and is known for its high permeability and poor solubility. Therefore, the prime objective of this research was to increase the rate of dissolution and improve the solubility of RTV using a polymer system. Solid dispersions consisting of binary polymer components i.e., chitosan (CH) and polyvinylpyrrolidone (PVP) were prepared using microwave microwave-assisted physical mixing technique and optimization of solid dispersion was performed with 32 factorial designs. Dispersions were analyzed for their physicochemical characteristics by the use of X-ray diffraction (XRD), differential scanning calorimetry (DSC), and fourier transform infrared spectroscopy (FTIR). The polymeric dispersions prepared were evaluated for the release of RTV throughout 1 h in 0.1N sodium chloride in a USP class II dissolving device. The phase solubility study demonstrated a considerable improvement in the saturation solubility of RTV when CH and PVP K30 were present either individually or in combination. Virtual interaction studies between the drug and polymers revealed physical interactions driven by van der Waals and hydrophobic forces between RTV and excipients. Carbonyl, amine, and hydroxyl groups, among others, were probably present in both RTV and CH, which allowed for these interactions to take place. There was no discernible interaction between the RTV and the polymers included in the FTIR research. The dispersion strategies have improved the dissolving rate, according to the in-vitro drug release investigation. A formulation including a polymeric dispersion of the optimal concentration of PVP and chitosan may efficiently boost the release of RTV, according to the in-vitro release profile.
38. Optimization of the Photodegradation of Metoclopramide Drug using Super Nanoparticles in Aqueous Solutions
Wesam AL H Alhaidry, Farah Aloraibi, Jasim M Abbas, Hawraa AZ Alhussein, Ruaa Sattar
Abstract
In the present research carry out to remove pharmaceutical pollutants as a model metoclopramide (MCP) drug from an aqueous medium utilizing a photocatalytic degradation method with super nanoparticles called TiO2 nanoparticles (NP). synthesis of TiO2 nanoparticles by utilizing the hydrothermal processes. The physical characterizations of materials by X-ray diffraction (XRD), field emission scanning electron microscopy (FE-SEM), thermogravimetric analysis (TGA), and transmission electron microscope (TEM). The results showed that the efficiency of the TiO2 nanoparticle increased by 88.88%. It also showed that the photocatalytic degradation rate increased with decreasing concentration of MCP drug increasing the intensity of the light led to an increase in the rate of photocatalytic degradation. Study effect of several factors, concentration on the drug, mass of nanoparticle, light intensity that the best conditions for the photocatalytic degradation of 0.3 g of the nanocomposite, MCP drug concentration of 50 m/L, pH solution 8, and light intensity 1.7 mW/Cm2, Thus, the photocatalytic degradation increased with decreasing the concentration of MCP drug. The obtained TiO2 nanoparticle exhibits best photocatalytic degradation than the commercial photo-catalysts TiO2 NPs. Finally, it is essential to evaluate the recycled photocatalytic degradation efficiency, which is one of the utmost significant factors towards photodegradation.
39. Enhanced Solubility and Dissolution Rate of Aceclofenac using Freeze Drying Technique
Vikrant Nikam, Sachin Somwanshi, Vivekanand Kashid, Kiran Kotade, Shubham Shete, Kapil Patil
Abstract
The purpose of this investigation was to determine whether lyophilization or freeze-drying Aceclofenac could improve the solubility of the medicine, making it more easily dissolved into tablets. The drug aceclofenac is classified as a biopharmaceutical classification system (BCS) class II medicine. The lyophilization process was facilitated by the addition of SLS as an adjuvant, which has the potential to enhance the dissolving rate. Aceclofenac was swiftly released from fast-dissolving tablets by including an appropriate ratio of PVP K-30. Aceclofenac from a lyophilized sample dissolved at a much faster pace than plain aceclofenac in-vitro. The amount of polymer had an effect on the dissolving rate. The dissolving efficiency of the drug and polymer is enhanced at a 1:2 ratio. Therefore, aceclofenac can be effectively dissolved using the lyophilization procedure.
40. Formulation Development and Evaluation of Highly Oxidative Degradative Drug Molecule Injectable Dosage form by Lyophilisation Techniques
Hitesh Bhakre, Ashish Agrawal, Vivekanand K Chatap
Abstract
Adrenaline (ADR) It is lifesaving and is the only first-line drug for the treatment of anaphylaxis. Adrenaline (ADR) is the endogenous catecholamine with potent alpha- and beta-adrenergic stimulating properties. Alpha-adrenergic action increases systemic and pulmonary vascular resistance, increasing both systolic and diastolic blood pressure. Adrenaline is released in the bloodstream, which increases heartbeat, muscle strength, blood pressure, and glucose metabolism. Oxidation degradation of the medicinal product is the main route of degradation. Affects chemical and physical changes in drugs during the formulation development process. Physicochemical changes in the product can affect both the safety and efficacy of the drug product.
Main product development strategy to develop, a stable, freeze-dried product of epinephrine for injection. The stability of adrenaline injection is of paramount objective as it is classified as a catechol compound that is sensitive to oxidation to o-quinone and therefore can react further to form highly colored compounds. Adrenergic drugs further react to form adrenochrome, a highly colored indole derivative. The rate of this reaction increased with pH, temperature and presence of the metal ions. Aqueous solutions of adrenergic agonists decompose rapidly when exposed to air, light, or heat, turning pink due to oxidation to adrenochrome and brown due to melanin formation. Due to its strong oxidizing properties and easy decomposition in aqueous solutions. To achieve this, the aqueous solutions of adrenergic agonists decompose rapidly when exposed to air, light, or heat, turning pink due to oxidation to adrenochrome and brown due to melanin formation. Due to its strong oxidizing properties and easy decomposition in aqueous solutions.
Main product development strategy to develop, a stable, freeze-dried product of epinephrine for injection. The stability of adrenaline injection is of paramount objective as it is classified as a catechol compound that is sensitive to oxidation to o-quinone and therefore can react further to form highly colored compounds. Adrenergic drugs further react to form adrenochrome, a highly colored indole derivative. The rate of this reaction increased with pH, temperature and presence of the metal ions. Aqueous solutions of adrenergic agonists decompose rapidly when exposed to air, light, or heat, turning pink due to oxidation to adrenochrome and brown due to melanin formation. Due to its strong oxidizing properties and easy decomposition in aqueous solutions. To achieve this, the aqueous solutions of adrenergic agonists decompose rapidly when exposed to air, light, or heat, turning pink due to oxidation to adrenochrome and brown due to melanin formation. Due to its strong oxidizing properties and easy decomposition in aqueous solutions.
41. Chronopharmacokinetic and Metabolite Studies of the Cardiovascular Medication Sacubitril
Arvind Umarkar, Subhranshu Panda, Hemant Suryavanshi
Abstract
People with “heart failure with preserved ejection fraction” have heart failure, but their ejection fraction is still pretty normal (HFpEF). When it comes to heart failure, people with normal or nearly normal ejection fractions are more likely to get it than those with lower ejection fractions. In clinical trials with HFpEF, medications such as angiotensin-converting enzyme inhibitors (ACEIs), aldosterone antagonists, beta-blockers, calcium channel blockers, and angiotensin receptor blockers (ARBs) did not yield any beneficial results. Sacubitril is prescribed to peritoneal dialysis patients with end-stage renal disease in order to manage their hypertension and heart failure. The concentrations of sacubitril and its primary metabolite in plasma, urine, and peritoneal dialysis fluid were determined using ultra-performance liquid chromatography-tandem mass spectrometry (UPLC-MS/MS). This method is effective because it doesn’t take much time but produces good results. Several samples of body fluids were taken with the help of protein precipitation. The positive ion mode of ionization from the UPLC-MS/electrospray MS was used to look at the extracts. With correlation values of 0.99991 for sacubitril, the suggested method was carefully tested. With this method, it is possible to find out exactly how much sacubitril are in plasma, urine, and peritoneal dialysis fluid. It is also honest, dependable, and nice. If the experiment works, we’ll know that peritoneal dialysis changed how sacubitril were cleared from the body.
42. Exploring the Antioxidant Potential of Cissus woodrowii (Stapf Ex Cooke) Santapau: A Study on Leaves and Stem
Pallavi N Patil, Santosh K Singh, Kiran A Wadkar
Abstract
Cancer, diabetes mellitus, cardiovascular disease, neurodegenerative illness, inflammatory disease, and many other pathologies have a common denominator: oxidative stress. The situation arises from the overproduction or ineffective quenching of free oxygen and nitrogen species within the cell. Antioxidant activity, nutritional value and traditionally roots were made into a powder and applied to cut wounds where pus had formed, ethnobotanical/traditional use is as an antitumor in Maharashtra. Owing to its ethnomedicinal importance, proper identification with pharmacognostic and phytochemical details and evaluation is vital for drug development and to prevent adulteration highlights and their role in laying down standardization. The present paper discusses phytochemical and antioxidant study of Cissus woodrowii (Stapf ex Cooke) Santapau. The both extract showed occurrence of glycosides, phenolic compounds, alkaloids, flavonoids also tannin and aqueous and ethanol extract of stem and leaves showed good antioxidant properties by DPPH assay.
43. Chronopharmacokinetic and Metabolites Investigations of the Cardiovascular Drugs Perindopril
Arvind Umarkar, Subhranshu Panda, Hemant Suryavanshi
Abstract
The heart and vascular systems are well-coordinated. There is a noticeable uneven distribution of regulatory mechanisms and pathogenic events over the course of a day. In addition, the physiological circadian clock of the cardiovascular system might be disrupted by several disorders. In terms of global mortality and morbidity, heart failure (HF) ranks high. The angiotensin receptor-neprilysin inhibitor perindopril is now a valid option for treating heart failure. There is a lack of comprehensive evaluations of perindopril’s safety and effectiveness in HF at the present time. First, we provided an overview of perindopril’s pharmacological actions, which include inhibiting the renin-angiotensin system and decreasing natriuretic peptide breakdown in the natriuretic peptide system. After that, we summed up the benefits of perindopril for heart failure patients with preserved ejection fraction (HFpEF) or reduced ejection fraction (HFrEF), such as lowering the risk of death and hospitalization, reversing cardiac remodeling, regulating biomarkers of heart failure, improving quality of life, providing antiarrhythmic effects, enhancing renal dysfunction, and regulating metabolism. Our discussion of perindopril’s safety and tolerability in treating HFrEF or HFpEF came to a close. Although there is a considerable risk of hypotension, perindopril demonstrated superior safety and tolerability when compared with placebo. For HFrEF patients, perindopril is a safe and effective therapy option, however, for HFpEF patients, it shows little benefit, according to the majority of studies. Soon, perindopril will likely be one of the most effective drugs available to treat heart failure.
44. Investigation of Antimicrobial Activity and Characterization of Isolated Allyl Isothiocyanate
Prashant B Patil, Hardik Goswami, Arjun Chaudhari, Jayvadan K Patel
Abstract
Allyl isothiocyanate (AITC) is a natural compound known for its potential antimicrobial properties. In this study, we present a comprehensive investigation into the isolation, characterization, and antimicrobial activity of AITC which is obtained from mustard seeds. The isolation of AITC was achieved through an efficient extraction process, employing extraction assembly. Subsequently, AITC was subjected to a series of physicochemical tests to elucidate the presence of physicochemical constituents. Furthermore, we employed UV-visible spectroscopy and infrared (IR) spectroscopy to obtain valuable insights into the structural features of AITC. To gain a deeper understanding of the phyto-constituents present in AITC, gas chromatography-mass spectroscopy (GC-MS) was used for phytochemical profiling. The antimicrobial activity of AITC was assessed against two pathogenic microorganisms, Staphylococcus and Escherichia coli. The outcomes of our study reveal the possible potential of AITC as an antimicrobial agent, demonstrating its inhibitory effects on the growth of both microbial strains and zone diameter of inhibitions are 12, 10, and 4 mm for Staphylococcus and 14, 12 and 6 mm for E. coli and hence the AITC extracts were found to have antibacterial activity. This research provides treasured comprehensive insights into the isolation, characterization, and antimicrobial belonging properties of AITC which is derived from mustard seeds. The findings suggest that AITC has promising applications in the field of antimicrobial research, opening avenues for further investigation into its potential therapeutic uses.
45. Pre-clinical and In-silico Analysis of the Augmentation of Dermal Regeneration by Punica granatum Linn Fruit Peel in Rats
Nimmy Varghese, Prerana Shetty, Srusha Samani, Harsha Ashtekar
Abstract
Background: Pomegranate is a very delicious fruit having miraculous properties. It contains flavonoids, polyphenols, tannins, organic acid and water-soluble vitamins which contribute to a wide variety of pharmacological activity. We investigated the dermal regeneration bracing potential of the extract of Punica granatum L. dried peel. Also, computational studies for finding the phytochemicals responsible for the pharmacological activity was carried out. Methods: Fruit peel of P. granatum L. was collected, dried and extracted by maceration using ethanol. We employed in-vivo screening methods viz. excision, incision and dead space wound repair animal models, silver sulfadiazine ointment was used as a reference standard. Results: Dose-dependent and significant (p <0.05) bracing of dermal regeneration was observed.
46. P Glycoprotein Mediated Drug Interaction between Digoxin and Orange Juice- Exploratory Study by In-vitro Approach
Deepalakshmi M, Anslin Joanna, Keerthana Venkat, Malwyn Mofhy, Arun K P
Abstract
P.gp is an efflux transporter that plays a vital role in drug transportation. Aim: This exploratory study is aimed to find the P-glycoprotein (P-gp) mediated drug interaction between digoxin and orange juice, conducted for a period of six months. The 3D structure of the human P-gp was predicted from the peptide by molecular threading using default settings. The structural analysis and verification server and the PDB were used to assess the stereo-chemical quality of these structures. The molecular structure of P-gp in a transport cycle has been investigated using a variety of methods. Molecular docking has been performed to predict the highest binding affinity to P gp with ligands of orange juice and ligands of ketoconazole. In 50% ethyl acetate extract of orange juice was prepared and a transcellular transport study was done using MDR1 transfectants and MRP2 transfectants LLC-PK1, LLC-GAS-COL150, LLC-pCI and LLC-MRP cells grown in M199 medium supplemented with 10% fetal calf serum at 37℃ in a humidified atmosphere of 5% CO2/95% air. The minimum inhibitory concentration is found to be125 mcg/mL. Hence, the loading concentration along with orange juice is found to be 24.562 mcg/mL and the concentration less than that is found with poor sensitivity. Whereas the concentration above 125 mcg/mL loaded with orange juice is found to inhibit P-gp. The absorbance of orange juice and digoxin was measured at 470 nm. Since digoxin is not sensitive to orange juice beyond the concentration of 125 mcg/mL, it is considered as the MIC. Hence orange juice is a moderate p-gp Inhibitor and it escalates the serum digoxin toxicity. Orange juice is inhibiting the P-gp which increases the serum toxicity levels of digoxin.
47. Design and Discovery of Genistein-based Drugs as a Potential Tyrosine Kinase Inhibitor for Lung Adenocarcinoma through Hybrid In-silico Methods
Vijay Wakale, Ramanlal Kachave, Pranjal Gholap, Kiran Mahajan, Harshal Tare
Abstract
This research employs a comprehensive approach to investigate potential therapeutic candidates for lung adenocarcinoma through drug-drug transcriptomic similarity analysis and molecular docking simulations. Using the Connectivity Map Touchstone tool, we identified compounds with high transcriptomic similarity to genistein, revealing potential shared mechanisms of action. The selected compounds, including avrainvillamide-analog-2, were further assessed through molecular docking simulations against the tyrosine kinase inhibitor (TKI) enzyme. Avrainvillamide-analog-2 exhibited a remarkable binding affinity in pocket C2, interacting with key amino acids. The results provide valuable insights into the pharmacological properties of the identified compounds, laying the groundwork for future experimental validations and drug development initiatives. Additionally, cavities detection by CB Dock server and structural refinement by PDB REDO contribute to the overall understanding of ligand binding and protein structure. This integrative approach offers a holistic perspective for identifying potential lead compounds and understanding their molecular interactions, facilitating the rational design of novel therapeutics for lung adenocarcinoma.
48. In-silico Design and Development of Multi-Target Agents Targeting Glycogen Synthase Kinase-3 Beta and Vascular Endothelial Growth Factor Receptor 2 for Acute Myeloid Leukemia
Asmita Gaikwad, Nandu Kayande, Harshal Tare, Babaso Udugade, Ramanlal Kachave
Abstract
This research focuses on the in-silico design of multi-target agents for acute myeloid leukemia (AML), targeting GSK-3β and VEGFR2. Using TTD data, we selected a promising target pair and considered 20,818 agents. Ligand-based screening in ChEMBL identified compounds with diverse structures and favorable interactions. Protein structures (GSK-3β: PDB ID 1Q5K, VEGFR2: PDB ID 3QTK) underwent rigorous quality assessment, indicating high-quality models. Molecular docking revealed varied affinities, with CHEMBL183504 showing strong affinity for GSK-3β in pocket C1, and CHEMBL185922 for VEGFR2 in pocket 2. CHEMBL181959 exhibited dual affinity. Further experimental validation is needed. In conclusion, this study provides insights for AML therapy, guiding compound selection and structural quality assessment for potential drug development.
49. Designing, Creating, and Assessing a Modified Pulsincap Delivery System for Intestine Targeting of Fluvastatin in Accordance with Circadian Rhythm
M Mahesh, S Jayakumari
Abstract
The current study’s objective remains to create the Pulscap delivery system using an insoluble capsule core that contains fluvastatin sodium microspheres. Eudragit RL 100 polymer fluvastatin sodium microspheres were made using the solvent evaporation method. To reduce the possibility of stomach upset, these microspheres were hand-filled into capsules, plugged with hydrogel plugs, then sealed with ethyl cellulose acetate and dipped in an eight: two (vol/vol) Acetone: ethanol solution by butyl pthalate of (0.75%) and 5% cellulose acetate phthalate solution. Formulated dosage form was assessed for in-vivo X-ray imaging studies, in-vitro drug release studies, and in-vivo imaging studies, pharmacokinetic study of the optimized formulation was conducted in a two-way cross-over design with 6 rabbits in each group and the pharmacokinetic parameters (Cmax, Ka, Ke, MRT and AUC0-α) are measured. A Pharmacodynamics study was also performed on lipid profiles in six groups of rabbits. Optimized formulation (F20) which is prepared with a drug and polymer ratio of 1:3, is selected based on a dissolution study which shows a percentage release of 99.98. ± 0.12% at 17th hour. In the in-vivo study, the plasma concentration at 12th hour 53.8 ± 0.02% and at 32nd hour 13.9 ± 0.05%. Pharmacokinetic parameter Cmax (ng/mL): 53.8 ± 0.41, MRT (h): 20.0 ± 0.14, t1/2 (h): 8.52 ± 0.014, Kel (h-1) :0.08 ± 0.014, Ka (h-1):0.25 ± 0.02, AUC0-a (ng h/mL): 944.9. ± 4.05. Serum lipid profile in high cholesterol rabbit after treatment with F20 formulation total cholesterol:240.83 ± 19.76, HDL-C:37.33 ± 2.16, triglycerides:318.67 ± 7.74, VLDL-C:63.73 ± 1.55, LDL-C:139.77 ± 18.74. Compared to lovastatin SR release, lovastatin pulsatile release, and fluvastatin SR release, the results imply that the F20 formulation’s pulsatile drug delivery has established good drug delivery for medications entering the gastrointestinal tract, and it displays superior pharmacokinetic and pharmacodynamic parameters.
50. Formulation of Herbal Topical Dermatological Dosage Form by Quality by Design Approach
Rupali H Tiple, Shamli R Jamane, Deepak S Khobragade, Dharmendra R Mundhada
Abstract
Objective: The study developed an optimized dosage form by quality by design (QbD) approach containing Azadirachta indica (Neem) leaf extract and a combination of selected herbal oils viz. A. indica oil, Eucalyptus citriodora oil and Cymbopogon martini oil and assessed for its antifungal efficacy, stability and dermal safety.
Methods: Ointment was prepared using the fusion method from an extract of neem leaves with a combination of herbal oils viz. A. indica, E. citriodora, C. martini, bees wax and soft-paraffin. Utilizing the Box-Behnken Design (BBD), the variables such as the percentage of soft paraffin, beeswax and melting temperature were optimized in relation to the output variables such as viscosity, spreadability, and finally the antifungal efficacy, which was further quantified. Wistar albino rats were used (n = 5/test, positive and negative control) to evaluate the acute dermal toxicity test of the formulated ointment. Stability studies were assessed at 25 ± 2℃/ 60 ± 5% RH and 40 ± 2℃/ 75 ± 5% RH.
Results: Melting point and percentage of beeswax significantly affect viscosity and spreadability. Optimal viscosity was obtained at 5.4% beeswax and 89.6% soft-paraffin when melted at 58℃. No dermal toxicity was observed by the ointment when comparable to petroleum jelly, both differed significantly with negative control. The absence of new spots on chromatograms, a prominent zone on agar plates, and negligible changes in spreadability (p = 0.112) all suggested physical stability, chemical stability, and antifungal efficacy, respectively.
Conclusion: Neem leaf extract and a blend of selected herbal oils; A. indica, E. citrodora, and C. martini, when combined to formulate ointment, proved reliable and stable dosage form with significant anti-fungal efficacy. The formulated ointment might be helpful tool for dermatophytes management.
Methods: Ointment was prepared using the fusion method from an extract of neem leaves with a combination of herbal oils viz. A. indica, E. citriodora, C. martini, bees wax and soft-paraffin. Utilizing the Box-Behnken Design (BBD), the variables such as the percentage of soft paraffin, beeswax and melting temperature were optimized in relation to the output variables such as viscosity, spreadability, and finally the antifungal efficacy, which was further quantified. Wistar albino rats were used (n = 5/test, positive and negative control) to evaluate the acute dermal toxicity test of the formulated ointment. Stability studies were assessed at 25 ± 2℃/ 60 ± 5% RH and 40 ± 2℃/ 75 ± 5% RH.
Results: Melting point and percentage of beeswax significantly affect viscosity and spreadability. Optimal viscosity was obtained at 5.4% beeswax and 89.6% soft-paraffin when melted at 58℃. No dermal toxicity was observed by the ointment when comparable to petroleum jelly, both differed significantly with negative control. The absence of new spots on chromatograms, a prominent zone on agar plates, and negligible changes in spreadability (p = 0.112) all suggested physical stability, chemical stability, and antifungal efficacy, respectively.
Conclusion: Neem leaf extract and a blend of selected herbal oils; A. indica, E. citrodora, and C. martini, when combined to formulate ointment, proved reliable and stable dosage form with significant anti-fungal efficacy. The formulated ointment might be helpful tool for dermatophytes management.
51. In-vitro Evaluation and Optimization of Sacubitril and Valsartan Floating Tablet using Natural Polymer
Anil K Goyal, Vinesh Kumar
Abstract
Oral systems have become gradually extensive for human consumption because of their numerous advantages, such as formulation efficiency, cost-effectiveness, and patient safety compliance. These systems offer a versatile platform for controlled drug release, allowing precise targeting of absorption site in the gastrointestinal tract. Accomplishing ideal therapeutic results for certain medications often requires precise control of drug release at specific locations within the gastrointestinal tract. In this study, our goal was to create a floating drug delivery system for two vital cardiovascular medications, sacubitril and valsartan. Our specific objectives were to extend floating time, prolong stomach residency, and reduce floating lag time. The strategy involved harnessing the synergistic potential of natural polymers in optimal proportions to enhance drug activity. Following the principles of quality by design (QbD), we systematically explored various formulation factors to optimize the drug delivery system. Analysis of tablet characteristics revealed significant variations in key parameters, such as swelling index, floating lag time (FLT), total floating time (TFT), and drug content for both sacubitril and valsartan. The enhanced formulation (F12) stood out with a remarkable swelling index of 93.4%, a floating lag time of 6.7 seconds, and an impressive total floating time of 12 hours. Furthermore, high drug content percentages were achieved, with sacubitril at 98.70% and valsartan at 94.65%. The successful development and optimization of the floating tablet formulation carry substantial clinical implications. The extended gastric retention, controlled drug release, and high drug content of the optimized formulation suggest enhanced bioavailability and therapeutic efficacy for both sacubitril and valsartan. The prolonged total floating time offers convenience to patients, potentially improving medication adherence in managing cardiovascular diseases. In conclusion, this study highlights the formulation and optimization of floating tablets as a noteworthy advancement in drug delivery technology, promising improved therapeutic outcomes and enhanced patient convenience.
52. Development of Vaginal Tablet of Clotrimazole Prepared by Applying the Concept of Percolatio Threshold
Hardikar S Rajan, Shaikh N M Mustaqeem, Ansari D M Akbar, Peerzade M Yasir
Abstract
Clotrimazole is the drug of choice in the treatment of vulvovaginal candidiasis and belongs to biopharmaceutical classification system (BCS) class IIb. Therefore, it should be presented in appropriate form adopting a suitable formulation approach to ensure its fast and complete release in the vagina. Solid dispersion of clotrimazole was prepared using microcrystalline cellulose as a carrier material after confirming their miscibility into each other by the ‘melting point depression’ method. Vaginal tablets of the solid dispersion of clotrimazole were prepared by direct compression using co-processed crospovidone as a novel disintegrant (1.5% w/w) to ensure fast disintegration of the tablet. Co-processed crospovidone was selected as a novel disintegrant and its proportion in the formulation was decided by applying the concept of percolation threshold. The superior functionality of co-processed crospovidone as a disintegrant was because of its larger pore size i. e., 4.27Ao than the pore size of crospovidone 3.99Ao. The faster ingress of water through the larger pores leads to the fast disintegration of the tablet. Rapid release of the drug from the disintegrated tablet dosage form was confirmed by performing in-vitro antifungal studies. The statistical analysis of the data obtained after applying the student ‘t’ test indicated that there was a difference in the means of zone of inhibitions between the tablets of optimized composition and the tablets the plain clotrimazole at p<0.5.
53. Box-Behnken Design for Formulation, Characterization and In-vivo Antidiabetic Activity of Pioglitazone Loaded Nanostructured Lipid Carriers
Modekar SD, Mohale DS, Kochar NI, Chandewar AV
Abstract
This study employs a 23 full factorial design in the design of experiment (DOE) technique to assess the impact of critical quality attributes (CQAs) on critical process parameters (CPPs) in the formulation of pioglitazone (PGZ) loaded nanostructured lipid carriers (NLCs). The three chosen CPPs are the quantity of liquid lipid (Captex 300), the proportion of solid lipid (Glyceryl Palmitostearate), and the amount of surfactant. The CQAs evaluated are entrapment efficiency (%EE) and particle size. The PGZ-loaded NLCs are prepared through a solvent injection method. The lipid phase, consisting of dissolved medication and lipids in ethanol, is rapidly injected into an aqueous phase containing the surfactant. The resulting dispersion undergoes analysis for entrapment effectiveness and particle size. Additionally, the in-vivo antidiabetic activity of the optimal formulation is examined using diabetic rat models induced by streptozotocin (STZ), and relevant biochemical parameters are assessed. The results demonstrate that the proposed PGZ-loaded NLCs exhibit superior antidiabetic activity and favorable physicochemical characteristics compared to free PGZ. This study provides valuable insights into the formulation and characterization of NLCs for enhanced diabetes management, emphasizing their potential as a promising delivery system to improve the therapeutic efficacy of antidiabetic drugs like PGZ.
54. In-silico Study of Methyl Beta D-xylopyranoside: A Spectroscopically Screened Small Molecule from Aganosma dichotoma
Sreya Kosanam, Rajeshwari Pasupula
Abstract
Background: To develop scientific evidence of unexplored traditional plants.
Methods: Standardization of leaf powder was done as per World Health Organization (WHO) guidelines, followed by fourier-transform infrared spectroscopy (FTIR) analysis to identify basic phytoconstituents. Preliminary phytochemical analysis and spectroscopic analysis was done to validate the identified phytoconstituents. Molecular docking was done to identify a small molecule, methy beta D-xylopyranoside.
Results: The air-dried leaves and barks were powdered and subjected to extraction based on the polarity of solvents through soxhlation, namely, methanol, ethanol, and chloroform, to obtain four different extracts. Further, preliminary phytochemical tests and qualitative determination of the different biologically active compounds from leave powder Aganosma dichotoma using FTIR revealed the presence of different phytoconstituents. And gas chromatography-mass spectrometry of crude extracts revealed different chemical entities with varying quantities and followed by in-silico molecular docking studies of hub genes against the photochemical small molecule. Thus, the identification of different biologically active compounds in the extracts of leaves A. dichotoma warrants further biological and pharmacological studies.
Conclusion: Small molecules identified from A. dichotoma have robust activity against myocardial infarction, but need to be validated through in-vitro and in-vivo studies.
Methods: Standardization of leaf powder was done as per World Health Organization (WHO) guidelines, followed by fourier-transform infrared spectroscopy (FTIR) analysis to identify basic phytoconstituents. Preliminary phytochemical analysis and spectroscopic analysis was done to validate the identified phytoconstituents. Molecular docking was done to identify a small molecule, methy beta D-xylopyranoside.
Results: The air-dried leaves and barks were powdered and subjected to extraction based on the polarity of solvents through soxhlation, namely, methanol, ethanol, and chloroform, to obtain four different extracts. Further, preliminary phytochemical tests and qualitative determination of the different biologically active compounds from leave powder Aganosma dichotoma using FTIR revealed the presence of different phytoconstituents. And gas chromatography-mass spectrometry of crude extracts revealed different chemical entities with varying quantities and followed by in-silico molecular docking studies of hub genes against the photochemical small molecule. Thus, the identification of different biologically active compounds in the extracts of leaves A. dichotoma warrants further biological and pharmacological studies.
Conclusion: Small molecules identified from A. dichotoma have robust activity against myocardial infarction, but need to be validated through in-vitro and in-vivo studies.
55. Formulation Development of Mucoadhesive Tablets for Treatment of Hypertension using Losartan Potassium
Ghanshyam M Chavan, Jyothirmayee Devineni, Dhruv Dev, Abhay R Shirode, P S Minhas
Abstract
Controlled-release losartan potassium incorporated bucccoadhesive tablets were prepared using guar gum and hydroxy propyl methylcellulose K4M (HPMC K4M). The polymers had demonstrated considerable influence for all reactions. Ethylcellulose, a naturally impermeable material, was employed as a backing layer. The direct compression approach was used to create nine distinct losartan potassium formulations. Drug and polymer compatibility was determined through preformulation research utilizing fourier transform infrared (FTIR) spectroscopy. Buccoadhesive tablets were evaluated by swelling, bioadhesive characteristics, pH and in-vitro drug dissolution. The bioadhesive strength of guar gum was found to be greater than that of HPMC K4M. The swelling effect provided by both polymers was adequate. All formulations were judged to have an adequate surface pH, with values falling between 7 and 5, suggesting no discomfort to the buccal cavity. Ex-vivo residence times ranging from 7.2 to >10 hours for all tablets tested demonstrated a high degree of adhesion. The improved formulation follows Fickian diffusion release process. The optimized formulation underwent a stability investigation in accordance with International Council for Harmonisation (ICH) criteria, and no significant changes were found.
56. Evaluation of Insulin Loaded Microspheres for Oral Delivery
Rinki Vishwakarma, Harshal Tare
Abstract
Microsphere-based colon-specific medication delivery devices should improve bioactive chemical administration and residence periods. In the first step, insulin microspheres were made using Eudragit RL 100 and L-100 by quasi-emulsion solvent diffusion. Microspheres were made since prior research showed that colon tissue macrophages could take up drug carrier systems with a molecular weight of 956 m or less. The uptake process allows accurate medication delivery to the specified site. Microspheres’ longer residence time than conventional drug delivery methods may allow dosage reduction and therapeutic efficacy. Because microspheres are permeable, they may be compacted and used to make stronger tablets. Thus, the CPDRS1 formulation performs well, enabling insulin delivery via an anti-diabetic microsphere. Drug-polymer ratio affects microsphere size and form. Variations in emulsifying agent amounts affect microsphere sizes and manufacturing yield. Using appropriate polymer and emulsification agent concentrations improves insulin-loaded Eudrajit L microsphere (Eudrajit RL) formulation and manufacturing yield.
57. Design and Development of Insulin Loaded Microspheres for Oral Delivery
Rinki Vishwakarma, Harshal Tare, Sachin K Jain
Abstract
Protease inhibitor-encapsulated human insulin microspheres were developed and evaluated in this research in order to determine the optimal formulation. Manufacturing human insulin microspheres involved coating them with eudragit S-100, stabilizing them with polyvinyl alcohol, and evaporating the solvent from w/o/w multiple emulsions. Excellent encapsulation efficiency and pH-dependent controlled release were demonstrated by human insulin-loaded eudragit L-100 microspheres with a protease inhibitor. This helped encapsulate and transfer insulin to the best absorption zone. Thus, insulin absorption and physiological response increased. Thus, insulin formulations enhance efficacy, making microsphere insulin injection more efficient as a diabetic treatment. Drug-polymer ratio affects microsphere size and form. The effect of emulsifying agent amount on microsphere size and manufacturing yield. Eudrajit RL, microspheres loaded with insulin, are more successfully formulated and manufactured at optimal concentrations of polymer and emulsifying agent.
58. Extraction and Characterization of Okra and Almond Gum as a Pharmaceutical Aid
SR Chaudhari, UR Dhuppad
Abstract
This study centers on the retrieval and analysis of almond gum and okra for their possible use as medicinal additives. Various measures were used to evaluate the extracted gum, including micrometric analyses, flow properties, organoleptic qualities, swelling index, ash value, Carr’s index, and Hausner ratio. Extracted okra gum had outstanding flow properties, as shown by its total ash content of 0.56% w/w, Carr’s index of 71.10%, and Hausner’s ratio of 3.46. The measured pH value was 6.9. Although the gum could not dissolve in organic solvents, it was able to dissolve in warm water. This indicates that the formulation of the chemical may be used without experiencing any negative consequences.
59. Isolation of Gum from Tamarind and Fenugreek Plants and Its Evaluation as Pharmaceutical Excipients
SR Chaudhari, UR Dhuppad
Abstract
In contemporary pharmaceutical dosage forms, a variety of auxiliary substances are combined with active compounds to aid in production and achieve the intended effects of the active components. Plant gum is a widely recognized polysaccharide within the pharmaceutical industry, performing an array of functions including stabilizing, disintegrating, suspending, emulsifying, and gelling. Naturally occurring gum is preferred over commercially produced gum due to its affordability, emollient properties, non-irritating nature, natural composition, and lack of toxicity. The costly nature, hazardous properties, contribution to environmental contamination during production, reliance on non-renewable resources, potential adverse effects, and low patient adherence are all drawbacks of synthetic polymers. Gum exhibits considerable potential as an innovative drug delivery system (NDDS) in conjunction with a variety of pharmacological formulations. The advancements achieved in the application of natural polysaccharides, mucilages, and pectins within the domain of medicinal sciences are examined in this research article.
60. Design and Discovery of Silmitasertib-based Drugs as a Potential Casein Kinase II Inhibitor for Cholangiocarcinoma through Hybrid In-silico Ligand-Based Virtual Screening with Molecular Docking Method
Pravin Tajane, Nandu Kayande, Avinash Bhosale, Sumit Deore, Harshal Tare
Abstract
This research investigates the design and discovery of silmitasertib-based drugs as potential inhibitors of casein kinase II (CK2) for cholangiocarcinoma using hybrid in-silico methods. The study employs a two-fold approach, including ligand-based virtual screening and molecular docking, to assess the inhibitory potential of silmitasertib-based compounds. The ligand-based virtual screening involves the construction of a diverse compound library, followed by energy minimization and conformational analysis, revealing a set of compounds with varied similarities to silmitasertib. In parallel, the CK2 model undergoes meticulous selection, validation, and refinement through PDB REDO, showcasing significant improvements in model quality. Molecular docking results highlight promising candidates, with N-(2, 4, 6-trimethylphenyl) phenanthridin-6-amine (MCULE-1492185963-0) emerging as a lead compound with superior binding characteristics compared to silmitasertib. This hybrid in-silico approach demonstrates the potential of silmitasertib-based compounds as CK2 inhibitors for cholangiocarcinoma and identifies a lead compound for further experimental validation. The findings contribute valuable insights to the design of novel drugs for cholangiocarcinoma treatment, setting the stage for future experimental and clinical investigations.
61. Design, Development and Physicochemical Evaluation of Effervescent Tablets of Antihistamine Drug
Vikrant Nikam, Avinash Bhosale
Abstract
Purpose: Effervescent bilastine tablets were the focus of this investigation because of their ease of administration and the fact that some patients, especially younger ones or those with impaired swallowing abilities, have trouble ingesting oral dosage forms.
Methods: Using the wet granulation process, 20 mg of effervescent bilastine tablets were produced. Pre-compression properties assessed for powder blend and granule combination. Here are some post-compression properties of the tablets that were examined: friability, hardness, drug content, pH, dissolution time, content uniformity, water content, X-ray, and Differential scanning calorimetry (DSC). We also measured carbon dioxide content and effervescence duration. To get the greatest results, we looked for effervescent systems that dissolved quickly in water and had the right properties before and after compression.
Results: Based on their physicochemical properties, F2 formulations were determined to be best formulations, and the results demonstrated that the wet granulation process had greater flowability.
Conclusion: Sweeteners such as mannitol, sodium saccharine, methylparaben, and citric acid were chosen for this investigation, along with sodium bicarbonate. If you want to hide the bitter flavor of bilastine, sodium saccharine is your best bet. From a physicochemical and physical property standpoint, the wet granulation process outshines the alternatives.
Methods: Using the wet granulation process, 20 mg of effervescent bilastine tablets were produced. Pre-compression properties assessed for powder blend and granule combination. Here are some post-compression properties of the tablets that were examined: friability, hardness, drug content, pH, dissolution time, content uniformity, water content, X-ray, and Differential scanning calorimetry (DSC). We also measured carbon dioxide content and effervescence duration. To get the greatest results, we looked for effervescent systems that dissolved quickly in water and had the right properties before and after compression.
Results: Based on their physicochemical properties, F2 formulations were determined to be best formulations, and the results demonstrated that the wet granulation process had greater flowability.
Conclusion: Sweeteners such as mannitol, sodium saccharine, methylparaben, and citric acid were chosen for this investigation, along with sodium bicarbonate. If you want to hide the bitter flavor of bilastine, sodium saccharine is your best bet. From a physicochemical and physical property standpoint, the wet granulation process outshines the alternatives.
62. Preparation and Evaluation of PLGA-based Nanoparticles
Ram K Choudhary, Kandukuri A Kumar, Srividya Kommineni, Minal Narkhede, Jyothirmayee Devineni
Abstract
The current study aimed to increase the stability and therapeutic efficacy of the antitubercular medication rifampicin by reducing or preventing its breakdown in the stomach pH state. Ascorbic acid was used as an antioxidant in the preparation of rifampicin-loaded Poly(lactic-co-glycolic acid) (PLGA) nanoparticles for the investigation. A multistep emulsion process was used to create dig-laden nanoparticles, and different techniques were then used to assess the final product. Ten different kinds of formulations were created for this study. According to the study’s findings, ascorbic acid can increase rifampicin’s stability and bioavailability by reducing its breakdown in acidic pH conditions. The results also show that changing the ascorbic acid concentration makes a statistically important difference in the way the medicine breaks down.
63. Formulation and Evaluation of Mouth Dissolving Tablet of Biperiden HCL for Treatments of Parkinson’s Disease
Mahavir K Sharma, Rupa Singh, Tejas K Patel, Bhavik Jani, Dhairyashri Kher
Abstract
Seven formulations were developed using superdisintegrating substances like sodium starch glycolate, crospovidone, and cross-carmellose sodium at different concentrations. Three batches were created by employing varying concentrations of the super disintegration approach, utilizing sodium starch glycolate as the superdisintegrating agent. The batches underwent evaluation regarding sensory characteristics, firmness, breakability, weight consistency, disintegration time in a simulated environment, time is taken for wetting, laboratory tests on drug release within a controlled environment, and assessments of product stability. Fourier transform infrared spectroscopy (FTIR) studies confirmed the absence of drug-excipient interactions. In this examination, mouth-dissolve tablets of biperiden HCL were successfully ready with favorable parameters, including organoleptic properties, hardness (3.2 kg/cm3), friability (0.23%), weight variation (100 mg), disintegration time within a controlled laboratory environment (17 seconds), wetting time (11 seconds), and in-vitro drug release studies (99.80%). The study concluded that the biperiden hydrochloride mouth-dissolving tablet was effectively formulated using the direct compression method, demonstrating improved patient compliance.
64. Donepezil and Quercetin Simultaneous Estimation in Rat Plasma Using Developed Bioanalytical HPLC Method: Relevance in Pharmacokinetic Studies
D Sonawane, V Pokharkar
Abstract
The objective of this investigation was to create and apply a reliable reverse phase high performance liquid chromatography (RP-HPLC) technique for the concurrent measurement of donepezil (DPZ) and quercetin (QT) in rat blood samples for pharmacokinetic research. This is the first publication that introduces a method for DPZ and QT simultaneous determination in rat plasma by high-performance liquid chromatography (HPLC). Using a mobile phase of methanol and HPLC grade water (pH 2.8; adjusted with 0.05% v/v orthophosphoric acid) 45:55 v/v with 2-3 drops of triethylamine (TEA) in an isocratic elution mode at flow rate of 1.0ml/min, DPZ and QT were successfully separated chromatographically on a Hypersil gold C-18 column (250 mm × 4.6 mm, 5μm). The retention time for DPZ and QT was observed to be 6.3 and 12.3 minutes and was detected at an isobestic wavelength of 273 nm using a UV detector. The method was shown to be precise (%RSD < 2%), accurate (96–100%), and specific for the simultaneous detection of DPZ and QT. Several freeze-thaw cycles of the treated plasma samples did not significantly affect the analyte’s stability. The method’s applicability was subsequently confirmed through an oral pharmacokinetic investigation in rats. Since the results were deemed trustworthy, the validated RP-HPLC method may be used to simultaneously detect and quantify both drugs. The method worked well for evaluating the pharmacokinetic characteristics in wistar rats following a single oral dose of 5 mg/kg of QT and 10 mg/kg of DPZ. It is well acknowledged that the chromatographic process is straightforward, robust, accurate, exact, and repeatable.
65. Formulation and Evaluation of Gastro Retentive Floating Tablet of Cetirizine Hydrochloride using Linseed Mucilageas Polymer
Manjusha A. Bhange, Mahendra C. Gunde, Shubhada B. Ukey, Pravinkumar B. Suruse
Abstract
This study’s objectives were to create and assess gastric-floating controlled release tablets employing flaxseed mucilage as polymer. Linseed mucilage was isolated from Linum usitatissum seeds. Compatibility studies were performed on drug and other excipients. This study employed individual and mixed polymers to manufacture floating CH tablets. The polymers HPMC, MCC, and linseed mucilage were utilized in various ratios. Five distinct formulae were created (F1-F5 by powder a direct compression method. Formulations was tested for various parameters including in-vitro drug release and floating ability. The findings of all evaluation parameters are substantial. With an 8-hour floating time and a medicine release rate of 98.4% at end of the 24 hours, the formulation (F3), including hydroxyl propylmethyl cellulose and Linseed mucilage was shown to be the best.
The current study focuses on the formulation of floating tablets using a natural polymer as a binder (Linseed mucilage). However, in-vivo experiments are still needed to establish the efficacy of the manufactured CH floating tablets.
66. Synthesis, Pharmacological Evaluation, and Docking Studies Of Ethyl Coumarilate Derivatives as Potential Anti-bladder Cancer in a Mouse Model
A K Khalaf, O A Omar
Abstract
In our study, we performed the green synthesis of twenty-one new organic compounds derived from ethyl coumarilate and treated with ammonia derivatives, such as hydrazine, phenylhydrazine, semicarbazide, and thiosemicarbazide. These reactions yielded a five-member ring incorporating benzofuran, and similar reactions with urea, thiourea, and guanidine produced a six-member ring incorporating benzofuran. All compounds were synthesized in our previous work1 and evaluated for their effects on bladder cancer in experimental mice using docking analysis. Among these twenty-one compounds, we selected five based on docking program analysis. These five compounds showed the highest negative ΔG value, indicating strong interaction and effective inhibition of three important enzymes, TNF-alpha, COX-2, and IL-6, responsible for inflammation in the body. The results demonstrated that the prepared organic compounds exhibited robust binding and inhibition towards these enzymes. Subsequently, a study was conducted on 85 male mice, divided equally into seven groups, with each group consisting of five mice. The control group received a normal diet and distilled water, while groups 2 to 7 were administered doses of N-butyl-N-(4-hydroxybutyl) nitrosamine (BBN) at a dose of 0.05% in drinking water for four months. Groups 3 to 7 received intraperitoneal injections of compounds A, B, C, D, and E at three different doses (0.5-1-1.5 mg/kg) for 21 days. Unfortunately, all the mice in group 7 died when this compound was used, possibly due to its high dose. Biochemical results revealed that compound B exhibited intriguing anticancer activity, reducing TNF-alpha levels and inhibiting COX-2 and IL-6 enzymes, reversing bladder cancer injury. Moreover, histopathological examination indicated significant improvement, with the complete disappearance of cancer in the bladder caused by compound B.
67. A Novel Deep Learning Model for Drug-Drug Interactions
Ali K. A. Raheem, Ban N. Dhannoon
Abstract
Drug-drug interactions (DDIs) can lead to adverse events and compromised treatment efficacy, emphasizing the need for accurate prediction and understanding of these interactions. This paper proposes a novel approach for DDI prediction using two separate message-passing neural networks (MPNN) models, each focused on one drug in a pair. By capturing each drug’s unique characteristics and interactions, the proposed method aims to improve the accuracy of DDI prediction. The results of the individual MPNN models are then combined to integrate the information from both drugs and their molecular features. Evaluating the proposed method on a comprehensive dataset, we demonstrate its superior performance with an accuracy of 0.95, an area under the curve (AUC) of 0.99, and an F1-score of 0.88. These results highlight the effectiveness of the proposed approach in accurately identifying potential drug-drug interactions. Using two separate MPNN models offers a flexible framework for capturing drug characteristics and interactions, contributing to our understanding of DDIs. The findings of this study have significant implications for patient safety and personalized medicine, potentially optimizing treatment outcomes by preventing adverse events. Further research and validation on larger datasets and real-world scenarios are necessary to fully explore this approach’s generalizability and practicality.
68. Therapeutic and Anticancer Properties of Nerium oleander– A Poison as Medicine
Akhila R James, Sakthidasan Jayaprakash
Abstract
Cancer is a heterogeneous disease and ranks among the most pressing health concerns faced by humans and requires a proactive treatment approach. Plants are a rich source of compounds and offer a promising avenue for cancer research. Chemotherapy has so far been effective, but it comes with some very unpleasant side effects. Nerium oleander, an evergreen plant cultivated throughout the world, has many metabolites, including cardiac glycosides, phenols, saponins and terpenoids. The plant and its derivatives have been an essential component of traditional medicine for treating several ailments from the beginning of time, notably cancer, diabetes mellitus, asthma, and cardiac disease. However, the scientific community has not gone much further into the information. This review aims to understand the therapeutic applications of N. oleander, focusing on cancer. The leaf extract, anvirzel and PBI-05204 has entered clinical trials and other derivates like oleandrin and breast in are still under in-vitro and in-vivo studies. In order to combat cancer, the plant operates on several cancer-related signaling pathways, including the Akt mTOR downstream pathway.
69. Herbal Nano Formulations for Topical Drug Delivery: Prospective for Multiple Skin Disorders
Jyoti Arsude, Machindra Chavan, Sumit Joshi, Shriram Pethakar, Ganesh Dama
Abstract
Dermatological conditions exert their influence across the globe, encompassing a broad spectrum of maladies ranging from commonplace afflictions such as acne and eczema to more formidable challenges like psoriasis and cutaneous malignancies. The realm of topical drug delivery stands as a pivotal modality in the domain of dermatology, proffering precise and minimally invasive therapeutic avenues. In recent times, the fusion of herbal curatives with the marvels of nanotechnology has surfaced as a pioneering strategy.
This comprehensive review undertakes an exploration of the amalgamation of herbal constituents within nano-sized drug carriers, catering to the domain of topical applications, with a particular emphasis on their potential to address a myriad of dermatological conditions. The outset of this review is dedicated to the elucidation of the meticulous criteria governing the selection of herbal components and the underpinning rationale behind their integration into nanoscale formulations, thereby spotlighting the rich heritage of botanical remedies intrinsic to traditional medical practices.
Subsequently, meticulous scrutiny of nanotechnology’s role in the domain of cutaneous drug conveyance ensues, elucidating diverse nanoparticle typologies and their respective mechanisms of therapeutic action. The crux of this review centers upon the manifold approaches of herbal nanoformulations, encompassing lipid-based matrices, polymer-driven carriers, liposomal constructs, micellar entities, nanoemulsions, solid lipid nanoparticles, dendritic platforms, and nanogels. For each of these approaches, illustrative case studies are presented, thereby affording perspicacity to their bespoke utility in the management of diverse dermatological conditions.
In the ensuing discourse, the potential of herbal nanoformulations in the amelioration of acne, mitigation of psoriatic manifestations, alleviation of eczematous distress, acceleration of wound healing, attenuation of scar formation, and prophylaxis against cutaneous neoplasia is subjected to meticulous examination. The purview extends to the discerning analysis of clinical trials and the practice informed by empirical evidence, thereby shedding illuminative insight into the safety and efficacy profiles of these innovative formulations.
Concomitantly, the challenges entailing regulatory adherence, standardization, and the enforcement of rigorous quality control are thoughtfully addressed, with a subsequent contemplation of the trajectories shaping the future of this burgeoning discipline. In summation, this review underscores the intrinsic value of interdisciplinary synergism and underscores the compelling imperative for relentless research efforts that propel herbal nanoformulations to the vanguard of mainstream dermatological therapeutics. In doing so, a new epoch in the management of cutaneous disorders is heralded, one that promises safe, efficacious, and patient-centric interventions, thus ushering in a transformative era in the domain of dermatological care.
This comprehensive review undertakes an exploration of the amalgamation of herbal constituents within nano-sized drug carriers, catering to the domain of topical applications, with a particular emphasis on their potential to address a myriad of dermatological conditions. The outset of this review is dedicated to the elucidation of the meticulous criteria governing the selection of herbal components and the underpinning rationale behind their integration into nanoscale formulations, thereby spotlighting the rich heritage of botanical remedies intrinsic to traditional medical practices.
Subsequently, meticulous scrutiny of nanotechnology’s role in the domain of cutaneous drug conveyance ensues, elucidating diverse nanoparticle typologies and their respective mechanisms of therapeutic action. The crux of this review centers upon the manifold approaches of herbal nanoformulations, encompassing lipid-based matrices, polymer-driven carriers, liposomal constructs, micellar entities, nanoemulsions, solid lipid nanoparticles, dendritic platforms, and nanogels. For each of these approaches, illustrative case studies are presented, thereby affording perspicacity to their bespoke utility in the management of diverse dermatological conditions.
In the ensuing discourse, the potential of herbal nanoformulations in the amelioration of acne, mitigation of psoriatic manifestations, alleviation of eczematous distress, acceleration of wound healing, attenuation of scar formation, and prophylaxis against cutaneous neoplasia is subjected to meticulous examination. The purview extends to the discerning analysis of clinical trials and the practice informed by empirical evidence, thereby shedding illuminative insight into the safety and efficacy profiles of these innovative formulations.
Concomitantly, the challenges entailing regulatory adherence, standardization, and the enforcement of rigorous quality control are thoughtfully addressed, with a subsequent contemplation of the trajectories shaping the future of this burgeoning discipline. In summation, this review underscores the intrinsic value of interdisciplinary synergism and underscores the compelling imperative for relentless research efforts that propel herbal nanoformulations to the vanguard of mainstream dermatological therapeutics. In doing so, a new epoch in the management of cutaneous disorders is heralded, one that promises safe, efficacious, and patient-centric interventions, thus ushering in a transformative era in the domain of dermatological care.
70. The Role of Artificial Intelligence in the Pharmaceutical Sector: A Comprehensive Analysis of its Application from the Discovery Phase to Industrial Implementation
Prajwal S Shinde, Ashish Y Pawar, Swati G Talele
Abstract
The incorporation of artificial intelligence (AI) technology into the pharmaceutical sector is a groundbreaking revolution, promising to enhance drug development significantly by boosting speed, efficiency, and effectiveness. This transformative journey encompasses several key facets, notably the sophisticated analysis of complex data, the optimization of drug delivery systems, the acceleration of drug discovery, the identification of valuable biomarkers and drug candidates, and the fine-tuning of treatment outcomes. Beyond these crucial strides, AI is reshaping healthcare at large, elevating decision-making processes, and deepening our understanding of diseases and pharmaceuticals. The broader domains within this AI-driven transformation encompass themes such as “Revolutionizing Pharmaceutical Product Development Through AI,” where AI platforms like the Chemputer successfully synthesize compounds and estimate granulation completion times, improving production efficiency. In “Transforming Pharmaceutical Manufacturing with AI, “AI optimizes manufacturing processes, further enhancing efficiency.” Enhancing Clinical Trial Design Through AI” harnesses AI to improve patient selection and adherence, utilizing genome and exposome profiles for precise and efficient clinical trials. AI also proves valuable in preclinical phases, predicting lead compounds. Moreover, AI extends its influence to brand recognition and market positioning of pharmaceutical products, leveraging technology and e-commerce platforms for distinct product identities and effective marketing strategies. In “Convergence of AI and Nanomedicine,” AI delves into complex formulation development, optimizing drug delivery methods via molecular analysis and simulation tools. Furthermore, AI’s role in addressing challenges in the pharmaceutical market, such as reducing financial burdens and risks related to virtual screening, is pivotal. The sector’s substantial growth and its integration into pharmaceutical companies’ strategies through collaborations signify a promising future for AI in healthcare. In summary, the incorporation of AI in the pharmaceutical industry holds immense potential for enhancing production processes, clinical trial design, market positioning, nanomedicine, and overall industry efficiency. These collective advancements mark a transformative era in pharmaceutical innovation and patient care.
71. Molecular and Cellular Expressions in Breast Cancer Responsible for Drug Resistance
Surendra Agrawal, Pravina Gurjar, Deepak Khobragade
Abstract
Breast cancer continues to be a prevalent and highly lethal cancer affecting women globally. Despite significant advancements in early detection and the development of specific therapeutic approaches, the issue of medication resistance remains a prominent challenge in managing this intricate ailment. The study offers a comprehensive analysis of the mechanisms behind the development of treatment resistance in breast cancer cells. The objective of this study is to provide a comprehensive understanding of the molecular and cellular mechanisms behind the occurrence of therapeutic ineffectiveness. This study elucidates several molecular subtypes of breast cancer and their pharmacological responses. The significance of estrogen receptor (ER), progesterone receptor (PR), and human epidermal growth factor receptor 2 (HER2) in the development of treatment resistance is emphasized. Additional research on the intricacies of innate and acquired drug resistance mechanisms, including genetic modifications, tumor heterogeneity, and the presence of cancer stem cells, has shed light on the multifaceted nature of drug resistance and its dynamic evolution throughout treatment. Furthermore, this study provides a comprehensive analysis of the impact of microenvironmental variables, including hypoxia, immune evasion, and tumor-stroma connections, on the development of drug resistance. The investigation of the interplay between tumor suppressors and oncogenes in the emergence of drug resistance is now underway, yielding valuable insights into prospective targets for therapeutic intervention.
Additionally, this study examines the limitations associated with conventional chemotherapy, endocrine therapies, and targeted medicines, while elucidating the mechanisms underlying treatment resistance and proposing potential strategies to overcome it. Emerging therapies like immunotherapies, epigenetic modulators, and new drug delivery methods are looked at to see if they have the potential to get around mechanisms of resistance and improve patient outcomes. This review aims to give clinicians, researchers, and other healthcare workers a full picture of breast cancer’s complex drug resistance mechanisms. By figuring out the molecular complexities and signaling pathways that lead to treatment resistance, we aim to speed up the development of new therapeutic approaches and personalized interventions. This will bring us closer to the long-awaited goal of beating drug resistance and making breast cancer a manageable, treatable condition.
72. Cubosomes: Recent Developments and Applications from a Global Perspective
Rakesh Mishra, Akash Aher, Tanaji Nandgude, Keshav More, Anuja Kolsure
Abstract
Liquid crystalline cubosomes are self-assembly of aqueous lipid and surfactant mixture. They are discrete and sub-micron in size. It is an innovative lipid-based nanosystem resembling well-known vesicular systems including niosomes and liposomes. Cubic phases incorporate lipophobic, amphiphilic and hydrophilic, components through the utilization of a rounded bi-continuous lipid bilayer and water channels. Cubosomes contain lipids such as phytantriol (PHYT) and glycerol monooleate (GMO) which are amphiphilic in nature that are diffused in water and structured in 3-D as a “honeycomb” structure with suitable stabilizer (Poloxamer 407). Cubosomes are generated by mostly two techniques i.e., top-down, and bottom-up methods. UV spectrophotometer, X-ray scattering, transmission electron microscopy, and photon correlation spectroscopy are used to characterize and evaluate cubosomes. They are commonly used in the administration of oral, ophthalmic, transdermal, and chemotherapeutic drugs. The liquid crystalline phase and bicontinuous cubic form nanoparticles are thoroughly discussed in this paper. In the current review search criterion used parameters affecting cubosomes bi-continuous lipid bilayer by top-down and bottom-up methods mostly. The sources referred from peer-reviewed recognized journals. Keywords used as filters were cubosomes, amphiphilic lipids, top-down, bottom-up, bicontinuous, GMO, and phytantriol (PHYT). For the purpose of a comprehensive update literature review over a range (1976–2023) has been conducted on the recent developments cubosomes system.
73. Therapeutic Implementation for Hyperpigmentation and Anti-aging: A Cosmeceutical Approach
Jajnadatta Panda, Abhisek Pal, Pritipadma Panda, Archana Panigrahy
Abstract
Nowadays the most preferred substance to glow skin surface by cosmeceutical products for the aged population and hyperpigmentation cases. These type of skin queries are seen in different environmental conditions including pollution, and radiation. The skin care industries are developing cosmetic products by using natural and synthetic ingredients which is biodegradable and compatible with the skin layer. Cosmetic products currently show drug-like profits because it contain vitamins, antioxidants, essential oils, phytochemical constituents, and enzymes. Cosmo-pharmaceutical products were developing rapidly to avoid skin aging or hypo/hyperpigmentation. The melanocyte or melanin is the main reason for this factor. Selecting natural extracts or resources helps to increase the therapeutic effect and reduces toxicity. The reviewer and researcher found that the term cosmeceutical, skin glowing agent, or hyperpigmentation is widely used in various treatments of melasma, and post-inflammatory hyperpigmentation. The cosmeceutical carefully preclinical and clinical evaluation studies were carried out for safety, and efficacy and no other adverse reactions were shown. Therefore the dermatologist can only provide accurate information to the patient. For the fastest growing area of research and development for a novel formulation of micro-emulsion, nano-emulsion, liposomes, niosomes, solid lipid nanoparticles and nanospheres. These nanocarriers help to incorporate into the formulation and enhance the skin permeation, high stability, and customized release properties with targeting and higher efficacy. The quality of cosmetics and cosmeceuticals is based on evidence of in-vivo and in-vitro efficacy and therapeutic effect.
74. Unlocking the Potential of In-silico Approaches: Drug Development and Vaccine Design
Priya V Nikam, Sanjay Kumar, Sachinkumar D Gunjal, Mrunalini H Kulkarni, Surya P Singh
Abstract
Unmatched in its field, bioinformatics combines several academic fields such as statistics, computer science, mathematics, and biology to create state-of-the-art techniques for biological data retrieval, storage, and analysis that lead to a thorough understanding of the biological world. Countless options currently accessible in field of living sciences by the expansion of in-silico biology. Paradigm of life sciences has changed as a result of in-silico technologies, which offer researchers a valuable and affordable way to focus on in-silico techniques like homology modeling, epitope prediction, and molecular docking, which have impacted drug discovery and vaccine design. These techniques also provide previously unheard-of predictions and insights.
75. A Birds Eye View on Solid Lipid Nanoparticles and Applications in Drug Delivery System
Anita H Pagar, Ashish Y Pawar
Abstract
Solid lipid nanoparticles (SLN) might provide fresh opportunities for treating challenging ailments. The SLN were established in the 1990s to replace emulsions and liposomes, in addition to polymeric nanoparticles (NP) as carrier systems. SLN are wet cohesive dispersions with solid biodegradable lipids as their matrices. Drug delivery techniques called SLN use both liquid and solid lipids as their primary matrices. It was demonstrated that SLNs have several benefits over conventional carriers for drug therapy, a longer half-life, tissue-targeted administration, higher permeability, enhanced bioavailability, enhanced solubility, as well as the capacity to enhance storage stability. Because of their exclusive size-dependent characteristics as well as their capability towards incorporating drugs, SLN’s currently a possibility towards designing promising pharmacological prototypes for drug transport as well as targeting. The objective of tailored as well as monitored drug delivery is now unsettling researchers’ interests across the globe, and can be accomplished through the support of SLNs. The present investigation emphasizes SLNs’ numerous characteristics as well as development and evaluation processes, formulation factors, delivery routes, surface changes, toxicity, and biomedical applications.
76. Extrapyramidal Effects of First and Second Generation Antipsychotics: A Review
Sharumathi SM, Bhavatharini S, Rinu MX, Arun KP, Deepalakshmi M
Abstract
Antipsychotics are essential for treating major psychiatric disorders like schizophrenia. Second-generation antipsychotics were developed to reduce the risk of extrapyramidal symptoms (EPS) caused by antipsychotic medications. While second-generation drugs have a lower risk of EPS than first-generation treatments, studies show that they can still cause EPS, with clozapine being the least risky and risperidone the most. A literature search of PubMed and Scopus databases until April 2023 found that high doses, a history of past EPS, comorbidities, and specific second-generation medications can increase the risk of EPS. The choice of a first-generation comparator also influences study findings. Although the prevalence and severity of EPS vary with antipsychotics, these medications have not met expectations in terms of tolerability. EPS is still a clinical issue, even in the era of second-generation antipsychotics. This review offers a concise overview of EPS induced by antipsychotics.
77. Nanogel: Types, Methods of Preparation, Limitation, Evaluation and Application – A Systematic Review
Saloni Srivastava, Supriyo Saha, Vikash Jakhmola
Abstract
Nanogels combine the characteristics of nanomaterials with hydrogels. To meet the expanding demands from various areas, a sizable number of nanogels have been designed and manufactured using the emulsion solvent diffusion nano precipitated method, emulsion evaporation of the solvent method, reverse micellar method and modified diffusion emulsification method. Thermosensitive nanogel, pH-sensitive nanogel, ultrasound-sensitive magnetic response, response to multiple stimuli, chain transfer polymerization, photo-induced crosslinking polymerization and modifications for active targeting are the types of nanogels based on response towards stimuli and polysaccharide, chitosan, pullulan, hyaluronic acid, alginate, cyclodextrin, gum acacia, protein are used to prepare nanogel. Nanogels have considerable potential and novelty within the biomedical sector due to their uniformity, adjustable dimensions, little toxicity, resilience in the presence of serum, and capacity for responsive behavior with a comparatively high drug encapsulation capacity. Nanogels have considerable potential in bioactive substance delivery, organ targeting, and chemotherapy. The article highlighted the preparation, types, evaluation and applicability of nanogel as a targeted delivery system.
78. Overview of Antihypertensive Transdermal Drug Delivery System
Shital Bidkar, Akshada Tandale, Abhishek Meher, Jayant Bidkar, Ganesh Dama
Abstract
In order to boost bioavailability and enhance patient compliance, this review focuses on the antihypertensive action of transdermal patches. Using a transdermal method for administering medication (TDDS), it is possible to administer a systemic medicament via a simple skin patch. Among the most prevalent human diseases is hypertension. There is a strong correlation between hypertension and cardiovascular mortality and morbidity. The evolution of skin science, innovation, and experience that led to these patches began with the earliest written records of human history and continues to this day through with a combination of trial and error, clinical observation, and research evidence. Because it’s a long-term condition, treatment will take a while.
79. Premedication of Ranitidine and the Action of Hypersensitivity Reactions to Paclitaxel
Harsh K Brahmbhatt, Nidhi Patel, Tejas K Patel, Tantul Sarkar
Abstract
Paclitaxel is used asa chemotherapeutic agent for curing various types of cancer. To reduce the hypersensitivity of the chemotherapeutic effect, premedication of antihistaminic drugs like ranitidine, cetirizine, diphenhydramine, fexofenadine and desloratadine are prescribed. The antihistaminic drugs are given as premedication to prevent the formation of hives on the body. Ranitidine can be replaced by another antihistaminic drug which reduces the side effects and increases the efficacy of the drug. Studies were conducted comparing the antihistamine and non-antihistamine groups and tests like the chi-square test, and the Wilcoxon-Mann-Whitney test to determine the extent of hypersensitivity. There are immediate and non-immediate drug hypersensitivity reactions occurring in cells that initiate the allergic reaction. These allergic reactions like flushing, itching, dizziness, nausea, vomiting, swelling, etc lead to affect the respiratory, cardiovascular, gastrointestinal, and other body parts. In this article, the method used for the study of hypersensitivity reaction is specified with the test to determine the allergic reaction on the skin and desensitization of the rapid hypersensitivity of the drug.
80. Ethanopharmacological Activities of Mentha arvensis: An Updated Review
Reshu, Avijit Mazumder, Saumya Das
Abstract
Economical natural menthol is derived from Mentha arvensis Linn (menthol mint) oil. It is an aromatic perennial herb. The leading Mentha producing state in area and production is Uttar Pradesh and India is the leading exporter contributing about 80% of essential oil, menthol crystal and allied products. It is a native herb from the Labiatae family and is most frequently referred to as “pudina”. It has historically been used to treat ischemic heart disease and hypertension. Terpenoids, alcohols and phenolics are just a few of the bioactive substances that have been identified from this plant. These bioactive compounds’ pharmacological activities include antibacterial, neuroprotective, antioxidant, antiulcer, immunomodulatory, antimutagenic, and anti-tumor properties. Studies on Ayurvedic, unani, and other traditional medical systems have also revealed this plant’s pharmacological capabilities. The current article provides a summary of the plant’s general description, phytochemical ingredients, historical context, and pharmacological qualities.
81. Thevetia peruviana: Its Phytochemistry, Traditional and Medicinal Uses, and Pharmacological Activities
V Singh Chauhan, Avijit Mazumder, Shobhini Chandel
Abstract
Thevetin peruviana, a member of the Apocynaceae family, is also known as digoxin, fortunate nut, yellow oleander, and other names. After consumption, Thevetia peruviana plants have the potential to be fatal. In South Asian countries, especially in Sri Lanka and India, T. peruviana is frequently used for international self-harm. Around the world’s tropical and subtropical regions, T. peruviana is a common cause of toxicological emergencies. The entire plant is hazardous due to the presence of several cardiac glycosides, including neriifolin, oleandrin, thevetin A, and thevetin B. Oleander consumption causes hyperkalemia, vomiting, diarrhea, abdominal pain, and all of the above. In the majority of cases, supportive care and the administration of activated charcoal are used in the clinical therapy of either N. oleander or T. peruviana poisoning. T. peruviana-related information is compiled in this article.
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