1. Formulation and Evaluation of Haemocoagulase Gel for Dental Pulp- an
In-vitro study
Swati Karkare, Nilima Thosar, Milind Wagh, Nikita Wagh
Abstract
This study aims to develop a novel hemostatic gel of hemocoagulase, a snake venom-derived serine protease enzyme, by incorporating it into the matrix of bioadhesive polymers to prevent damage due to hemorrhage. Haemocoagulase was combined with polymers Carbopol 940 and HPMC K 100, and these formulations were evaluated for physical properties, efficacy, safety and stability. Batches F3 and F6 were selected for further studies on animal models, which were found to be safe without any skin irritation effect and effective as hemostats with blood clotting times of 1.24 ± 0.007 min and 1.36 ± 0.014 min, respectively, in a rat liver incision model. From this study, it can be suggested that the combination of hemocoagulase with bioadhesive polymer can provide a novel hemostatic tool for controlling bleeding.
2.
In-vitro Antidiabetic Activity of Ethanolic Extract from Khla (Schumannianthus dichotomus Roxb.) Rhizome
Yuttana Sudjaroen, Kanittada Thongkao, Pimporn Thongmuang
Abstract
Thai traditional medicine, rhizome has a bland taste, and after decoction, it is used to reduce body heat and fever and treatment of skin diseases. Recently, the methanolic extract of rhizome had reported the hepatoprotective and hypoglycemic activities in mice. Aims of this study were conducted to determine the nutritional value of rhizome and to evaluate α-glucosidase, and α-amylase inhibitory activities of ethanol extract from the rhizome (KE). The rhizome had a high content of dietary fiber and iron, while it was low in calories, fat, and carbohydrates. Thus, it can become an ingredient of a healthy diet. The total phenolic content of KE contained 229.8 ± 6.23 mg of gallic acid equivalent (GAE)/g. There was strongly inhibited α-glucosidase (IC50 = 0.11 ± 0.03 mg/mL) and comparable with the antidiabetic drug acarbose (IC50 = 0.10 ± 0.03 mg/mL). Therefore, KE was slightly inhibited by α-amylase (IC50 = 0.42 ± 0.05 mg/mL), when compared with acarbose (IC50 = 0.016 ± 0.001 mg/mL). Thus, the phytochemicals of different extracts are necessary to be identified. Therefore, the advance techniques were the limitation of our study.
3.
Microemulsion Drug Delivery of Anti-malarial Formulation
Jaiswal Nilesh, Mehta Parulben
Abstract
Malaria affects millions of people every year, especially in our world. The main treatments are oral antibiotics and vaccines. The rise of the malaria parasite, now resistant to most anti-viral drugs, is causing a global crisis. Furthermore, low water solubility and permeability of both new and old antibiotics cause limited oral bioavailability and non-compliance from patients. Lipid formulations are frequently employed to lessen toxicity, boost solubility, and improve effectiveness. The findings of studies on oral-specific lipophilic drug delivery systems, such as self-emulsifying drug delivery systems, are reviewed in this article. (SEDDS). SEDDS increases the absorption of anti-inflammatory drugs by promoting the formation of liquid emulsions that dissolve the drug in the intestine. However, traditionally used SEDDS are usually in liquid form, administered into the oral cavity, and have poor safety. This article discusses a new solidification process that can be easily and economically scaled up by using existing equipment. This strategy might also increase patient compliance and product stability. Oral SEDDS has a substantial potential influence in the fight against malaria.
4.
Formulation, Development & Evaluation of Mallotus philippensis Extract Loaded NLCS based Nanogel for Psoriasis
Nandini, Hemant KS Yadav, Jasmine, Sanchit Puniani
Abstract
The current study’s objective was to develop and evaluate the potential of Bergenin-loaded nanostructured lipid carriers (NLCs) as a novel topical therapeutic for psoriasis, obtained from
Mallotus philippensis. NLCs loaded with Bergenin were created using a modified Hot-melt emulsification technique, and then Box-Behnken design optimization was performed. The Independent factors were concentration of solid lipid, the concentration of liquid lipid and the concentration of surfactant. Particle size, entrapment efficiency, and drug permeation percentage were the dependent variables. The Bergenin-nano-lipid carriers (NLCs) that has been optimized has a Particle size of 148 ± 0.37 nm, an %Entrapment efficiency of 93.44 ± 0.45%, and a drug permeation percentage was found to be 83.56 ± 0.137. and the zeta potential was – 0.0617 ± 5.53 mV and the polydispersity index (PDI) was 0.30 ± 0.03. Bergenin’s existence within the NLCs was verified by FTIR. The outcomes show that Nanostructured lipid carriers have the ability to deliver Bergenin for topical psoriasis treatment.
5.
Preparation, Characterization and Evaluation of Monosaccharide Tagged Nanostructured Lipid Carriers for Targeting of Etravirine to Macrophagic AIDS Viral Reservoirs
Bala Tripura Sundari, CVS Subramanyam
Abstract
Purpose of the study: The present study aimed to develop and examine monosaccharide-decorated nanoparticles specifically designed for macrophage targeting of etravirine.
Methods: Nanostructured lipid carriers (NLC) were prepared with stearylamine as such or after tagging with mannose and galactose as one of the lipid components of NLC. Prior to synthesis, a docking study was used to analyze the potential for interaction of the stearylamine- sugar conjugates with respective lectin receptors. Mannose and galactose-conjugated stearylamine were separately synthesized. Fourier-transform infrared spectroscopy (FTIR), mass spectrometry (MS) and nuclear magnetic resonance (NMR) studies were used to assess successful reactions. Etravirine-loaded non-targeted nanostructured lipid carriers (NLCs) were synthesized with the emulsification solvent evaporation method and characterized for parameters such as zeta potential,
in-vitro release, entrapment efficiency and particle size. To create targeted nanoparticles, stearylamine was replaced with either of the conjugated lipids in the formulation. For stability, all NLC dispersions were lyophilized.
In-vitro investigations included cellular uptake and cytotoxicity assessments in the RAW 264.7 macrophage cell line. Following intravenous administration of the NLCs in Wistar rats,
in-vivo biodistribution was evaluated.
Results: The docking studies showed good binding potential of both conjugated lipids for respective receptors. Evaluation of synthesized products showed successful conjugation of sugars to stearylamine. The synthesized nanoparticles demonstrated impressive etravirine loading capabilities and exhibited a circular shape with a mean size of approximately 260 nm. Drug release from all NLC formulations persisted for over 24 hours and remained stable after lyophilization.
In-vitro evaluations in the RAW 264.7 macrophage cell line revealed that mannosylated nanoparticles had enhanced uptake when compared to non-targeted and galactosylated counterparts.
In-vivo plasma and tissue distribution studies corroborated the
in-vitro findings, as the mannosylated NLCs displayed a higher distribution into organs with a rich presence of macrophages.
Conclusion: The studies indicate that while sugar tagging of nanoparticles can prove to be an effective strategy for targeting drugs to macrophagic tissue for tackling latent AIDS virus, the choice of sugar is critical.
6.
Box-Behnken Design Optimization of Captopril-Loaded Transferosomes: Formulation and Characterization
Ismail Y, Mrunalini Harish Kulkarni, Yamjala Ganesh Kumar, G Dharmamoorthy
Abstract
This study aimed to overcome the limitations of oral delivery and enhance the permeation of Captopril (CPL) by developing transferosomes. Transferosomes encapsulating CPL were prepared using a thin film hydration method. Seventeen formulations were prepared, varying Soya lecithin, Tween-20, and sonication speed. The formulations were evaluated for vesicle size (VS), polydispersity index (PDI), and entrapment efficiency (EE%). The optimized formulation’s discharge profile was compared with that of the CPL suspension. Transferosomes exhibited VS ranging from 244 to 376 nm and EE% from 65 to 91%, with zeta potentials ranging from -51 to -26 MV.
In-vitro and
ex-vivo permeation studies demonstrated superior drug permeation for transferosomal formulations compared to plain CPL suspension. CPL transferosomes represent a promising delivery system for prolonged and controlled drug discharge, offering potential improvements in hypertension management.
7.
Optimizing Transdermal Patch Design: A Quality by Design Approach for Dysmenorrhea Relief
Sanjay Kumar, Anirudh Singh Deora, Narahari KV, Tanveer Shaikh
Abstract
This study explores the potential of transdermal patches as a systemic delivery system for donepezil (DPZ), aiming to circumvent hepatic first-pass metabolism and mitigate oral administration-associated side effects. DPZ, known for its poor solubility and adverse effects, is formulated into transdermal patches using a matrix-type approach with PVP K30 and HPMC K100 polymers alongside dimethyl sulfoxide as a plasticizer. Through solvent casting on a mercury surface, the patches are prepared and assessed for physical properties and drug-excipient interactions using FTIR analysis. The results demonstrate satisfactory physical characteristics, including appearance, weight variation, and tensile strength. Notably, formulations containing HPMC K100 (400 mg) and PVP K30 (300 mg) exhibit enhanced DPZ discharge, signifying their potential as an effective drug delivery system for mitigating DPZ-associated side effects.
8.
Creation and Expansion of Bioadhesive Transdermal Gel of Levobupivacaine Loaded Nanoparticles for Enhancement of Anesthetic Effect
Ram Kumar Choudhary, Anasuya Patil, Ramesh Abhimanyu Gadekar, G Dharmamoorthy
Abstract
The present research work aimed to prepare a bioadhesive gel containing Levobupivacaine-loaded nanoparticles (NPs) to improve local anesthesia as transdermal patches were patient-friendly and easy to therapy. This study focuses on developing a The NPs were created using the ionotropic gelation method and assessed for particle charge, vesicle size and its distribution, and surface morphology. The improved NPs were incorporated into a gel and evaluated for their physicochemical assets. Among the NPs, NP4 was identified as the best based on its physicochemical properties. The NG-6 bioadhesive gel formulation stood out as the top gel among those tested. The NG-6 gel exhibited superior skin permeation ended 14 hours compared to other NPs. This bioadhesive transdermal gel with Levobupivacaine nanoparticles offers a promising approach to enhancing anesthetic effects.
9.
Investigation of Olive Leaf Polyphenol Extract Loaded Silver Nanoparticle Optimization by Box-Behnken Design
Renganathan A, Srinivasan R
Abstract
Silver nanoparticles (AgNPs) are synthesized and optimized by reducing and stabilizing them with olive leaf extract. The successful synthesis of AgNPs was verified by UV-vis spectroscopy, SEM imaging, and DLS measurements, demonstrating characteristic features such as a surface plasmon resonance peak, spherical morphology, crystalline structure, and narrow size distribution with good stability. Utilizing Box-Behnken Design (BBD), the optimal synthesis conditions were determined, with a silver nitrate concentration of 1 mM, olive leaf extract volume of 10 mL, and reaction time of 60 minutes, yielding AgNPs with desirable properties. Statistical analysis revealed the significant influence of individual variables and their interactions on AgNP characteristics. Lower concentrations of silver nitrate and olive leaf extract led to smaller particle sizes and higher zeta potentials, while longer reaction times resulted in larger particles and lower zeta potentials. Among the experimental runs, Run 11 exhibited the most favorable properties, with 54 nm particle size, -36 mV zeta potential, and an encapsulation efficiency of 92.28%. ANOVA analysis further elucidated the significant effects of synthesis parameters on zeta potential, particle size, and encapsulation efficiency. In conclusion, the optimized formulation obtained through BBD offers a tailored approach for the synthesis of AgNPs with desired properties, suitable for various applications such as biomedical, catalytic, and sensing applications. The comprehensive understanding of synthesis parameters and their effects provided by this study facilitates the rational design of AgNPs for specific applications, enhancing their potential in diverse fields.
10.
Cytoprotective Effects of Phloretin on Long-Term Post-Prandial Hyperglycemia-induced Esophageal Damage in Rats
Neelkanth M Pujari, Mohammad Khushtar, Anuradha Mishra, Deepika Gupta
Abstract
Esophageal damage arises from gastroesophageal reflux disease, where the contents of the stomach and duodenum flow back into the esophagus, causing an inflammatory lesion. Phloretin, a phytoconstituent classified as a flavonoid possessing both nutritional and medicinal properties, was the focus of this study. The experiment aimed to investigate the impact of phloretin on experimental esophagitis in albino rats. Rats in various groups underwent the induction of esophagitis through the administration of a Fructose solution (10%) and indomethacin (5mg/Kg). The resulting hyperglycemia from regular Fructose solution intake over 28 days was assessed. After sacrifice, the rats were evaluated for the esophagitis index. Additionally, esophageal tissues underwent further analysis for oxidative stress parameters, including TBARS, SOD, Catalase and GSH. Treatment with phloretin demonstrated a significant inhibition of the esophagitis index. Furthermore, phloretin contributed to the restoration of altered levels of oxidative stress parameters back to normal.
11.
Chrysin Embedded Metal Organic Framework for Anticancer Drug Delivery
VK Patil, JK Patel, AK Patel
Abstract
Metal-organic frameworks (MOFs) have garnered significant attention in the field of cancer drug delivery owing to their porosity, high drug-loading capacity, and large surface area. In our recent research, we synthesized a redox-responsive MOF using zirconium (Zr) as the metal ion and 4,4-dithiobisbenzoic acid (DTBA) as the organic linker. The synthesis method employed was the hydrothermal method, and it was observed that the MOF synthesized at 400°C had a particle size of less than 200 nm and a zeta potential of +35 mV, indicating its suitability as a carrier for drug delivery. Chrysin, a natural anticancer drug, was used in this study. Glutathione, which is abundantly present in tumor cells, cleaves the disulfide bond in the organic ligand (DTBA), leading to faster drug release. By incorporating chrysin into the synthesized MOF, we observed faster in vitro drug release, with 88 and 89% at pH 7.4 and 5.5, respectively. The synthesis of ZrDTBA MOF opens up new opportunities for its application in drug delivery.
12.
Impact of Nanoethosomes Loaded with Polyherbal Extracts on the Mechanisms Involved in Wound Healing In-vitro Research
Mekala K, Shaheedha SM, Prakash R
Abstract
This study focuses on formulating and optimizing Polyherbal Nanoethosomes for controlled drug delivery, utilizing a polyherbal extract comprising
Basella alba L.,
Portulaca oleracea L.,
Lawsonia inermis L.,
Trigonella foenum L., and
Peristrophe paniculata L. Comprehensive characterization revealed a variety of secondary metabolites within the extract. The primary goal was to create poly herbal extract-entrapped ethosomes that could be integrated into a sustained-release transdermal gel dosage. We prepared nanoethosomes using phosphatidylcholine, ethanol, Tween 80, and SLS, and optimized them using Design Expert software. The characteristics included size (particle size: 121 ± 2.60 nm) and entrapment efficiency (81.91 ± 1.92%), followed by incorporation into a carbopol gel for skin application. We performed
in-vitro permeation studies and cytotoxic assays on L-929 cells, which revealed favorable outcomes. Optimized nanoethosomes displayed desirable particle characteristics, highlighting their potential for controlled drug delivery. The nano vesicular gels had good rheological and physical properties (polydispersity index: 0.41 ± 0.04, zeta potential: -8.12 ± 1.25 mV), which meant they could be used topically. This research underscores the compatibility of plant extracts with formulation components, offering a foundation for Polyherbal Nanoethosomes in pharmaceutical formulations. The study emphasizes precise control over particle attributes and suggests potential applications in enhancing drug release and bioavailability.
13.
Preparation of Mouth Dissolving Sublingual Film of Fixed Dose Combination of Hydrochlorothiazide and Losartan Potassium and Statistical Optimization of Film
Attal V, Daniel K
Abstract
Fast-dissolving films (FDFs) are innovative dosage forms offering advantages such as improved patient compliance, rapid onset of action, precise dosing, and favorable taste. Particularly beneficial for patients unable to swallow or require immediate drug absorption, FDFs dissolve rapidly in the mouth, releasing medication directly into the oral cavity. The sublingual application enhances drug delivery due to the high permeability of the sublingual mucosa, bypassing hepatic first-pass metabolism. This route is advantageous for drugs like losartan potassium (LP) and hydrochlorothiazide (HCZ), which benefit from enhanced bioavailability and faster onset of action. Preformulation studies included UV spectroscopy for λmax determination (LP: 282 nm, HCZ: 250 nm), DSC for thermal analysis (LP: 289.11°C, HCZ: 104.76°C), and solubility studies confirming LP’s solubility in acidic pH and HCZ’s increased solubility in pH 6.7 buffer. Compatibility studies using FTIR and DSC validated stability with excipients. Formulation optimization with HPMC E15 resulted in films with characteristics like film weight (145.66–167.0 mg), thickness (0.246–0.326 mm), folding endurance (898.0–1274.0), pH (6.0–6.70), disintegration time (77.66–174.6 s), tensile strength (77.04–141.90 g/cm²), and drug release profiles (LP: 68.78–96.22%, HCZ: 59.49–95.43% at 21 minutes). In summary, this study successfully developed LP and HCZ FDFs with optimized characteristics, demonstrating their potential in hypertension management and improving therapeutic outcomes.
14.
Formulation Development and Evaluation of Transdermal Patches of Apigenin
Fatima Tirkey, Abhishek Dwivedi
Abstract
Apigenin is a flavonoid that is abundantly present in fruits and vegetables. It has a diverse range of therapeutic properties, including cardioprotective, neuroprotective, analgesic, and cancer-preventive effects. Its safety profile, even at higher doses, makes the compound particularly valuable. Apigenin, along with excipients, was used to formulate patches using the solvent-casting method on a glass mold. Seven distinct batches of patches were formulated using different combinations of polymers. The drug-polymer ratios employed in these formulations were (1:2), (1:3), (1:4), (1:4), (1:(2:8), (1:(1:9), and (1:(2:8) for both drugs. The formulated patches were evaluated and results indicate that the transdermal patches (TP5) have promising results.
15.
Formulation Development, Evaluation and Anticandidal Screening of Herbal Cream of Trianthema portulacastrum Linn.
Sumeet Dwivedi, Mahavir Chhajed, Sandeep Ashokrao Wathore, Sonam Upadhya
Abstract
Trianthema portulacastrum, commonly known as black pigweed (E) and patharchata (H) belongs to the family Lamiaceae is a flowering medicinal pants. The plant contains various bioactive compounds such as trianthenol, leptormol, cinnamic acid, beta cyanin and ecdysterone. Traditionally, almost every part of the plant is used for the treatment of inflammation, fungal infection, pain, liver disorders, etc. In the present study, hydroalcoholic extract of leaves of
Trianthema portulacastrum was taken to formulate herbal cream in three different batches, i.e., C-I, C-II and C-III, using different concentrations of the extract and prepared cream. Also, the anti-candidal activity of the herbal cream was determined in the fungus
Candida albicans. The results obtained indicated that the herbal cream containing hydroalcoholic extract of the selected plant possesses significant anti-candidal activity and hence it may used in the treatment of fungal infection.
16.
Optimization In-vitro Evaluation and Scratch Wound Healing Assay of Hexacosane Topical Gel for Wound Healing
Sruthy PN, Saravanan Govindaraj
Abstract
The compounds hexocosane, a sterol hydrocarbon identified in the dichloromethane extract and isolated from marine sponges of the genus
Agelas. Hexocosane possesses anti-inflammatory and antioxidant activities that reduce inflammation and oxidative stress, they promote cell proliferation and angiogenesis, facilitating tissue regeneration and repair. This multifaceted approach makes this secondary metabolite a promising candidate for developing advanced wound care therapies that effectively address both infection control and wound healing. On the basis of viscosity,
in-vitro release, and skin retention, optimal gel formulations were developed with hexocosane (1%) to achieve the best results. A response surface methodology Box-Behnken design was applied on three factors and three levels [carbopol 940 (1, 1.25 and 1.5%), hydroxypropyl methylcellulose (HPMC) (1,1.5 and 1.2%), and propylene glycol (0–1–1.5% and 1–2%, respectively] using three factors and three levels. In order to assess the spreadability and viscosity, a glass slide and a Brookfield viscometer were used. An assay was conducted to determine how topical gel affects wound healing. The optimization study of the gel formulation, involving variations in adhesive polymer (Carbopol 940), release retarding polymer (HPMC K4M), and penetration enhancer (Surfactant), has identified three noteworthy formulations (F4, F8 & F14). Each formulation is characterized by specific attributes such as viscosity,
in-vitro drug release, and skin retention. All samples were found to elicit significant wound healing efficacy as evidenced from the representative photomicrographs. The maximum efficacy was elicited by formulation (F4) with 100 mg drug at the time duration of 36 hours
17.
Development and Analysis of Colon-Specific, pH-Responsive Polymer Delivery of Irinotecan Hydrochloride Tablets for Colon Cancer Treatment
Mahalekshmi V, Balakrishnan N, Ajay Kumar TV, Parthasarathy V
Abstract
For the formulation of enteric-coated tablets containing irinotecan hydrochloride, this thesis focuses on HPMC and ethylcellulose, both of which are pH- and oxidation-resistant polymers. The integrated polymer-drug tablet mixture was coated with 15% of eudragit S100 and L100, which is a methacrylic acid copolymers, that’s soluble at pH 7. Both the physical characteristics with the
invitro release kinetics pattern of the enteric-coated tablets were characterized. In the invitro release study, different pH environments were used, comparable to the gastrointestinal tract (GIT): 0.1 N HCl solution for two hours, pH 6.8 phosphate buffer for three hours, and pH 7.4 phosphate buffer for six hours. Using this device, you can simulate the pH level of the mouth, the digestive tract, and the urinary tract. As a result of consistent release studies, formulation F7 released 88.2% of the drug after 12 hours. Models such as Higuchi, Korsmeyer-Peppas, and zero-order reactions were used to analyze the GIT. This directed the development of a sustained delivery pattern that may be perfect for colonic IRT administration in the eventual treatment of colon cancer. Among the nine formulations, F7 formulated with EC and HPMC extended best sustained release pattern of drug, hence it is suitable for treating colon cancer.
18.
Comparison Study of Aloin-Curcumin Nanoparticles by Taking 2 Different Ratios and Analyses by Using Drug Design Experimental Study
Rishika Chauhan, Balwan Singh, Ram Dayal, Anuj Malik
Abstract
Numerous chemopreventive drugs like aloin and curcumin have demonstrated potential effects in cancer treatment; however, their efficacy is limited by low bioavailability. Thus, the primary goal of this research was to formulate a unique method by using the herbal drugs synergistically and improve the bioavailability of these anticancer drugs here, using the nanoprecipitation method for two well-active constituents of known natural herbal compounds. Aloin (AL)-curcumin (CUR) were co-loaded into polymeric nanoparticles made of poly (D, L-lactide-co-glycolide) and surfactant-polyvinyl alcohol, with the experiment’s response being evaluated using Stat-Ease software. To create dual-loaded nanoparticles containing aloin and curcumin, using different ratios sand optimizing the best formulation. (60:120). For aloin curcumin, optimize the better formulation with controlled release formulation having less than 100 nm size of particle and drug entrapment was 86.09% while for (60:60) of aloin -curcumin having 99.1 nm particle size of drug and encapsulation efficiency was 72.05%.
19.
Spectrophotometric Assessment of Pyrocatechol Drug Employing Oxidative Coupling Reaction with 4-amino antipyrine as a Model of Pharmaceutical Compounds
Abbas Fadhil Ali, Mustafa Aziz Rahi, Kamil K Atiyah Altameemi, Mohammed Kassim Al-hussainawy, Munthir Abdulwahid Abdulhussain
Abstract
A rapid, simple, sensitive, and higher stability spectrophotometric method was developed the determine that it is stable Pyrocatechol drug in pure and pharmaceutical preparations. The method is based on an oxidative coupling reaction among Pyrocatechol drug and 4-amino antipyrine (4AAP) in the presence of potassium iodate (KIO3) in an acid medium to form a color complex that stable violet dye and a maximum absorption at 505 nm. The best optimum conditions and other analytical factors have been evaluated. A calibration curve of absorbance of several concentrations that obey the law of Beer-Lambert over the range concentration of pyrocatechol drug 10 to 100 mg/L, with (LoD =1.2*10-4 mg/L), (LoQ=3.4*10-4 mg/L), The relative standard deviations RSD% of the proposed methods were less than 0.68%). In contrast, recovery average and determination parameters are 99.9%. The method was used successfully for the determination of drugs in a pharmaceutical preparation with the best accuracy and precision. At range about 99.1 to 100.2% with RSD less than 0.3%. The analytical result for the estimation of the pure drug is presented together with the use of the proposed process for the analysis of some commercial pharmaceuticals. The data compare favorably with those of official and reported ways.
20.
Silver and Iron Nanoparticles: Green Synthesis and Characterization
Ravindra Waykar, Srinivasakumar Kumarapillai
Abstract
Biosynthesized nanoparticles (NPs) are gaining traction because they leverage physiologically active plant secondary metabolites, enabling eco-friendly synthesis and offering exclusive biological benefits. This innovative nanomedicine technology shows great promise in medicine, providing a novel method for drug delivery and treatment. The advancement of biosynthesized nanomedicine has notable implications for the pharmaceutical and medical sectors, presenting a more precise and effective way to address diseases. This paper introduces a cost-effective, environmentally friendly, and dependable method for synthesizing silver and iron NPs. The method involves employing the aqueous leaf extract of
Vallisneria spiralis Linnaeus. The biosynthesized NPs were analyzed utilizing several methods, including transmission electron microscope (TEM), dynamic light scattering (DLS), UV−visible spectroscopy, and ICP-MS.
21.
Development and Optimization of Gellan Gum-Based Gastro-Retentive Microbeads for Enhanced Controlled Release of Acyclovir
Ranjan Kumar Sethi, Sunit Kumar Sahoo, Pravat Ranjan Guru
Abstract
Modified release systems offer enhanced spatial and temporal control over drug delivery, leading to better blood plasma profiles, targeted therapy, reduced side effects, and improved patient compliance. Recent advancements focus on using biocompatible polymers to achieve sustained or controlled drug release, particularly for gastroretentive systems that enhance oral bioavailability and minimize dose-dependent toxicity. This study explores the formulation of floating microbeads of acyclovir (ACV) using various hydrophilic polymers. The prototype oral formulations demonstrated superior micrometric properties, including bulk density, tapped density, Carr’s index, Hausner’s ratio, angle of repose, average particle size, yield, and drug content.
In-vitro dissolution studies revealed controlled release characteristics, with optimal floating time and entrapment efficiency achieved using specific concentrations of olive oil and polymers. Drug release trailed the Korsmeyer-Peppas model, indicating a diffusion-controlled mechanism. The formulations exhibited good storage stability,
in-vivo floating ability, and higher bioavailability in rabbits compared to ACV solutions. The results suggest that hydrophilic polymers are effective for formulating floating microbeads with controlled release and reproducible profiles.
22.
Design, Development and Characterization of Gastroretentive Floating Tablet of Levofloxacin using Natural Polymer Peanut Husk
Gyanendra Kumar Saxena, Ruchi Tiwari
Abstract
In the present study, levofloxacin gastroretentive floating tablet (GRFT) was formulated using peanut husk powder as a natural release modifier for providing sustained drug delivery at the stomach to effectively treat infections. Preformulation studies such as UV analysis and drug excipients study using Fourier-transform infrared (FTIR) were performed. Peanut husk powder was prepared by crushing and grinding the dried peanut husk. The GRFT formulations (GRFT1- GRFT9) were formulated using the direct compression method with varied concentrations having peanut husk powder, HPMCK4M and carbapol 934, along with other ingredients. Formulations were characterized based on the pre-compressional parameter and post-compressional parameters. The results for GRFT5 were found to be best among all batches as it showed sustained %drug release of 89.52 ± 0.3% upto 12 hours and it revealed enhanced therapeutic performance of the drug. However,
in-vivo study needs to be performed for a better comparison of data with
in-vitro results.
23.
Design and Optimization of Ibuprofen and Ranitidine Hydrochloride Tri-Layer Tablets in Immediate Release Formulation by Quality by Design
Karthikeyan V, Rupesh Soni
Abstract
The current trend in pharmaceutical process development and optimization is known as quality by design (QbD). This methodical approach is founded on the concept that quality should be integrated into the product from the start, rather than assessed after manufacture. In this study, we demonstrate methods to improve the process parameters for making tri-layer tablets by applying QbD principles in a methodical way. Dependent elements with high to medium impact on the process. According to the study’s results, all systems showed signs of instant release. It appears that the structure of each formulation and the properties of the polymer utilized have a significant impact on the rate and mechanism of drug release. Substantial medication release is observed in the three-layer formulations. Both the pace and mechanism of drug release are significantly affected by the tablet’s geometrical features and structure, as well as the weight and thickness of the barrier layers. While data suggested that Fickian diffusion was primarily responsible for drug release in two-layer tablets, three-layer tablets showed signs of either anomalous diffusion or erosion/relaxation. Therefore, the drug was stabilized as immediate-release directly compressible triple layered Average core weight of tri-layered tablets (mg) was 1000 for ibuprofen, 100 for placebo and 200 for ranitidine, thickness (mm) was 9.00 ± 0.3, hardness (N) was 110 ± 25, core tablet weight was 1300.000 ± 2% mg and coated tablet weight was 1325 mg. Using other moisture-sensitive medications. This study provides the foundation for future research into optimizing the properties of tablets made by direct compression.
24.
Formulation and Evaluation of Nanoparticle Loaded Hydrogel Containing Antifungal Agent for the Treatment of Onychomycosis Using Factorial Design
Fiza Farheen, Hemant Kumar Yadav, Abhay Raizaday
Abstract
SLNs are hopeful carriers for the topical delivery of antifungal drugs. This research aimed to develop a topical gel combining Efinaconazole-loaded SLNs with fluconazole to enhance the treatment of onychomycosis. The objective was to formulate a nail gel that capitalizes on the localized action and improved adherence of efinaconazole, a crucial agent in treating nail disorders like onychomycosis. The formulation utilized an alcohol-based system with specialized ingredients to ensure low surface tension and optimal wetting properties. Fluconazole, a broad-spectrum third-generation triazole antifungal, was included for its systemic and superficial antifungal activity. It works by inhibiting the formation of ergosterol, a key component of fungal cell membranes, by blocking the fungal cytochrome P-450 enzyme. The SLN-based delivery system allows for the slower release of Efinaconazole, while fluconazole diffuses more rapidly. The optimized gel formulation showed sustained drug release, with Efinaconazole releasing 32.85% of the drug by the 8th hour, compared to 74.05% for fluconazole during the same period. A stability study on the F4 formulation, which utilized Carbopol 934, was conducted according to ICH guidelines and demonstrated that the gel maintained its quality attributes, such as color, odor, homogeneity, pH, and viscosity over 6 months of testing. These results indicate that the F4 topical gel formulation is stable and suitable for long-term use.
25.
Application of Box-Behnken Design for Formulation Optimization of Sorafenib loaded Nanoparticles Targeting to Liver Carcinoma: Ex-vivo Intestinal Permeation and Cytotoxicity Study
Gnyana Ranjan Parida, Gurudutta Pattnaik, Amulyaratna Behera, Dibya Lochan Mohanty, Suraj Sahoo
Abstract
The anticancer drug sorafenib (SFB) was formulated as a polymeric nanoparticle using Box-Behnken design. The solvent evaporation method was utilized to develop the sorafenib polymeric nanoparticles. Formulations were then evaluated in terms of their morphological structure, entrapment efficiency (EE%), zeta potential, polydispersity index (PDI), and particle size.
Ex-vivo intestinal permeation studies for pure drugs, as well as optimized formulation, were performed in rats. Furthermore, the anticancer activity was evaluated using the HepG2 cancer cell lines. Transmission electron microscopy (TEM) revealed that the improved formulation had a particle size of 175 nm, PDI of 0.134, zeta-potential of -23.8 mV, and the sorafenib-loaded PLGA NP were recognized as spherical particles. Over 90% of the drug was released in less than 24 hours, with an EE% of 85.1%. Sorafenib-loaded PLGA NP efficiently inhibited HepG2 cells.
26.
Development and Evaluation of Herbal Antiacne Gel Formulation Using Curcumin Phytosomes
Angum MM Ibrahim, Siham K AbdelRahim, Huriyyah A Alturaifi, Intisar AM Elalawy
Abstract
Acne vulgaris is a persistent inflammatory condition affecting the pilosebaceous unit that manifests as various skin lesions, including papules, comedones, cysts, pustules, and abscesses. Curcumin, extracted from
Curcuma longa rhizomes (Family: Zingiberaceae), is identified for its potent antioxidant, wound-healing, and anti-inflammatory properties. This study aimed to develop an herbal antiacne gel formulation incorporating bioactive curcumin in phytosomes. The formulated gel was evaluated for several physicochemical properties, including pH, spreadability, viscosity, drug content, etc. Additionally, the optimized gel formulation was tested for its
in-vitro antiacne action against
Propionibacterium acnes. Results showed that developed antiacne gel containing curcumin phytosomes was comparable to a commercially available antiacne product. Stability studies demonstrated that the formulated product remained stable for three months under accelerated stability conditions as per ICH guidelines.
27.
Optimizing Orphan Drug Rucaparib Transdermal Patches for Ovarian Cancer: A Design Expert-Based Strategy for Prolonged Drug Release
Hina Deepak Mehta, Saravanakumar Kasimedu, Bharath Raj KC, Vema Kiran
Abstract
This study aimed to develop and characterize transdermal patches for rucaparib using a Box-Behnken design (BBD), evaluating drug permeation at 8, 12, and 24 hours, with optimization through Design Expert software. The patches were formulated with HPMC K15, ethyl cellulose, and PVP K30. The physicochemical properties and drug infusion were tested and characterized. The transdermal patches developed in this study were found to be soft and flexible, indicating good handling properties and potential for comfortable application. The patches demonstrated sustained drug release, extending beyond 24 hours, which is crucial for preserving consistent beneficial levels of rucaparib in the systemic circulation. The optimal formulation, as identified through the BBD using Design Expert software, included HPMC K15 (100 mg), ethyl cellulose (200 mg), and PVP K30 (40 mg). This combination effectively facilitated prolonged drug penetration while keeping the flexibility and integrity of the patches. The study concludes that the formulated transdermal patches using HPMC K15, ethyl cellulose, and PVP K30 offer an effective means for prolonged delivery of DPZ and MMZ. The optimized patches support sustained discharge for a prolonged time, which can improve patient compliance and therapeutic outcomes in treating ovarian cancer. The use of a systematic design approach, such as the BBD, proved beneficial in optimizing the formulation parameters, ensuring the development of high-quality transdermal patches with desirable properties for clinical application.
28.
Characterization of Bimetallic (Zinc and Gold) Nanoparticles of Cryptostegia grandiflora Plant Extract and Their Biological Screening
RS Jadhav, AT Inamdar, SK Mohite, RM Gavali
Abstract
The goal of this learning was to explore the uses of
Cryptostegia grandiflora plant extract in the green formulation of bimetallic zinc-gold nanoparticles along with pharmacological evaluation. Green synthesis and other techniques are more advantageous than chemical and physical procedures because they produce nanoparticles in an environmentally responsible and economically viable manner. An ethanolic extract of
C. grandiflora was obtained through the use of Soxhlet extraction. Additionally, an ethanolic extract of
C. grandiflora and components from the extract were identified using GC-MS research after mixing plant extract (
C. grandiflora) with zinc acetate and chloroauric acid solutions and letting it sit for a while. UV-visible spectroscopy was employed to analyze the formation of nanoparticles, while FTIR was used for their characterization.
29.
Development and Characterization of Gingerol-Assisted Silver Nanoparticle and Chitosan Alginate Membrane for Antibacterial and Wound Healing Activity
Manisha Khaire, Papiya Bigoniya
Abstract
This study synthesized and characterized gingerol-loaded silver nanoparticles (Ag-NPs), which were incorporated into chitosan-alginate (Cs/Alg) films for advanced wound care applications. Gingerol was isolated with a 9.81% yield, forming pale-yellow needle-shaped crystals with a melting point of 32ºC. The purity and structure of gingerol were confirmed through thin-layer chromatography (TLC), UV-visible, fourier-transform infrared spectroscopy (FTIR), and high-performance liquid chromatography (HPLC) analyses. The synthesized Ag-NPs, particularly from the GN3 batch, exhibited a small particle size (36.52 ± 3.52 nm), high stability (zeta potential of -23.20 mV), and notable encapsulation efficiency (76.35%) and yield (74.11%). Scanning electron microscopy (SEM) and transmission electron microscopy (TEM) analyses revealed their spherical and smooth morphology. Stability tests over three months showed no substantial changes in particle size, ZP, or %EE. The Cs/Alg films demonstrated appropriate thickness, weight, water uptake, and pH changes, with GN-CM4 showing the best performance.
In-vitro drug release studies indicated increased release rates, especially for GN-CM4, which also exhibited the highest antibacterial activity.
In-vivo studies on excision and burn wound models showed that GN-CM4 promoted complete wound closure by day 21, enhanced hydroxyproline levels, reduced myeloperoxidase content, and facilitated superior tissue regeneration. These findings underscore the potential of gingerol-loaded Ag-NPs in enhancing wound healing through their anti-inflammatory and antibacterial properties.
30.
Synthesis, Spectral Characterization and Biological, DNA Binding, Molecular Docking and ADMET Studies of a New Benzyl (Z)-N’-((E)-3-Ethoxy-2-Hydroxybenzylidene) Carbamohydrazonothioate and Its Co (II), Ni (II), Cu (II) and Zn (II) Metal Complexes Derived From S-Benzyl Thiosemicabazide-Salicylaldehyde
M Sridhar, P Ramesh, K Laxma Reddy, A Krishnam Raju
Abstract
This study presents the synthesis, characterization, and biological evaluation of metal complexes derived from benzyl carbamohydrazonothioate. The ligand was synthesized through a condensation reaction and subsequently complexed with various metal ions, including Cu(II), Ni(II), Co(II), and Zn(II). The resulting metal complexes were characterized using a range of spectroscopic techniques, including FT-IR, UV-Vis, and NMR spectroscopy, confirming the successful coordination of the metal ions with the ligand. The structural elucidation was further supported by elemental analysis and molar conductance measurements. The biological activities of the synthesized complexes were evaluated for their antibacterial, antifungal, and antioxidant properties. The results indicated that the metal complexes exhibited enhanced biological activities compared to the free ligand, suggesting their potential as effective antimicrobial and antioxidant agents. This study highlights the significance of metal complexation in enhancing the biological efficacy of organic ligands.
31.
Design and Development of Solid Lipid Nanoparticles of Tofacitinib Citrate for the Treatment of Rheumatoid Arthritis: A Quality by Design Approach
V Deepika, S Srinu Naik
Abstract
Solid lipid nanoparticles, or SLNs, have gained popularity recently as a possible drug delivery method. However, the idea of using SLNs for organ and site-specific drug administration is still in its early stages due to the difficulties associated with this approach. The aim of this study is to develop SLNs with improved pharmaceutical characterization and anti-arthritic efficacy. Tofacitinib citrate (TC)-loaded SLNs were created using the microemulsification method, with the addition of stearic acid, chitosan, and Tween 80 to improve skin permeability. Seventeen SLNs were developed and characterized for particle size, entrapment efficiency (EE), and percentage drug release according to the Box-Behnken design. The DSC analysis revealed a strong endothermic peak at 166.18°C, significantly different from the pure TC reported at 218.05°C. This indicates a notable alteration in the endothermic peak of the SLNs, demonstrating a relationship with the excipients used in this investigation. XRD study highlighted significant characteristic drug peaks at positions 21.06 and 23.63 (2ɵ). These peaks represented the modifications that were seen in pure TC. The SEM analysis of the optimized lipid nanoparticles showed a smooth surface and a spherical appearance. The particle size analysis of the optimized formulation showed an average size of 181.5 nm. Also, the polydispersity index (PI) revealed a value of 0.495, indicating homogeneous dispersion. The zeta value was 8.2 mV, indicating stability.
32.
Development and Evaluation of Voriconazole Loaded Transfersomal Gel for Enhanced Antifungal Activity
Amareshwar S, Abbaraju Krishna Sailaja
Abstract
The BCS class II antifungal drug voriconazole (VRC) has a broad spectrum of action. Its solubility is still a major problem for formulation scientists despite numerous attempts to improve it. The thin-film hydration technique produced the voriconazole-loaded Transfersomes, optimized using the Central Composite Design (CCD) and then included as a gel into Poloxamer 407P. Several parameters were assessed for the prepared VRCT, including particle size, zeta potential, surface shape, potential chemical interaction, and polydispersity index (PI). The SEM study also revealed the appearance and surface of optimized transferosomes are symmetrical. The optimized formulation’s average size was found to be 238.8 nm by the particle size analysis. Similarly, a value of 0.449 was found by the polydispersity index (PI). To evaluate voriconazole Transfersomal gel’s (TG4) antibacterial efficacy, an antimicrobial investigation was conducted. The creation of Transfersomal gel formulation offers a topical drug administration method that is more effective and improves patient compliance.
33.
Formulation and Evaluation of Sustained Release Dosage Form of Venlafaxine Hydrochloride for Enhanced Treatment of Neurodisorders
Nilesh Sureshrao Mhaske, S Sathesh Kumar
Abstract
In the present study, we have designed and developed a sustained-release tablet formulation of Venlafaxine Hydrochloride. The optimized formulation was then subjected to various evaluation parameters. The formulation of venlafaxine hydrochloride sustained release tablets with a dosage of 500 mg included the utilization of several hydrophilic polymers, including jackfruit mucilage, HPMC K4, and PVPK30, as release retardants. This was done to extend the duration of drug release to 12 hours. The formulation features, including pre-compression and post-compression investigations, were conducted individually according to established protocols. The tablets were determined to be compliant in terms of weight uniformity, hardness, thickness, diameter, friability, and drug content. Separate in-vitro dissolution studies were done for both tablets. The venlafaxine hydrochloride SR formulation F18 was optimized to provide the desired release profile for up to 12 hours. The Venlafaxine Hydrochloride SR formulation was optimized and exhibited zero-order release kinetics. The stability studies conducted under accelerated conditions at a temperature of 40 ± 2°C and a relative humidity of 75 ± 5% yielded good results. The study indicated that the sustained release administration of Venlafaxine HCl is potentially efficacious. It reduces the frequency at which the patient has to take medication and improves patient adherence. Our objective is to conduct
in-vivo pharmacokinetic studies of the formulation to verify the drug’s entry into the systemic circulation.
34.
Antihypertensive Activity of Peptides Derived from Toman Fish Albumin (Channa micropeltes): In-silico Angiotensin-Converting Enzyme Inhibitory Study
Noer Komari, Eko Suhartono, Samsul Hadi, Kamilia Mustikasari, Gusti Muhammad Perdana Putera
Abstract
The peptides from protein hydrolysis can be as bioactive peptides. Currently, the process of protein hydrolysis can be done
in-silico technique, an alternative to bioactive peptide identification more effectively and efficiently. This study aims to predict bioactive peptides
in-silico technique of albumin hydrolysis from Toman Fish (
Channa micropeltes), which had the potential as an antihypertensive drug. Toman fish albumin sequence (A0A191TFW5) was obtained from the UniProt database. The identification of bioactive peptides was performed by simulating enzymatic hydrolysis with three human digestive enzymes: trypsin, chymotrypsin, and pepsin. The hydrolysis simulation of albumin was conducted using the ExPASy PeptideCutter program. The generated peptides’ potential activities, solubility, and ADMET (absorption, distribution, metabolism, excretion, and toxicity) properties were predicted using various online prediction tools. Molecular docking was performed on the bioactive peptides to determine the Gibbs free energy (ΔG) and to illustrate the interaction between the bioactive peptides and the active site of the Angiotensin Converting Enzyme (ACE) as a comparison was used captopril which was a commercial ACE inhibitor. The results showed that bioactive peptide candidates were AI, VL and LVP. These peptides were potentially a candidate for alternative antihypertensive drugs.
35.
Bioguided Fractionation and Isolation of Natural Antidiabetic Agents from Polyherbal Tablet
Sunayana R Vikhe, Sharvari V Vikhe, Rahul L Vikhe, Vilas B Ghawate
Abstract
Polyherbal antidiabetic tablets were formulated, evaluated and compressed by combining the powder extract of
Nigella sativa,
Trigonella foenum, and
Glycyrrhiza Glabra. A number of tests were carried out, including a uniformity weight test, an assessment of the tablets’ hardness and friability, an ash value, moisture content, an extractive value that is soluble in water or alcohol, density (bulk and tapped), repose angle, Carr’s index, disintegration time with preliminary phytochemical screening. The tablet also had
ex-vivo antidiabetic performance to enzymes alpha-amylase as well as glucosidase. To ensure the presence of active ingredients, thin-layer chromatography was performed. Column chromatography as performed using silica gel G as a stationary phase. The column of material was created using acetic acid, toluene, and ethyl acetate. As follows: (5.0:4.2:0.8) for 10 ml. The mobile phase of the sample, which contains toluene, ethyl acetate, acetic acid (50:42:8) and fractions, was isolated, collected and sent to IIT Bombay for GCHRMS analysis. In GCHRMS, the chemical constituent was found to be 2 H-Pyran-2-one, tetrahydro-4-hydroxy-4-methyl-, Tetrahydro [2 , 2’] bifuranyl-5-one, 1H-Benzimidazole, 2-(1-methylethyl)-, Bifenthrin, Propionamide, 2,2-diphenyl-N-(2-pyridinyl)-, Dihydromyristicin, 2-Dodecanone, di-p-Tolyl sulfone. The tablets showed promising results for alpha-amylase and alpha-glucosidase inhibition activities.
36.
Unveiling the Therapeutic Potential of Basella alba: A Comprehensive Investigation into Its Anti-arthritic Properties, Phytochemical Profile, and Molecular Docking Insights
Jithin Mathew, Shreeja M, Swathi AR, K Ragesh
Abstract
The study investigated the therapeutic efficacy of
Basella alba, a traditional medicinal plant, against rheumatoid arthritis. Comprehensive analyses, including phytochemical screening, physicochemical evaluation, molecular docking, and antioxidant assays, were conducted. The physicochemical properties, such as ash and extractive values, indicated the high quality and purity of the plant material. Molecular docking studies showed that active compounds in
B. alba exhibited strong binding affinities to key proteins involved in rheumatoid arthritis pathogenesis, suggesting potential inhibitory activity. Antioxidant capabilities were assessed through DPPH and nitric oxide scavenging assays. Phytochemical evaluation confirmed the presence of alkaloids, flavonoids, steroids, and triterpenoids. The secondary metabolites revealed significant mineral content (12% ash value), low insoluble mineral residues (1% acid-insoluble ash value), and high levels of hydrophilic (23.32% water-soluble extractives) and lipophilic compounds (8.48% alcohol-soluble extractives). Linoleic acid, palmitic acid, and cis-13-octadecanoic acid exhibited the highest binding affinities to the COX II receptor in molecular docking studies, with linoleic acid showing the strongest interaction. The DPPH assay showed a rise in antioxidant activity with increasing concentration, reaching 71.34% suppression at 100 μg/mL. The nitric oxide scavenging assay showed concentration-dependent antioxidant activity, reaching 64.20% inhibition at 100 μg/ml. The results suggest that the ethanolic extract of
B. alba has significant antioxidant and anti-arthritic potential.
37.
Formulation Development of Mucoadhesive Vaginal Gel of Secnidazole and Voriconazole
Vaidya VR, Powar PV, Pandya SV, Yadav VD
Abstract
Purpose: Over the preceding decades, developing conventional drug delivery in to modified form has acquired importance in the pharmaceutical industry. Vaginal drug delivery system offers localized drug administration of drug and also avoids unwanted side effects of oral drug delivery. Vaginal drug delivery system has significant role in medical practice. Even though VDDS has a lot of advantages over the other routes of administration. The goal of developing the Mucoadhesive Vaginal Gel was to achieve the synergistic effect of voriconazole and secnidazole in the treatment of bacterial and fungal vaginal infections.
Method: Mucoadhesive antimicrobial vaginal gel was optimised using Design expert software using Carbopol 934, HPMC K4M polymers.
Result: Formulation was evaluated for various rheological parameters ,antimicrobial activity, invitro drug release and stability study. The spreadability and pH was found to be 5.5 to 7.4 cm and 4.12. Its compatible with vaginal pH. The selected optimized F8 formulation is the best formulation and the drug ratio is 2:1. and optimum gel viscosity is 1874 cps. antimicrobial study revealed that faster drug release of test formulation was compared to marketed product. It indicates as inhibition zone.
Conclusion: The combination of drugs can serves as better option for treating vaginitis, compared to single drug formulation. Mucoadesion increases contact time of drug with affected area which rendered formulation more effective.
38.
The Milling Method in Formation of Inclusion Complex p-Methoxycinnamic Acid-Hydroxypropyl-β-Cyclodextrin
Dewi Isadiartuti, Helmy Yusuf, Dwi Setyawan, Juni Ekowati
Abstract
p-methoxycinnamic acid (
pMCA) is a substance with several pharmacological activities, derived from the rhizome of
Kaempferia galanga Linn. The solubility of
pMCA can be increased by the formation of inclusion complexes (IC) using hydroxypropyl-β-cyclodextrin (HPβCD) compounds. IC are obtained through the milling method, which is a simple, environmentally friendly, and low-cost manufacturing method. The process involves the pounding of material with a certain speed and impact force. This research aims to characterize the
pMCA-HPβCD IC made using the milling method. Milling the mixture of
pMCA and HPβCD using a ball mill is a common technique to enhance the formation of the inclusion complex. The IC’s physical characteristics were analyzed in terms of their morphology, particle size, crystallinity, and thermal properties. The dissolution profile was also performed using paddle-typed dissolution apparatus (Type II) with 500 mL distilled water as dissolution medium. The amount of
pMCA dissolved was determined using UV spectrophotometry. The dissolution parameter was determined as dissolution efficiency at 60 minutes (DE60). The IC particles were irregular in shapes and porous. The size was reduced as compared to the individual components. The XRD revealed that the ICs were amorphous. The DE60 of IC increased by a factor of 4.3 compared to the pure pMCA. In conclusion, the milling method successfully formed complex of
pMCA-HPβCD with different characteristics from the initial compound and was significantly increased the percentage of the dissolved
pMCA.
39. P
hysiochemical Analysis, Antioxidant Activity, Antimicrobial Activity and Phenolic Profile of Ipomoea eriocarpa R. Br. Leaves
Prashant Kumar Singh, AKS Rawat
Abstract
Many active substances found in plants are essential in the treatment of transmissible and non-transmissible ailments. To enhance their well-being and capabilities, most people around the globe use medicines from plants and herbal origin. The goal of the current study was an assessment of physiochemical properties as well as measuring the effect of various solvents (ethanol, chloroform, and water) on the phenolic profile and on free radical scavenging potential. The standard procedures were used for the preliminary phytochemical, physiochemical and fluorescence analysis. Folin-Ciocalteu and colorimetric methods were used to determine the quantitative phytochemical analysis, respectively. The free radical scavenging potential was determined through 2,2-diphenyl-1-picrylhydrazyl (DPPH) and 2,2′′-casino-bis (3-ethylbenzothiazoline-6-sulphonic) acid (ABTS) assays. The antimicrobial activity was assessed using the disk diffusion method on a range of bacterial and fungal strains. The finding showed that ethanol was the best solvent for extracting polyphenols. The presence of alkaloids, carbohydrates, flavonoids, glycosides, phenolic compounds, and tannins was observed in the plant. Additionally, fluorescence characteristics and physiochemical parameters provided valuable data that can be used to establish standards for this plant. Results of quantitative phytochemical estimation revealed that the ethanol extract had a higher phenolic content (71.82 mg/g GAE) and flavonoid content (82.7 mg/g QE), while the aqueous extract had the lowest phenolic content (27.05 mg/g GAE) and flavonoid content (18.93 mg/g QE). The
I. eriocarpa ethanolic extract had the maximum scavenging potential against DPPH (32.36 μg/mL) and ABTS (55.54 μg/mL). The results of the antimicrobial activity assessment also indicate that the ethanol extract exhibited a greater inhibition zone when tested against both bacterial strains. Results of thecurrent study suggested that the ethanolic extract has significant antioxidant potential and has the capability of being a notable source of organic antioxidants for the formulation of functional foods.
40.
Graphene-Based Nano Drug Delivery of Curcumin for the Treatment of Dengue Fever
Das Pritam, Rana Amita, Rana Mahendra
Abstract
Graphene, which is defined as a single-layered sp2 hybridized carbon atoms placed in a honeycomb-like crystal lattice when converted to graphene oxide, has proven its worth by showing its tremendous capacity in controlling the release rate of drugs by entrapping in the numerous pockets present inside it through π-π stacking interaction when used as a nanocarrier. In this experiment graphene oxide was synthesized through traditional Hummer’s method and was used as a nanocarrier to target nanosized drugs, which was prepared by loading curcumin drug into the PVP functionalized graphene oxide by using necessary procedures. After the successful confirmation of the stability, functionalization, and compatibility through various characterization procedures and effective drug loading into the systems, the release behavior of the formulations has been checked through dialysis bag diffusion technique using potassium phosphate buffer saline (pH 7.2, 4.0 and 9.2) for selection of the best medium for determination of the successful sustained-release behavior of the drugs through the dialysis membrane which concluded with satisfactory, sustained and constant drug release phenomenon in the acidic environment reflecting an idea of the fact its favorable release in acidic pH. It is a fact known that dengue fever causes systemic acidosis i.e., reduction of the pH of blood below 7. Thus, when used
in-vivo there is a possibility that the formulation has easy access to its target and, performs the desired mechanism of action and can be used as a therapeutic delivery system against the Dengue virus.
41.
Synthesis, Evaluation of Antiangiogenic Activity of Novel Coumarinyl 4-Thiazolidinone Derivatives
Ishwar Bhat K, Vijaya Bhaskar K
Abstract
Cancer remains in the maximum percentage probability of death in spite of the latest advancement in prior diagnosis and different approaches to treatment. The major challenge in drug discovery for medicinal chemists is to develop new cytotoxic agents to cure cancer with fewer side effects. A new series of substituted coumarinyl 4-thiazolidinone derivatives (TZL1–TZL7) were prepared by treating different 4-hydroxy-3-(1-(phenylimino0ethyl)-2H-chromen-2-one with HSCH2COOH. The Schiff bases were obtained by treating 4-hydroxy coumarin with different aniline derivatives in the presence of C2H5OH. All the title compounds were purified and subjected to TLC to check their purity. Further, it was characterized by using IR, 1H-NMR, and mass spectral studies. Selected synthesized compounds (TZL1–TZL7) were screened for
in-vivo antiangiogenic activity by using the Zebrafish model. TZL2 had the best antiangiogenic effect with an average vein count of 2.7. TZL4, TZL5, and TZL6 had an average vein count of 4.1, 3.9, and 3.4, respectively.
42.
Synthesis, Characterization and Antibacterial Studies of New Crown Ether Prodrugs
Marwan Majeed Al-Lammi, Raheem Jameel M, Layla Jasim Abbas
Abstract
New three esters (E1, E2 and E3) from crown ethers and drugs were prepared by Stiglich esterification. These procedures began with the reaction of certain quinolones (levofloxacin, ciprofloxacin, and nalidixic acid) with thionyl chloride to produce a considerably more potent acylating agent. Next, for the production of ester prodrugs, 2-hydroxymethyl-15-crown-5 ether (a lariat crown ether) was esterified using an acid chloride in the presence of pyridine. These molecules were synthesized as carrier-mediated prodrugs in order to solve different pharmacokinetic and pharmacological difficulties, enhance physicochemical features, and augment the antibacterial efficacy of the parent drugs by structural modifications while avoiding bacterial resistance. The compounds` structures were verified by FTIR, UV, H1 & 13C-NMR spectroscopy and certain physiochemical qualities. In a concentration-dependent manner, all of the synthesized prodrugs’ biological studies revealed improved activity against certain bacterial species.
43.
Study of Nootropic Effect of Improved Nano Formulation Version of Levodopa in a Rat Model of Parkinson’s Disease Induced by 6-Hydroxydopamine
Rawal VP, Gangurde SA
Abstract
Background: More studies on Parkinson’s disease (PD) symptoms have demonstrated that the condition is multifaceted. PD is associated with cognitive problems & motor impairments, which lower quality of life. 6-hydroxydopamine is a common rodent Parkinsonism neurotoxin. 6-OHDA may damage neurons by increasing oxidative stress from hydroxyl radical production during autoxidation. 6-OHDA and oxidative stress have been shown to impair memory in rats. Thus, 6-OHDA mimics rat Parkinsonian and cognitive decline.
Objective: To construct a stable and easily administered nano-formulation with enhanced bioavailability by adding
Mucuna pruriens seed phytoactive Levodopa into Nanocochleates.
Materials and Methods: Free L-Dopa, nanoliposomes, and levodopa nanocochleates were tested in 6-OHDA-treated rats with PD on the 14th day following the 6-OHDA injection, open-field, morris-water-maze, and Y-maze tests assessed learning and memory.
Results: Oral LDNC may reduce 6-OHDA-induced catecholamine neurotoxicity, according to this study. In this 6-OHDA-induced PD model, the nano-formulation appeared to restore injured striatal cells
via antioxidant and DA-enhancing pathways.
44.
Formulation and Evaluation of Herbal Capsules Containing Gum Resin of Boswellia serrata
Sonel Gurjar M, Sangeetha M, Vikram J2, Gopinath S, Anantharaj V
Abstract
Boswellia serrata (Sallaki) is one of the most popular herbs, belonging to the family Burseraceae, whose dietary and therapeutic potential has been practiced since ancient days mainly for the treatment of arthritis and other inflammatory disorders. The therapeutic activity of oleo gum resin is typically due to the presence of active constituents such as 11-keto-β-boswellic acid and 3-o-acetyl-11-keto-β-boswellic acid. The main objective of the present research work was to formulate and evaluate the
Boswellia capsule. The plant
B. serrata is the best traditional medicine for the treatment of Rheumatoid arthritis without causing any side-effects when compared to synthetic drugs (NSAIDs). The herbal capsules were formulated and evaluated. The prepared formulation was subjected to evaluations like physical appearance, pH, dissolution, disintegration and phytochemical screening.
45. D
esign, Development and Characterization of a Niosomal Anticancer Drug Delivery System Formulation
Rajesh S. Palva, Yadav Vikas K, Rajnikant M. Suthar, Rahul Shete
Abstract
Objective: This study set out to create a niosomal formulation of ceritinib with the goal of delivering the medication specifically to the lungs while reducing side effects.
Method: Span 60, cholesterol and DCP were combined with the thin film hydration process to create niosomes. A central composite design was used to optimize the formulation, and the design of experiments was used to assess the impact of various variables on vesicle size and entrapment efficiency. The TEM and
in-vitro drug release tests were used to analyse the optimized niosomes.
Results: 395.5 nm was the particle size, 75.28% entrapment efficiency, 0.321 polydispersity Index (PDI), and -28.0 mV zeta potential of the optimized niosomes. 68.03% of the medication was released after 48 hours.
Conclusion: To address the issues with traditional oral ceritinib distribution, ceritinib-loaded niosomes were created in this study as a potential substitute.
46.
reformulation Studies of Pitavastatin Calcium– A Primary Step in Further Design of Chronotherapeutic Formulation Synchronized with Circadian Rhythm
V Anusha, MS Umashankar, Y Ganesh kumar
Abstract
The principal goal and objective of this present research work were to perform a preformulation analysis of Pitavastatin calcium to produce a further stable, efficient chroomodulated drug delivery system. Pitavastatin calcium was analyzed to study its micrometric properties, equilibrium solubility profile in different media, and determination of purity by subjecting to fourier-transform infrared spectroscopy (FTIR) studies, by determining the absorption maxima in the medium along with differential scanning Calorimetry- DSC. Spectral analysis of UV studies and calibration curve plotting was done for further analytical research. The melting point was analyzed, and PXRD studies were conducted to identify the crystallinity. The Pitavastatin calcium micromeritic properties were found to be good with bulk density- 0.408 g/mL, tapped density 0.476 g/mL, Carr’s index 14.2%, Hausner’s ratio 1.16 with 32.0050 angle of repose. The equilibrium solubility study indicates drug has peak solubility in media 0.1 N Hcl and reduced solubility in distilled water. The infrared spectrum indicated peaks corresponding to functional groups conforming to the purity. The UV spectrum exhibited absorption maxima at 250 nm in media 0.1N HCl and 245 in pH phosphate buffer 6.8 and in all other mediums, which is the same as the standard literature indication. The calibration curve exhibited linearity in accordance with Beer Lambert’s law. The PXRD studies produced 2θ values corresponding to pitavastatin calcium as per literature conforming to the crystallinity. The Preformulation analysis concludes that the drug was pure pitavastatin calcium with corresponding absorption maxima, an infrared spectral functional group with crystallinity. It specifies that the drug mandates the improvement of solubility for further formulation development.
47.
evelopment of Kopasanda Leaves Extract (Chromolaena odorata (L.)) Phytosome Using Solvent Evaporation Method
Sucilawaty Ridwan, Windah Anugrah Subaidah, Eskarani Tri Pratiwi
Abstract
Kopasanda (
Chromolaena odorata (L.) R.M.King&H.Rob) or siam weed exhibited various pharmacological activities such as anticancer, antidiabetic, and wound healing activities. The phenolic content of kopasanda leaf extract was high in the range of 56.15 mg GAE/g-242.3 mg GAE/g. But, it reported that phenolic compounds exhibited poor bioavailability because of their physicochemical properties. The phytosomes system improves the effectiveness of phytoconstituents. Aims of the research as prepare and evaluate the phytosome from kopasanda leaf extract. Kopasanda dried leaves were extracted by the sonication method. The solvent evaporation method was used in the phytosome preparation with various concentrations between extract and phospholipid ( 2:1; 1:1; 1:2; and 1:3). Furthermore, phytosome formation was analyzed for its entrapment efficiency, Polydispersity Index (PDI), particle size, spectroscopy infra-red (IR), and Transmission Electron Microscope (TEM) method. The total phenolic content (TPC) of crude was 110.969 ± 0.752 mgGAE/g. The optimum phytosome was gained with a concentration between extract and phospholipid (1:3). It resulted in the entrapment efficiency of 99.930 ± 0.001%, particle size, and polydispersity index equal to 206.5 ± 8.613nm and 0.528 ± 0.038. The morphology of the phytosome was spherical and the phytosome formation was verified by the IR spectrum by comparing the phytosome and the physical mixture of extract and phospholipid. The results obtained showed that phytosome containing kopasanda leaf extract was formed using the solvent evaporation method.
48.
Design, Devlopment and Evaluation of Gastroretentive Floating Microspheres of Glibenclamide: In-vitro In-vivo Studies
Radheshyam Samanta, Gaurav Tiwari, Naveen Gupta, Dharmendra Singh Rajput, Prasenjit Maity
Abstract
The current research study was designed to characterize the ethyl cellulose act as a carrier mediator used to prepare a floating microsphere of glibenclamide for developed gastroretentive sustain release floating drug delivery. Different microspheres of glibenclamide were formulated by the emulsion solvent evaporation technique of glibenclamide with EC in different ratios by using two solvent systems (ethanol and chloroform). After evaluating the micropolitics properties, %of yield value, drug loading efficiency, entrapment efficiency, diameter and surface morphology of the microsphere by using DLS and SEM, in-vitro drug release in gastric content, in-vitro buoyancy, and
in-vivo floatation using animal model, compatibility study by FTIR, DSC and any other analytical study to demonstrate all formulation (especially GM2) was showing excellent results. So this work shows great gastro etentive floating drug delivery system for prolonged periods of time which is very useful in future for further study.
49.
Stability-Indicating HPLC Method Development and Validation for the Simultaneous Determination of Vildagliptin and Dapagliflozin in Pharmaceutical Dosage Form
Deshmukh S B, Wagh P A, Yadav S S, Mane M B
Abstract
Vildagliptin (VD) and Dapagliflozin (DP) were determined simultaneously by RP-HPLC using an ultraviolet (UV) detector, a Hypersil Gold C18 (250 × 4.6 mm) column, 5 μm and a mobile phase of acetonitrile: water (adjusted with O-Phosphoric acid to pH 3) in ratio 40: 60% v/v. The estimation wavelength was chosen to be 213 nm. VD and DP were shown to have retention times of 2.9 and 8.3 minutes, respectively. Q2 (R1) ICH guidelines were followed during the validation process. VD and DP correlation coefficient R2 values are 0.9993 and 0.999, respectively. While DP’s linearity range is 1 to 6 μg/mL, VD’s is 10 to 60 μg/mL. The precision and accuracy studies show %relative standard deviation (%RSD) below 2%. Recovery% was assessed to meet the ICH Q2 (R1) guidelines criteria. The presented research on forced degradation showed stability indicating studies. The findings also demonstrated that the suggested method is suitable for determining VD and DP precisely and accurately.
50.
Nanoemulsion of Ethanolic Extract of Sungkai Leaves (Peronema Canescens Jack) for Anti-Acne Therapy
Witha Budiartina, Winda Putria Sari, Ali Napiah Nasution, Ermi Girsang
Abstract
This study investigates the phytochemical profile, total flavonoid content, antibacterial properties, antioxidant activities, and cytotoxicity effect of nanoemulsion ethanolic extract of Sungkai leaves. The ethanolic extract was formulated into three concentrations: 50, 100, and 150 ppm. Phytochemical screening revealed flavonoids, tannins, alkaloids, steroids, and terpenoids. The total flavonoid content was 90.542, 91.993, and 91.744% for the respective concentrations. Antibacterial activity against
Propionibacterium acnes showed inhibition zones of 17.6, 21.2, and 24.1 mm, indicating strong to very strong activity. Antioxidant activities, evaluated using DPPH, ABTS, and FRAP assays, showed IC50 values categorized as very strong. The cytotoxicity test exhibited moderate activity. These findings suggest that Sungkai leaf ethanol extract nanoemulsion has rich bioactive compounds with significant antibacterial and antioxidant properties, along with moderate cytotoxic activity, highlighting its potential for pharmaceutical and cosmetic applications.
51.
Comparative Evaluation of Herbal Lip Balms Formulated Using Various Natural Bases
Vadje Suvarna A, Waghire Nikhil R, Pimple Bhushan P, Kuchekar Mohini C, Sarda Priyanka P
Abstract
The demand for natural cosmetics, including lip balms, has increased in recent years. Studies on the physicochemical characteristics of the designed lip balms are scarce, though. As a result, this comparative study aims to develop lip balms with carrot root extract as a coloring pigment using various natural bases and test the physicochemical characteristics of developed lip balms in order to prepare the best formulation. Four distinct softening agents (White soft paraffin, mango butter, avocado butter, and kokum butter) and two distinct hardening agents (Candelilla wax bees wax) were combined in varying amounts to prepare eight different lip balm formulations. The formulations were subjected to various physicochemical evaluation studies such as melting point, breaking point, spreadability, water resistance and organoleptic evaluation like color and texture. According to this study, carrot root extract may be used as a natural coloring agent in lip balm formulations because of its antioxidant properties. The results showed that the four formulations with mango butter:bees wax (1.5:1), white soft paraffin:Candelilla wax(2:1), Mango butter:Candelilla wax(2:1) and Kokum butter: Candelilla wax(2.5:1) were the best when compared to standard. The research study’s findings suggested that in the future, candelilla wax and mango butter can be effective alternatives for others as hardening and softening agents, respectively.
52.
Teriflunomide Transdermal Cream: In-vitro And In-vivo Evaluation for the Treatment of Rheumatoid Arthritis
Venkata Nookaraju Sreedharala, Pavan Kumar Chintamaneni
Abstract
Rheumatoid Arthritis (RA) is an incurable long-term disease that requires continuous safe treatment. Currently, many anti-inflammatory agents and steroids are used to manage the diseases and are associated with a variety of side effects. There is a great need for a formulation that addresses the root cause of the disease and can be used for prolonged periods without any side effects. Hence, an attempt was made to develop a formulation of an alternative to steroid formulations that can be used for prolonged periods without/minimal side effects, i.e., teriflunomide topical dosage form. Teriflunomide tablet was approved for multiple sclerosis. It is the primary metabolite of leflunomide which is approved to treat RA. When leflunomide is administered orally converts to teriflunomide to elicit its action as such, leflunomide has no anti-rheumatoid effect. Both leflunomide and teriflunomide have different GIT side effects such as diarrhea, nausea, and hepatotoxicity on oral administration. To avoid these oral side effects of leflunomide and teriflunomide and to improve RA treatment compliance, teriflunomide was formulated as a topical cream. The developed topical cream is designed to be applied at night on the affected joints. It is intended to release the drug during the night, provide higher localized concentrations of the drug in the synovial joint and reduce GI and systemic side effects improving treatment compliance.
53.
Design, Development and Characterization of Nisoldipine Solid Lipid Nanoparticles: Statistical and Characterization Perspectives
Neeraj Kumar Chauhan, Anuj Malik
Abstract
The objective of this study was to develop and characterize solid lipid nanoparticles (SLNs) loaded with Nisoldipine (NIS), aiming to enhance the drug’s bioavailability and provide a sustained release profile. SLNs were prepared using a solvent evaporation method and evaluated for several critical parameters. The superfluity test assessed the homogeneity of the SLN suspension, while particle size, drug entrapment efficiency, shapes, and surface morphology were analyzed using SEM/DLS/TEM. Researchers studied the process of how drugs are released and performed
in-vitro drug release tests to establish the substance’s release profile. HPLC and FT-IR were used to verify the drug’s chemical stability and encapsulation effectiveness. Stability studies assessed the formulation’s stability over time throughout different storage settings. The SLNs exhibited a high degree of homogeneity in the superfluity test, with no phase separation. The drug entrapment effectiveness was over 80%, and the typical particle size was 150-250 nm. Microscopy and transmission electron microscopy revealed that the SLNs had a flat, spherical top. NIS exhibited a regulated sequence of kinematics and prolonged release during dissolution investigations. FTIR and HPLC confirmed the stability and integrity of the drug within the SLNs. Stability studies indicated that the formulation remained stable over time. NIS-loaded SLNs show significant potential as an effective drug delivery system, offering enhanced bioavailability, sustained release, and excellent stability.
54.
Design, Optimization and Performance Assessment of Memantine Buccal Films for Targeted Drug Delivery
Venkata Durga Seshu Priya P, Ruby S, Kumar M
Abstract
Memantine is primarily prescribed for treating moderate to severe Alzheimer’s disease by modulating glutamate, a key neurotransmitter involved in cognitive functions like memory and learning. By blocking excessive glutamate activity at NMDA receptors, memantine helps improve cognitive function and slow symptom progression in Alzheimer’s patients. In this study, solvent evaporation was used in the formulation of memantine in order to increase its bioavailability and sustain its release. Chitosan, HPMC, a mucoadhesive polymer, carbopol, a sensitive to pH polymer and propyle glycol, a permeation enhancer, were all incorporated in the formulation. All formulations underwent evaluation for moisture content, folding endurance, swelling index, mucoadhesive strength and drug content. Drug release profiles were assessed through
in-vitro diffusion studies. Results indicated that increasing concentrations of polymers led to higher mucoadhesive strength, consequently enhancing Memantine release from the system. The optimal formulation(F9), with carefully balanced polymer concentrations, demonstrated more resident time, sustained drug release and improved bioavailability.
55.
Experimental Antioxidant Activities of Synthetic 3,4-Dihydropyrimidine Derivatives
Mahmood S. Magtoof, Noor R Ali, Rabeah T Mahmood
Abstract
The synthesized of five new pyrimidine derivatives was prepared from the condensation in one pot reaction of ethyl acetoacetate, substituted aromatic aldehydes, urea, and FeCL3.6H2O, with 5 to 10 drops of hydrochloride acid as catalyst in reflexing ethanol. The yield of the product was found to be in the range of 55 to 90%. The antioxidant efficiency of synthesized compounds was estimated by using the 2, 2-diphenyl-1-picrylhydrazyl (DPPH) method, hydroxyl method, nitric oxide method, and superoxide radical scavenging assay method. The compounds 6a, 6e, and 6c demonstrated considerable radical scavenging activity, resulting in the presence of electron-donating substituent on replaced aldehydes. The confirmation compounds by spectral data by proton and
13C-nuclear magnetic resonance, infrared spectra, and MS spectra.
56.
Quality by Design Approach to Nasal Mucoadhesive Microspheres: Enhanced Sumatriptan Succinate Delivery through Formulation and Characterization
Shivanee Vyas, Anitha K N, Niranjan Babu Mudduluru, Lalchand D Devhare
Abstract
The primary therapeutic indications for sumatriptan succinate (STS) include the treatment of migraine and cluster headaches. To enhance mucoadhesion, sodium carboxymethyl cellulose (SCMC) and hydroxyl propyl methyl cellulose (HPMC K15M) were used in this study to develop nasal mucoadhesive microspheres of STS. A central composite design, facilitated by Design Expert software, was employed to assess the impact of polymer concentrations on mucoadhesion, involving nine different formulations. The study’s findings indicated that the microspheres were uniformly sized and spherical and that the polymers were compatible with STS. The optimal formulation, consisting of 220.711 mg of SCMC and 150 mg of HPMC K15M, demonstrated the highest level of mucoadhesion. This combination effectively regulated the discharge of STS from the mucoadhesive microspheres and significantly improved their mucoadhesive properties. These results suggest that the strategic use of SCMC and HPMC K15M can enhance the performance of nasal mucoadhesive microspheres, ensuring a controlled release of STS and improved adhesion to mucosal surfaces. This has the potential to optimize the therapeutic efficacy of STS in treating migraine and cluster headaches.
57.
Design, Formulation, and Optimization of Nicardipine-Loaded Gastroretentive Floating Microspheres: In-vitro, Ex-vivo and In-vivo Characterization
Sepuri Vijayalaxmi, Abbaraju Krishna Sailaja
Abstract
Nicardipine hydrochloride is highly soluble at low pH values. The objective of this investigation was to design, manufacture, and refine the drug’s floating microspheres to increase its bioavailability and prolong its period of residence in the gastrointestinal tract. To optimize the Box-Behken and prepare the floating microspheres, solvent evaporation was employed. The formulation F5 was discovered to be the best as anticipated by the design expert software’s point prediction. Evaluations of pre- and post-compressional parameters were conducted. Utilizing several kinetic models, the drug release pathways were examined. The drugs and excipients did not interact, according to the FTIR/DSC investigations. According to the radiological approach, F5 showed good
in-vitro buoyancy. The gastroretentive property of microspheres is revealed by X-ray pictures obtained at 2, 8, and 12 hours for the buoyancy investigation. F5 (235.04%) demonstrated a high relative bioavailability over oral tablets, according to the
in-vivo pharmacokinetic investigation. In comparison to the marketed formulation group, the F5-treated group experienced a considerably larger percent decline in BP values (20.00 ± 6.00 and 13.00 ± 4.00%, respectively) at 36 and 48 hours of the
in-vivo pharmacodynamic testing. For 90 days, the F5 formulation was maintained at 5 ± 2 and 25 ± 2°C, indicating the stability of nicardipine microspheres.
58.
An Approach to Development and In-vivo Evaluation of Beta Sitosterol Phytosomes by Taguchi Orthogonal Array Design
Srikala Kamireddy, S Sangeetha, Harekrishna Roy
Abstract
The research mainly focused on developing and optimizing beta-sitosterol phytosomes through a systematic Taguchi orthogonal array design and assessment of their performance in both beta-sitosterol phytosomes. The fabrication of phytosomes containing β-sitosterol was carried out using the rotary evaporation technique. An orthogonal array design was employed in the study to precisely optimize the phytosomes. In this two responses and three independent variables were analyzed. The data was analyzed by using statistical modeling. Characterization of these phytosomes involves Fourier transform infrared spectroscopy, entrapment efficiency, differential scanning calorimetry compatibility study, zeta potential and particle size. Based on the findings, an optimized phytsome formulation was developed to achieve the best results. The results indicated that beta-sitosterol phytosomes responses are significant. It effectively reduced body weight as well as levels of total cholesterol (126.120 ± 0.98 mg/dl), triglycerides (104.23 ± 2.8 mg/dl), HDL (39.31 ± 0.45 mg/dl), VLDL (21.67 ± 0.34 mg/dl), and LDL (76.43 ± 0.34 mg/dl) in rats compared to the other groups. The orthogonal array design study observed that the anti-hyperlipidemic activity of β-sitosterol was nearly as potent as that achieved with standard drug therapy.
59.
Design and Optimization of Solid Lipid Nanoparticles for Enhanced Therapeutic Activity of Linagliptin
Swathi Yambadi, Vasudha Bakshi
Abstract
To augment oral bioavailability, linagliptin (LGP) loaded solid lipid nanoparticles (SLNs) have been formed using the solvent evaporation technique of emulsification. Utilizing the Box Behken design (BBD), examining the relation between independent and dependent variables was possible. Particle size (PS), entrapment efficiency (EE), and
in-vitro drug release (DR) studies were considered response factors, whereas the various concentrations of lipid carrier, surfactant, and co-surfactant were considered process variables for optimization. The design expert program was used to obtain the optimized batch. At 24 hours, it was discovered that the optimized batch expected responses for PS, %EE, and %DR were 105.83 nm, 81.19, and 96.69%, respectively. The observed PS, %EE, and %DR responses of the optimized batch at 24 hours were determined to be 101.36 nm, 80.56, and 96.31%, respectively. There is no interaction seen in the basic physical mixing of drug and polymer, according to the FTIR spectra of pure drugs, polymers, and drug and polymer mixtures. The optimized formulation’s average size was found to be 138 nm by the particle size analysis. Similarly, a value of 0.255 was found by the polydispersity index (PDI). This suggests that the SLN in the formulation has a homogeneous size dispersion. With a zeta value of -32.8 mV, stability is indicated. Linagliptin was effectively developed as a drug with a 24-hour sustained release. Wistar rats were used in the
in-vivo evaluation of linagliptin SLN formulations. The drug bioavailability increased five times (a highly significant fivefold increase) in LGP-loaded SLNs (AUC
0-t ≈ 134.5 μg*h/mL) compared to raw LGP (AUC
0-t = 27.23 μg*h/mL).
60.
New Metal Complexes with Mannich –β-amino carbonyl ligand; Preparation, spectral Characterisation and Biological Activity
Baraa Kasim Mohammed, Enaam Ismail Yousif
Abstract
New metal complexes and a new beta-amino maniche carbonyl ligand were prepared and characterized. (((4-(tert-butyl)-2-((S)-(phenylamino) (p-tolyl) methyl)cyclohexan-1-one)) (HL) was formed from the reaction of aniline and 4-methylbesaldehyde with 4- (tert-butyl)cyclohexane-1-one at a 1:1:1 mol ratio respectively reaction of (4-methyl-2-((R)-(phenylamino)(p-tolyl)methyl)cyclohexan-1-one (HL) and MnII, CoII, NiII, CuII, ZnII and CdII metal ions in a 2:1 (L:M) ratio led to the isolation of monomeric complexes from analytical and spectroscopic techniques including; elemental microanalysis, magnetic susceptibility, conductivity, TGA, and FTIR, electronic and mass spectra and
1H,
13C-NMR characterization data indicated to a four- and six-coordinate isolate.Complexes Many bacterial and fungal strains were tested, and the data obtained showed that these complexes are more active against a variety of organisms, under experiment, than free associations.
61.
Evaluation of the Antihyperlipidemic Effect of Encapsulated Octacosanol for Lipid-Lowering Effect Against High-Fat Diet-Induced Hyperlipidaemia in Experimental Rats
Singh AK, Kharb R, Chakraborty GS, Mandal SD
Abstract
Background: Elevated blood lipid levels, or hyperlipidemia, are the main risk factors for cardiovascular illnesses and are frequently brought on by high-fat diets.
Objectives: In this work, high-fat diet-induced hyperlipidemia in experimental rats is used to examine the antihyperlipidemic efficacy of a test formulation containing 1-octacosanol.
Method: A healthy female Wistar rat was utilized for investigation, separated into four groups: normal, disease, standard control, and test group, receiving the 1-octacosanol formulation.
Results: Hyperlipidemia was induced in the rats through a high-fat diet over 28 days, followed by a 28-day treatment period. Various parameters, including lipid profile (LDL, TC, TG, VLDL, HDL), body weight and antioxidant properties (MDA, SOD, GSH), were evaluated. The results showed that the 1-octacosanol formulation significantly reduced body weight and improved lipid profiles by decreasing levels of TC, TG, LDL and VLDL while increasing HDL levels. Additionally, the formulation exhibited notable antioxidant properties, contributing to its lipid-lowering effects. Statistical analysis using ANOVA and multiple comparison tests confirmed the significance of these findings, underscoring the therapeutic potential of 1-octacosanol in managing hyperlipidemia and mitigating associated cardiovascular risks.
Conclusion: The test formulation of 1-octacosanol demonstrated a significant antihyperlipidemic effect in rats with high-fat diet-induced hyperlipidemia. The treatment effectively reduced serum levels of total cholesterol, triglycerides, LDL and VLDL while increasing HDL cholesterol levels. These marks suggest that 1-octacosanol has the potential as a therapeutic agent for managing hyperlipidemia, a key risk factor for cardiovascular diseases.
62.
Unveiling the Multi-Targeted Mode of Action: Investigating the Antiepileptic Activity of Murraya koengii Extract in PTZ-induced Seizures
Bawankar RD, Kawarkhe SS, Deshmukh SP, Sawarkar HA
Abstract
Recurrent seizures are the hallmark of the neurological condition known as epilepsy.
Murraya koenigii (curry leaves) has been traditionally used in medicine for various ailments. This study aimed at the anticonvulsant activity of HAEMK using a petylenetetrazole (PTZ) induced seizure model. Behavioral and biochemical parameters were assessed to determine the effectiveness of the extract in mitigating seizures. Albino mice were orally administered with different doses of the extract prior to PTZ administration. The behavioral parameters, including seizure latency, duration and severity, were monitored and recorded. Additionally, acetylcholine esterase, GSH, and malondialdehyde (MDA), three indicators of oxidative stress, were assessed in brain tissue homogenates. HAEMK-treated groups demonstrated a substantial increase in seizure latency and a decrease in seizure length and intensity compared to the control group. A dose-dependent MDA and acetylcholine esterase decreased concurrent GSH rise were seen in the HA-treated groups. These findings suggest that the hydroalcoholic extract of
M. koenigii possesses antiepileptic activity, possibly mediated through its antioxidative mechanisms.
63.
Synthesis, Formulation and Evaluation of Zinc Oxide Nanoparticle of Capparis zeylanica L. Stem
Bhavana Jain, Kishore Burade
Abstract
The current study’s focus is on using
Capparis zeylanica L. stem extract to produce nanosized zinc oxide (ZnO) biologically in a way that is economical, effective, and environmentally safe. The synthesized nanoparticles were characterized using several techniques such as UV-Vis spectroscopy, TEM, FTIR and UV-vis spectroscopy. UV-vis spectroscopy ranges 200 to 400 nm. Having particle size 248 nm having zeta potential -3.5 mV with different groups. The current work examined by formation of gel, which shows good spreadability.
64.
Development and Characterization of Ethanolic Extract of Cleome gynandra L. Loaded Solid Lipid Nanoparticles for the Management of Diabetes Mellitus
Abarnadevika A, Ariharasivakumar G, Anusha D
, Nagalakshmi S
Abstract
The bioactive components of the botanical remedy
Cleome gynandra L., which is famous for its antidiabetic effects, were extracted using ethanol. To improve its stability, bioavailability, and therapeutic potential, the extract was subsequently encapsulated within solid lipid nanoparticles (SLNs) using a high-pressure homogenization method with varying concentrations of lipids. Zeta potential, entrapment efficiency, kinetics of drug release, and particle size were among the numerous characteristics of the SLNs that were thoroughly examined. One important measure for determining whether bioactive compounds were successfully encapsulated within the SLNs is the entrapment efficiency. An impressive entrapment efficiency of more than 82.13% was shown by the optimized formulation F4. The optimized formulation F4 exhibited a mean particle size ranging from 243.5 to 261.7 nm, according to particle size analysis. This size range is ideal for improving cellular uptake and bioavailability. A negative charge was observed in the zeta potential measurements, which means that the SLNs are stable and do not aggregate. A PDI of 0.416 provided additional evidence of the nanoparticles’ stability and uniformity. A sustained release of about 62.57% over 7 hours was shown in the
in-vitro drug release profile data, indicating a long-lasting therapeutic effect. Improved therapeutic efficacy of antidiabetic treatment and more stable blood glucose levels are both benefits of the sustained release profile. The
in-vitro results of formulation F4 suggest that SLNs have the good stability, bioavailability, and therapeutic potential of
C. gynandra L.’s ethanolic extract when used as a delivery system.
65.
Design Strategies for Improving Oral Bioavailability of Tizanidine: Solid Dispersion Approach
Manisha Saini, Suresh Kumar, Vikas Jhawat, Rameshwar Dass
Abstract
Tizanidine is a poorly soluble drug that helps relax muscles and lower mild blood pressure. Solid dispersion of tinidazole may improve the solubility of the drug. The method involved mixing tizanidine with Soluplus in different amounts using a simple tumbling method for 15 minutes. The mixtures were then stored in a desiccator. These mixtures, in different ratios (5:5, 4:6, 3:7, 2:8), were dissolved in ethanol. Tablets were made using a tablet machine with direct compression. The tablets were tested for thickness, breakability, hardness, drug content, disintegration time, wetting time, how fast the drug was released, and stability. The optimized batch (F9) showed that the drug followed a steady release pattern, with an R
2 value of 0.984. Stability studies, done under specific conditions (40°C ± 2°C/75% ± 5%RH), showed no chemical or physical changes and no noteworthy drop in drug content. The pharmacokinetic study revealed that the height concentration (Cmax) was 97.53 ng/mL, and the drug’s half-life was 1.75 hours. The formulation was optimized using a design that tested different combinations of two factors: the amount of crospovidone (superdisintegrant) and camphor (subliming agent). The goal was to improve disintegration time and friability.
66.
Superporous Hydrogels as Super Disintegrants in Formulating Oral Disintegrating Tablets of Clozapine for the Treatment of Schizophrenia
Ramesh Babu Kota, Saravanan Kaliyaperumal
Abstract
In this study, clozapine was formulated as orally disintegrating tablets (ODTs) using a direct compression method, incorporating super porous hydrogels as superdisintegrants. The disintegration time, hardness, friability, and stability of these ODT formulations were systematically evaluated, along with detailed dissolution profiles. Surprisingly, friability measurements revealed values below 1%. All tablet formulations disintegrated completely within 1 minute, meeting the 3-minute disintegration time criterion specified by the USP for ODTs. Moreover, over 85% of the labeled clozapine content was dissolved within 15 minutes from the ODTs. FTIR analysis indicated no interaction or alterations between the active ingredient and excipients. Consequently, the ODT formulations prepared using super porous hydrogels as superdisintegrants represent a promising strategy. This approach could significantly aid in the development and manufacturing of generic clozapine products.
67.
Formulation, Development and Optimization of Silymarin Loaded Nanoparticle Orodispersible Tablets for its Anti-inflammatory Activity
Radhika N Kotame, Kratika Daniel
Abstract
The objective of this work was to enhance the anti-inflammatory properties of silymarin by developing and refining an orodispersible tablet formulation loaded with nanoparticles. Formulation development and optimization of silymarin-loaded nanoparticle orodispersible tablet for its anti-inflammatory activity is the focus of this research paper. Nanoparticle drug delivery systems can help to overcome these limitations by enhancing solubility and absorption. Disintegration and dissolution of Orodispersible tablets take place in the mouth rapidly without water, providing a faster onset of action. These nanoparticles were then incorporated into orodispersible tablets containing superdisintegrants and sweeteners using direct compression. A Box-Behnken design was utilized to systematically optimize the tablet formulation based on responses including disintegration time, wetting time, hardness and friability. After 15 minutes, SL-NP Formulation -3, which contains 5% crospovidone as a superdisintegrant, demonstrated maximal drug release, or 98.5%. Rats with paw edema caused by carrageenan were used to test the anti-inflammatory potential. Following three hours, the 400 mg/kg dose showed a strong 48% inhibition; the impact grew to 52% after three hours. Overall, the development of silymarin nanoparticle orodispersible tablets shows promise for improving the anti-inflammatory effects of silymarin through a synergistic combination of nanoencapsulation and rapid disintegrating tablet technologies.
68.
Solubility Enhancement of BCS Class II Antibiotic (Azithromycin) by Solid Dispersion Technique by Using Skimmed Milk
Pavankumar Dhoble, Bharat Tekade, Nilesh Gorde, Vishal Bodke
Abstract
Azithromycin has a low water solubility; Hence, dissolution represents a rate-limiting process. The goal of the present investigation is to improve azithromycin dissolution and solubility rate. The purpose of this study was to create, characterize, and test the dissolving characteristics of an Azithromycin solid dispersion with skimmed milk. Formulated tablet of optimized batch compared with marketed formulation and study its drug release and make a formulation that gives the highest rate of solubility.
This experiment was conducted utilizing the solid dispersion method. The rationale for solid dispersion is that it produces better results than other methods while costing less. Skimmed milk is used as a carrier to increase the solubility of azithromycin. Azithromycin purity is certified using assessment tests such as HPLC assay, UV spectroscopy, FTIR, and DSC. Azithromycin solid dispersion (Azithromycin in skimmed milk) SD2 consistently performs well in all physiochemical tests as compared to all batches. The designed tablet F2 batch releases the drug more effectively than the marketed one. Azithromycin’s solubility was successfully enhanced by utilizing the solid dispersion method with skimmed milk. Batch SD 2 gives the highest results in all parameters like solubility. Preformulation study, mainly in tablet formulation, also it gives the highest solubility.
69.
Novel Approaches and Emerging Trends in Hydrotropic Solubilization Technology
Aliunui Aime, Harpritkaur Bagga, Gunjan Chaudhari, Ujwal Vyas
Abstract
Hydrotropic solubilization technology enhances the solubility and bioavailability of poorly water-soluble drugs, a major challenge in pharmaceutical research. This review discusses hydrotropic agents’ structures, the solubilization process, and factors affecting drug solubility. It explores optimizing agent concentrations, the role of computer modeling and QSAR studies, and hydrotropes’ impact on overcoming biological barriers and improving pharmacokinetics and pharmacodynamics. The review highlights hydrotropic compounds’ potential in advancing pharmaceutical formulations and clinical applications.
70.
Oral Insulin: Challenges and Potential Solutions with a Case Study of Pharmaceutical Company Ventures
Anirudh R URS, Priyanka R Bhargav, Shreya Shanbhog, Manish Danda, Narendra Kumar S
Abstract
Oral insulin, in pill form, presents a non-injectable alternative. It is a transformative approach to diabetes management, potentially enhancing patient compliance. This paper examines challenges and potential solutions in oral insulin development, which are further bolstered by a case study on pharmaceutical ventures, namely, oramed, diasome, diabetology, biocon and emisphere.
71. M
icroneedle Transdermal Patches- A Novel Painless Approach with Improved Bioavailability for the Treatment of Diseases with Special Prevalence to Neonatal Infections
Gaurav Pundir, Srishti Morris, Vikash Jakhmola, Tarun Parashar
Abstract
Microneedle transdermal drug delivery systems (TDDS) present a compelling substitute for parenteral and oral administration methods in the treatment of several illnesses. The past several decades have seen a revolution in technology that has changed the production of micro-structured devices, including the development of microneedles for transdermal patches. These devices are used to deliver drugs, proteins, insulin, antibiotics, vaccinations, and other therapies through the skin. They are proven to be beneficial for the prevention of newborn infections. Successful treatments for conditions like cancer, diabetes, rheumatoid arthritis, Alzheimer’s disease, and migraines can be achieved with the use of transdermal microneedle patches. Microneedles have the potential to offer prolonged immunity, dosage sparing, and improved protection against viral challenges. The epidermis and dermis are immunologically rich layers, and because of the needles’ micron-size structure, these devices have shown to be significantly more effective at targeting these layers, indicating their potential utility in the creation of next-generation vaccines. Within the framework of developing vaccines. Microneedle transdermal patches’ main benefits are that they are easy to use, painless, and non-invasive. Here, we discuss the types of microneedle transdermal patches and how microneedle transdermal patches are now being used to treat infections in newborns and vaccination and as a more cost-effective self-administration approach. This also enhances the bioavailability when used in vaccination therapy. Next, we’ll go over how microneedle transdermal patches are currently used to treat a variety of illnesses effectively, including those that affect newborns.
72.
Nanosponges as a Drug Delivery System: Methods, Characteristics and Applications
Madhuri Mahesh Desai, Sujata Abhay Jadhav, Akshada Amit Koparde
Abstract
Nanosponges, which are crosslinked polymer nanometers in sized used for drug transport, have a unique three-dimensional appearance. Their versatility lies in their ability to accommodate drugs of various sizes. The research approach, polymer type, and drug content determine the diversity of nanosponges. Nanosponges excel as delivery systems due to their capacity for controlled and targeted drug release. They offer the flexibility to regulate the duration of drug action and residence time. Their biodegradable composition ensures low toxicity and safe usage. Available voids, along with the size of the test molecule, play a crucial role in the efficiency of encapsulation. Nanosponges exhibit numerous applications such as cancer treatment, transportation of enzymes and biocatalysts, oxygen, modification of drug solubility, and immobilization of enzymes. This study emphasizes the preparation method, characterization, influencing factors, drug loading, recent advancements, and patents in the field of nanosponges.
73.
Drug Delivery System That Self-Emulsify: Transportation of Drug From Gut to Target Organs
Jaiswal Nilesh, Mehta Parulben
Abstract
Microemulsions are highly popular for their specific uses, including vivid applications and this is due to their special properties, which include very high interfacial interactions with demonstrated stability from a thermodynamics point of view, and on the other hand, also very low interfacial tension, which is required to solubilize highly immiscible dispersions. This review’s goal is to briefly outline potential uses of micro-emulsion systems, their uses, limitations and possible
in-vitro and
in-vivo techniques. To characterise such dispersion systems, it is commonly known that adding the right surfactant or surfactant mixture can combine large amounts of two non-dissolving-target liquids, such as water and oil, into a single phase that is macroscopically homogeneous but microscopically heterogeneous. Owing to the advantages of lymph drug delivery, the drug-lipid conjugates, when they enter the lymph route, become an ideal approach for enhancing the absorption of such drugs to combat metastatic cancers of the lymph nodes and their drainage to specific organ systems where the cancer is already spread. As the route of lymph delivery is important where a tumor has already been cancerous, this formulation approach has distinct opportunities to transport needy molecules to cancerous sites in various organs, which also includes the lymph nodes. This review, particularly, lays more stress on an overview of microemulsions in general, the
in-vivo and
in-vitro characterization methods and potential applications related to target drug delivery via the lymphatic circulatory system.
74.
Global Progress in HIV Therapeutics: An In-Depth Analysis of Dispersible Fixed-Dose Antiretroviral Combination and Their Regulatory Pathways: A Review
Nitin Mehetre, Inderbir Singh
Abstract
This review offers a detailed examination of recent advancements in human immunodeficiency virus (HIV) therapeutics, with a particular focus on dispersible fixed-dose combinations (FDCs) of antiretroviral drugs and their associated regulatory pathways. The paper highlights the global progress made in the development and implementation of these formulations, emphasizing their benefits in facilitating administration and enhanced patient adherence. Dispersible FDCs are especially beneficial for pediatric, geriatric, and bedridden patients, as they simplify dosing and improve medication compliance. The review explores the evolution of FDCs, assessing their clinical efficacy and safety profiles while also discussing the regulatory frameworks and approval processes employed by major health authorities across the globe, including the United States Food and Drug Administration (FDA) and the European Medicines Agency (EMA), and other key regulatory bodies. By analyzing these aspects, the review aims to illuminate the critical role that FDCs play in optimizing HIV treatment and their broader implications for public health. Antiretroviral therapy has significantly transformed HIV/AIDS management, leading to extended lifespan and a better enhanced well-being for patients. Fixed-dose combinations have simplified treatment regimens and improved adherence. However, the path to developing and approving antiretroviral FDC dispersible tablets is fraught with regulatory challenges. This review not only identifies these challenges but also proposes strategies to overcome them, with the goal of ensuring timely access to safe and effective medications for HIV/AIDS treatment. Through this analysis, the review contributes to understanding how regulatory practices can support the advancement of HIV therapies and enhance global health outcomes.
75.
Promising Drug Delivery System for Cervical Cancer – A Future Approach
Gayatri S Ahir, Rahul G Ingle
Abstract
There is evidence that peptide targeting can be applied in cervical cancer therapy and for diagnosis involving the use of molecular imaging, hence developing peptide probes for this disease. Cervical cancer, which also has a high possibility of being prevented, is among the common tumors affecting women globally. Despite the occurrence being reduced greatly by screening, the illness remains fatal and its claims many lives annually, especially in the developing nations. In exercising such a perspective, specific public health efforts known to encourage physical activity, proper diet, and early detection of cervical cancer must begin to be taken seriously. When combined, doctors, health officers, and lawmakers could speed up the global deployment of such programs. California’s American Cancer Society, the present review enlists a host of pharmaceutical goods available in the market. This perspective of present-day research and manufacturing is devoted to the development of various types of nanocarriers for possible utilization in medication transport. Thus, overall cancer mortality appears to be not substantially different, though cancer incidence rates for both sexes are 50% lower in impoverished countries when compared to affluent nations. At the moment, there are new peptide probes that are developed solely for cervical cancer-perfectly suitable for targeting peptides applicable in therapeutic and diagnostic imaging. M13KE phage dodecapeptide (12-mer) peptide library was screened for recognition of human immunodeficiency virus type 1 (HIV-1) by immunofluorescence and flow cytometry; the S7 clone was identified as most suitable. A disease that affects many women is gynecologic health problems, and cervical cancer is the leading presenting complaint experienced regularly. Among these studies, QSAR, drug-likeness, PCA, dynamic cross-correlation matrix, molecular docking, molecular dynamics and quantum calculation properties can be listed. In the first literature survey, after identifying the potent antibacterial and anticancer activity of the molecule apigenin, some other promising derivatives were identified and more research has been carried out on them, focusing on their synthesized derivatives as inhibitors of DNA polymerase theta and cervical cancer caused by human papillomavirus. The results were streamlined by the use of
in-silico molecular docking, which showed that all Apigenin derivatives and the targeted proteins had potential energy-binding relationships. Further validation is essential because this study used
in-silico computational methodologies and produced excellent results. Applying
in-silico molecular docking made the data more comprehensible, which showed the possible energy bindings of the targeted proteins and all the Apigenin variants. Due to the fact that this work utilized
in-silico computational methods and obtained significant results, further validation is required. Hence, the present wet-lab experiments coupled with both
in-vitro and
in-vivo conditions, additional validation of the results.
76.
Innovating Pharmaceuticals: The Rise of 3D printing in Drug Delivery
Harpritkaur Bagga, Aliunui Aime, Gunjan Chaudhari, Ujwal Vyas
Abstract
Additionally known as three-dimensional (3D) printing, additive manufacturing has made major advancements possible in the fields of engineering, business, the arts, education, and medical. Thanks to recent developments, it is now possible to print three-dimensional to create complex, useful living tissues, biocompatible substances, cells, and supporting structures are combined. Regenerative medicine is utilizing 3D bioprinting. Additive manufacturing technology, or 3D printing, has been labelled the “next big thing” and is predicted to overtake cell phones in popularity. 3D printers use digital templates to produce actual, three-dimensional items. Adding layers to a print, commonly referred to as additive manufacturing, allows for the use of more than a hundred different materials, including nylon, metal, and plastic. Applications for 3D printing can be found in many different industries, such as industrial design, manufacturing, dental, automotive, aerospace, civil engineering, education, jewellery, footwear, and geographic information systems. It has shown to be a simple and affordable solution for a variety of use cases. Using computer-aided design tools and programming, three-dimensional printing is a sophisticated technique that adds material to a base surface to create three-dimensional things. Additive layer manufacturing, also referred to as 3D printing, is the technique of creating three-dimensional things by depositing or solidifying material one layer at a time. Using a computer-aided design module, pharmaceutical components are organized in a three-dimensional pattern. Afterwards, the constituents are converted into a machine-readable format resembling the surface of a three-dimensional dosage form. 3D printing has been used for jewelry, shoe-making, architecture, engineering & construction, the automotive industry as well as the aerospace field, dentistry and medicine, plus geographic information systems (GIS), civil engineering and education. After that stage of the process is completed, the surface transferred to the machine is then printed in different layers. Bioprinting is an interdisciplinary domain that integrates additive manufacturing with biology and material sciences to manufacture three-dimensional structures representative of living organisms. The ability to create biological tissues and organs has attracted considerable attention in biomedical research owing to the rising demand for personalized medicine. This scenario propelled bioprinting forward which received much interest thus triggering comprehensive research efforts by various players such as companies, universities as well as research institutes. The goal of this book is to provide a thorough analysis of the complex and rapidly evolving field of bioprinting by critically analyzing and evaluating the existing scientific literature.
77.
A Bird Eye View on In-situ Ophthalmic Gel: Challenges and Opportunities
Raghwendra R Waghmode, Dipak P Mali, Pratibha Salve, Shivsharan B Dhadde
Abstract
Ophthalmic
in-situ gel is an advanced formulation that converts from liquid to gel upon contact with the eye, providing SR of a drug. Precise examination is crucial because of the delicate nature of ocular drug administration. Traditional methods are inefficient, leading to the rapid elimination of drugs. This article explores polymers utilized in ophthalmic delivery of drugs, detailing their applications in addition to limitations.
In-situ gelling mechanisms convert liquid preparations toward gels beneath specific conditions, enhancing the delivery of the drug upon contact with the eye. Various mechanisms like temperature, pH, and ion-induced gelation are employed based on drug characteristics and desired properties. Understanding these mechanisms allows for the design of ophthalmic gels that progress drug bioavailability and patient compliance. These polymers also aid in prodrug investigation as well as enhancing ophthalmic penetration. Overall,
in-situ ocular gels offer a hopeful approach to incapacitating challenges in the ophthalmic delivery of drugs, providing efficient and versatile drug administration with prolonged retention and enhanced bioavailability.
78.
Titanium Dioxide (TiO2): A Versatile Excipient in Pharmaceuticals
Rahul G Ingle, Samiksha S Khobragade
Abstract
Titanium dioxide (TiO
2) is a commonly used excipient in pharmaceutical formulations, offering several benefits to pharmaceutical products. As a highly insoluble and thermally stable oxide, TiO
2 is utilized as an opacifying agent and suspending agent to improve the appearance, stability, and bioavailability of pharmaceutical products. Its high refractive index and high surface area make it an excellent adsorbent and filler material, while its non-toxic and odorless nature ensures its safe use in pharmaceutical applications. Here, the authors deliberate the properties and major applications of TiO
2 as a versatile excipient in pharmaceuticals. The mesmerizing physic-chemical features of TiO
2 depend on the size and shape of particles. At present, TiO
2 has added countless considerations as an auspicious photocatalyst due to its extraordinary features such as excellent photocatalytic, electronic, and optical features, high stability, and economical and non-toxic nature. Moreover, the benefits of using TiO
2 as an excipient are discussed, including its ability to improve product appearance, stability, and bioavailability. The review also reports the challenges associated with TiO
2, including environmental concerns and biocompatibility issues. However, the benefits of TiO
2 far outweigh its drawbacks, making it an extensively accepted excipient in pharmaceuticals. Inclusively, this article aims to provide a comprehensive overview of TiO
2 as an excipient in pharmaceuticals, highlighting its unique properties, several applications, and benefits.
79.
A Discussion of the Properties of Nanoparticles
Nirosha Bolledla, Vasudha Bakshi
Abstract
Nanoparticles (NPs) have begun as versatile building blocks through applications spanning diverse fields. This review provides a general idea of nanoparticle properties, highlighting recent advancements and future prospects. Various techniques, such as sol-gel synthesis, chemical reduction, and green synthesis, offer control over shape, size, and composition, supporting custom-made production for precise applications. NPs possess high surface area-to-volume ratios and tunable optical, magnetic, and catalytic properties, alongside biocompatibility and functional ability, making them suitable for various applications. In medicine, NPs facilitate drug delivery, imaging, diagnostics, and therapeutics, ensuring targeted delivery and enhanced efficacy. In electronics, they drive advancements in displays, sensors, photovoltaics, and data storage. Additionally, NPs contribute to energy technologies like fuel cells, batteries, solar cells, and catalysis for renewable energy production. Despite their promise, NPs raise concerns about environmental and health impacts. Efforts are underway to address issues like toxicity, environmental persistence, and regulatory oversight for their safe use. In conclusion, NPs denote a rapidly progressing field with significant potential to address challenges and drive innovation across industries. Continued research and collaboration are crucial to explore their synthesis, properties, applications, and impacts, ensuring sustainable and responsible utilization of nanotechnology.
80.
Pharmacological and toxicity concerns of plant Prunus armeniaca including adoptive nanotechnology for precise delivery of their active constituents
Kunal Chandrakar, Sandeep Tiwari, Manisha Chandrakar, Khomendra Kumar Sarwa
, Ritesh Patel
Abstract
Prunus armeniaca is a well
–known apricot. Its fruit kernel and seed are mostly reported for medicinal use
. Neuroprotective, antidiabetic, and anticancer potentials are highlighted in scientific literature
. Apart from medicinal applications, various scientific reports are available to confirm its potential toxic effect especially to produce allergic symptoms, birth defects, and cyanide
–like poisoning
. Nowadays nanotechnological concepts are well applied in drug delivery systems to improve drug targetability with precision to avoid unnecessary exposure of drugs to tissues
. Delivery of active constituents obtained from this plant is also taken as payload in silver and gold nanoparticles for efficacy assessment
. The present literature summarizes the potential health benefits, toxicity, and nanotechnological advancement regarding this valuable medicinal plant
. The review concise available scientific information in a single platform covering its traditional use, geographical location, and nutritional values
.
81.
Aptamer Insights in Targeting and Designing of Therapeutic Drugs
Mishra A, Abdullah SM, Koley S, Modak S, Das A
Abstract
In the therapy of chronic and dangerous conditions like as cancer, heart disease, neurological illnesses, or retinal angiopathy, we frequently require most effective dosage schedule with adequate precision and sufficient therapeutic potential. Among these entities with the capacity to behave in a target-specific way are aptamers. Usually, they are produced by an iterative screening procedure named “Systemic Evolution of Ligands by Exponential Enrichment (SELEX)” which is used to complicate nucleic acid libraries. For several biological purposes, including targeted treatment, aptamers are potential and could be easily molded into desirable needs and also be tested in a manner that is not very extravagant or pricey. Chemical modification can be employed to enhance their pharmacological actions or prevent enzymatic degradation, hence guaranteeing their chemical integrity and bioavailability in a physiological setting. The recent advancements made in drug targeting and design with the use of aptamers are the main topic of this review. This review will highlight current developments and go over prospects and problems in the fields of aptamer-based targeted therapy, including aptamer therapeutics.
82.
Role of Lichen Extracts as a Potential Source of Natural Fungicides
Rashmi S, Rajkumar H G
Abstract
Plant pathogens and the diseases they cause are major to humanity. Each year, we lose more than thirty percent of crops worldwide to bacterial and fungal diseases. Lichen is a composite organism made up of two unrelated species: algae and fungi. These two components live together and behave as a single organism. When two organisms live together in this way, they provide mutual benefits to one another. They are referred to as symbionts. Lichens produce many rare secondary products not found in other plants. The uniqueness of many aromatic products sparked early chemical interest in lichen compounds. Lichens are an underutilized source of industrially important as it proven many biological activities, and yet there is much more to study about their efficacy. Lichen bioactive metabolites showed promising use in biopharmaceutical applications and for the preparation of new formulations or innovations to support human life. This review aims to summarize the research and development trends from the past and present in the bioactive fungicides against plant pathogens.
83.
An Extensive Review on Novel Liposomes : Classification, Methodology, Characterization, Current Formulations
Anjali Dhillon, RituVinay Singh , Kishna Ram Senwar
Abstract
Liposomes are vesicles consisting of a phospholipid, hydrophobic drug, hydrophobic tail, hydrophilic tail, cholesterol, targeting agents, positive and negatively charged lipids, and a drug encapsulated in the center of the phospholipid group having a spherical shape. The phospholipid consists of an equal number of aqueous membranes, making the liposomes an important nanocarrier for the drug delivery to the targeted site. Various liposome-based products have recently been approved and are in clinical trials. This review will discuss the structure, classification, types, and method of liposome preparation and various marketed liposomal products.
84.
An Overview of the Components, Techniques, and Innovation Used for Fast-Dissolving Films
Achal Dingalwar, Anil Pethe, Tanmay Kopare, Umesh Telrandhe
Abstract
Fast-dissolving films (FDFs) stand as a cornerstone in modern pharmaceutical innovation, heralded for their unrivaled convenience, patient adherence, and the swift onset of action. Within the realm of this paper lies a meticulous exploration of FDFs, delving deep into their intricate formulation intricacies, manufacturing methodologies, and diverse therapeutic applications. The formulation journey traverses the meticulous selection of film-forming polymers, plasticizers, taste-masking agents, and active pharmaceutical ingredients (APIs), each element meticulously calibrated to achieve optimal efficacy. Diverse production techniques, spanning solvent casting, hot melt extrusion, and spray drying, are scrutinized with precision, shedding light on their inherent advantages and nuanced limitations. Beyond the realm of formulation and manufacturing, this review embarks on an expansive voyage into the vast therapeutic landscape that FDFs traverse. From the treatment areas of central nervous system disorders to the realms of cardiovascular diseases, allergies, and pain management, the versatility and adaptability of FDFs emerge as a beacon of hope for patients and practitioners alike. Yet, amidst the brilliance of FDFs, inherent challenges linger, from stability concerns to the intricate dance of bioavailability and the ever-watchful eye of regulatory scrutiny. However, within these challenges lies the fertile ground for future research and development endeavors, beckoning forth a new era of innovation and advancement in the realm of rapidly dissolving films. This study stands as an indispensable compass, guiding researchers, pharmaceutical scientists, and practitioners toward the forefront of FDF development and implementation.
85.
Designing a Prevention Skills Activity Module for Drug Trainees
Siti Hajar Halili, Hamidah Sulaiman
Abstract
Drug abuse affects all groups regardless of whether they are highly educated, professional, unemployed, or uneducated. This drug prevention skills activity module contains five skills, namely problem-solving skills, personality problem-solving skills, healthy lifestyle skills, self-adjustment skills, and stress management skills. Each skill is equipped with at least five activities to enable users of this module to gain skills and be able to apply them in their lives. This module provides benefits to prospective counselors and trainees because, from this activity, the trainees can understand the overall summary of the activities that have been carried out. It is hoped that this module is beneficial and can be applied to increase awareness of drug abuse in families and communities in this country.
86.
An Overview of Three-Dimensional Printing in Pharmaceutical Technology
Prasanthi Boddu, Ushaswi Akula, Pranathi Karanam
Abstract
Three-dimensional printing (3DP) in pharmaceutical technology is a new technique that can build the desired objects directly from CAD models using a layer-by-layer material build-up approach. This article presents an overview of the 3DP technique with a brief look into the history of the 3DP process and various methods like stereolithography, fused deposition method, hot melt extrusion, polyjet, etc., their merits and demerits, and applications of 3DP in pharmaceutical technology. The challenges 3DP has surmounted in the areas of pharmaceutical and biomedical research related to additive manufacturing are outlined in this review.. The use of 3DP has increased recently. Personalized medicine may now have access to a whole new range of options due to 3DP. The concept of specialists and researchers is to create customized oral pills using 3DP. Since technology is still developing, any regulations on security, safety, and privacy have yet to exist. Thus, these issues will be of more significant concern shortly. The applications of 3DP technologies in modern drug delivery are highlighted in this article, which expounds on using these technologies for forward-thinking advancements in pharmacy practice.
87.
Lipids Selection and Methods of Nanostructured Lipid Carrier for Topical Use
Rahman F, Hendradi E, Purwanti T
Abstract
Background: The utilization of nanoparticle systems presents a promising means for enhancing the efficacy of specific therapeutic interventions, particularly in topical applications. One of the nanoparticle systems that possesses several advantages is the nanostructured lipid carrier (NLC). It is comprised of solid and liquid lipids that form a lipid matrix with the addition of a surfactant. The utilization of lipids in NLC could impact various physical characteristics and drug release.
Objective: This study aims to ascertain the considerations involved in selecting solid and liquid lipids.
Method: The research approach to be undertaken is a systematic literature review, which refers to an investigation conducted through the process of identifying, evaluating, and interpreting all pertinent findings related to a study, topic, or phenomenon associated with NLC.
Results: the obtained results reveal that various NLC-related articles indicate that polymorphism, the solubility of active compounds, and the ratio of solid and liquid lipids may exert a significant influence on the physical characteristics and release of active compounds.
Conclusion: Consideration of the choice between solid and liquid lipids can be made to optimize topical therapeutic efficacy.
88.
Harnessing the Power of Curcumin: Evaluating Its Efficacy as an Antileishmanial Agent in the Fight Against Leishmaniasis
Minal Gopichand Ambilkar, Gaurav Sanjay Mude, Aashumi Ashok Kucheriya, Rahul Madhukar Bhoyar
Abstract
Over 100 countries are impacted by the dangerous parasite disease leishmaniasis, which is categorized as a neglected tropical disease (NTD). Protozoan parasites use sandflies and other vectors to spread the disease. Herbal compounds like turmeric curcumin have demonstrated promise in the treatment of parasitic illnesses despite their limited bioavailability and water solubility. From small, self-healing skin lesions to serious intestinal infections, leishmaniasis can cause a wide range of illnesses in humans. Since there isn’t a gold standard test for one type, mucocutaneous leishmaniasis (MCL), it can be difficult to diagnose. Treatments for MCL can be quite harmful, which emphasizes how crucial a correct diagnosis. This study aims to assess the diagnostic performance of PCR (polymerase chain reaction) for MCL and to compare the findings with the authors’ most recent clinical research findings.
89.
Recent Advances and Future Prospects in Polymer-Mediated Drug Delivery Systems: A Comprehensive Review
Bharathy, Pavithra, V Thanikachalam, Punniyakoti
Abstract
Polymer-based drug carriers have revolutionized the pharmaceutical landscape, providing innovative approaches for efficient drug delivery. These advanced systems have significantly mitigated traditional challenges, offering new avenues for targeted and controlled drug release. This paper aims to explore polymers, focusing on their classification, properties, drug release mechanisms, and pharmaceutical applications while emphasizing recent advancements and future prospects in the field. Polymers can be classified based on their origin, biodegradability, and physical properties. Their unique characteristics, such as biocompatibility, flexibility, and ability to modify surface properties, make them ideal for drug delivery applications. The review delves into various drug release mechanisms employed by polymer-based systems, including diffusion, degradation, swelling, and stimuli-responsive release. These mechanisms ensure a controlled and sustained release of therapeutic agents, enhancing efficacy and reducing side effects. The pharmaceutical applications of polymer-based drug carriers are vast, encompassing targeted delivery to specific tissues or cells, sustained-release formulations, and the delivery of complex molecules like proteins and nucleic acids. Despite their advantages, polymer-based drug delivery systems face limitations, including potential toxicity, stability issues, and manufacturing challenges. Addressing these limitations through continued research and development is crucial for advancing the field. Recent advancements, such as smart polymers and nanotechnology integration, hold promise for overcoming these challenges and improving drug delivery efficiency. In conclusion, polymer-mediated drug delivery systems represent a significant leap forward in pharmaceutical technology. This review highlights the importance of polymers in modern medicine, their potential to revolutionize drug delivery, and the ongoing efforts to optimize their use in clinical applications.
90.
Prescribing Pattern of Antidiabetic Drugs and Its Adherence to American Diabetes Association Guidelines in Patients of Type 2 Diabetes Mellitus with and Without Comorbidities
Amin SS, Jogdand SD
Abstract
Diabetes mellitus is a persistent metabolic illness defined by high amounts of glucose in the blood, and it presents a substantial worldwide health problem. The incidence of diabetes is escalating at a quick pace as a result of variables including urbanization, lack of exercise and changing dietary patterns, particularly in developing countries where undiagnosed cases are prevalent. This review examines the prescription patterns of antidiabetic drugs for type 2 diabetes mellitus patients (T2DM), both with and without comorbidities, and evaluates adherence to the American Diabetes Association (ADA) guidelines. Effective management of T2DM is critical to preventing complications, but poor medication adherence remains a significant issue, leading to adverse outcomes and high healthcare costs. This review analyzes commonly prescribed oral hypoglycemic agents, their mechanisms of action, and side effects and discusses the importance of managing T2DM to prevent microvascular and macrovascular complications. Challenges in adhering to ADA guidelines include lack of awareness, physical and architectural barriers, effective communication, and financial constraints. Addressing these challenges through multidisciplinary care, continuous medical education, and comprehensive public health interventions is essential for improving patient outcomes and mitigating the global diabetes epidemic.
91.
Quantum Dots: An Emerging Approach for Lung Cancer Management
Bhawna, Choti Kumari, Yogita Ale, Neha Kukreti
Abstract
Nanotechnology is an empirical approach that promises hope and novel treatment possibilities for cancer. This state-of-the-art technology offers innovative methods for diagnosing and treating a variety of illnesses. Though there have been some positive advances since the discovery of quantum dots (QD) nano-transporters, these advances are still in their development, even though they have been shown to be beneficial to society. QD has shown to be incredibly suitable for bio-imaging, targeted gene delivery, pharmacological research, biosensing, photodynamic therapy, and diagnosis through its usage in natural imaging and photography. The overview’s main goal was to emphasize how important QD is for both cancer detection and therapy. The goal is to provide readers with a basic understanding of QD, including its benefits and applications in lung cancer management. Furthermore, we have discussed the many studies pertaining to cytotoxic analysis in order to demonstrate the safety of QDs. The current study provides a concise summary of the current research, fabrication methods, and applications of QD in lung cancer treatment.
92. Potency of Natural Compounds in Inhaled Micro/Nanoparticle for Lung Infection Therapy
Shafa Azaria, Noorma Rosita, Dewi Melani Hariyadi
Abstract
Pulmonary infection is a disease-causing death worldwide that attacks the lower airway organs by various kinds of microorganisms. Antibacterial or antiviral has been used for the therapy of lung infections, but up to this point the case of resistance to drugs is still high. Therefore, to overcome this problem, it is necessary to develop new drugs, namely natural drugs. However, natural drugs have limitations (physicochemical properties and low bioavailability), so the development of inhalation natural drug delivery systems is needed. Various studies have been conducted to develop inhalation natural drug delivery systems such as microparticles, microsponges, nanoparticles, nanomicelles, etc. The use of these delivery systems has been shown to have a positive impact on the physico-chemical properties, bioavailability and antibiotic/antiviral activity of natural drugs through targeted delivery of lungs both
in-vitro and
in-vivo.
93.
A Review on Proniosomes as a Novel Drug Delivery System
Prasanthi Pakalapati, Manthina Mohan Varma
Abstract
Proniosomes are desiccated versions of surfactant-coated, water-soluble carrier particles. Before usage, on agitation in heated aqueous solution, they are rehydrated in a matter of minutes to create niosomal dispersion. In storage and transit, proniosomes maintain their physical stability. The drug contained within the proniosomes’ vesicular structure increases the drug’s potency, improves its absorption into the target tissue, and lowers its toxicity. Niosomes are technically more promising than liposomes as drug carriers since they are more chemically stable and don’t have many of the glitches of liposomes, like high cost and problems with phospholipid purity. Focusing on proniosome preparation, characterization, and application in targeted drug delivery, this study highlights their general approaches.