1. Study on Natural Gums and Resins as Release Retarding Agents in Development of Sustained Release Matrix Tablets of Didanosine
Y Indira Muzib, K Swetha, YR Ambedkar
Abstract
Didanosine is an anti-retroviral drug which helpful in preventing human immunodeficiency virus (HIV) from multiplication in the body. This drug has a relatively short half-life and low absolute bioavailability and requires frequent dosing. So to avoid this frequent dosing and to improve the patient’s compliance, the development of sustained-release tablets is necessary. Natural gums and resins play an important role in retarding drug release. Didanosine extended-release matrix formulations developed with wet granulation using gum kondagogu, guar gum, gum olibanum, and olibanum resin, and evaluated for pre and post-compression parameters. The outcome of all evaluation tests is reached IP specifications. Formulations with kondagogu F1-F3 failed to extend the drug release. F4-F6 was formulated with gum kondagogu and guar gum, in which F4 prolonged the release up to 12 hours with 98.23%. The formulations F7 with olibanum resin release 96.13%, and F10 with gum olibanum releases 93.15% drug at the end of 12 hours. The conclusion from the study was that natural polymers could be used to enhance drug release for an extended period.
2. Validated Area Under Curve Quantitative UV Spectrophotometric Analysis of Rebamipide in Drug Formulations
Karajgi SR, Kulkarni RV, Potadar SS, Ingale Anand
Abstract
A very simple, accurately perfect, precisely repeatable procedure has been proposed for the estimate of rebamipide in medicines. Evaluation of previous works indicates the fact that, so far no UV spectrophotometric scheme for quantifiable estimate by area under curve technique for the drug rebamipide is not described. Therefore, there was a need to plan a different methodology to analyze the medicine employing dimethyl formamide in the form of solvent. This medication monitors Beer’s law in the range of concentration 20 to 200 μg/mL in the ultraviolet range, particularly areas between 320 and 340 nm for are under curve because the absorption maximum was found to be 330 nm in the selected solvent. The recovery readings proved the offered technique’s accuracy and outcomes were authenticated par accordance with the International Council for Harmonisation (ICH) references. The discoveries were reasoned to be consistent as well as agreeable. As a consequence, this optional technique was successfully used to estimate rebamipide quantitatively in conventional analytical applications.
3. Novel Proniosomes of Manidipine: Optimization and
In-vivo Evaluation
J Ashwini, Vasudha Bakshi
Abstract
The objective of the current study is to produce proniosomes of manidipine using the thin film hydration method for the management of hypertension. Statistical optimization was performed using the Box-Behnken design. The generated formulations were tested for particle size, entrapment effectiveness, and drug release at 12 hours. The improved proniosomes were further assessed for surface morphology, ATR, and differential scanning calorimetry (DSC). The improved proniosomes were also assessed for an
in-vitro and
in-vivo investigation on dexamethasone-induced hypertension. It was noted that there was no significant interaction with excipients. DSC indicated a considerable shift in the endothermal peak and showed interaction with the study’s excipients. Niosomes and drug crystals were seen to be dispersed in small areas during the scanning electron microscope (SEM) analysis. The study also showed that the optimized proniosomes have asymmetrical surfaces and appearances. The zeta value in the research was -6.7 mV, indicating stability. According to the optimized proniosomes formulation, F14 released 99.97% of the drug at its highest concentration in 12 hours. ANOVA results from an
in-vivo investigation confirmed a satisfactory outcome in decreasing raised blood pressure, as shown by the F and
p-values.
4. Kojic Acid Containing Novel Drug Delivery System on Facial Dyschromia: Characterization and Their Evaluation
Prantika Mondal, Vijay Bhalla, Reena Tyagi
Abstract
Stubborn skin pigmentation issues like post-inflammatory hyperpigmentation (PIH) and melasma are the primary reasons people seek cosmetic consultations. Treating these conditions topically is challenging, as it involves inhibiting various stages of production of the pigment process. A powerful tyrosinase inhibitor like, kojic acid (KA) is employed as a formulation to regulate pigmentation production by suppressing the melanogenesis process. It’s important to note that the application of KA has been approved by the Food and Drug Administration (FDA), US, for dermatological treatments. The goal of this investigation was to formulate a nanoemulsion containing kojic acid for skin delivery using an emulsification method. The characteristics of the KA nanoemulsion were thoroughly examined through techniques like fourier transform infrared spectroscopy, (FTIR) particle size analysis and transmission electron microscopy (TME). In addition, the formulation’s performance was evaluated through both
ex-vivo permeation study and
in-vitro release study. Analysis of the FTIR, X-ray diffraction (XRD), and differential scanning calorimetry (DSC) results revealed that kojic acid with other ingredients in the formulation did not exhibit any chemical interactions. The kojic acid nanoparticles that were produced exhibited a spherical shape and were uniformly distributed, with an average size diameter of 184 nm. In
in-vitro tests, it was observed that 87.67% of the drug was released within 12 hours. Moreover,
ex-vivo permeation evaluation demonstrated that 81.24% of the drug permeated the skin within 8 hours of application. The thermal stability studies confirmed the stability of the kojic acid nanoemulsion, with no signs of creaming, cracking, or phase separation in the formulation. In conclusion, the findings of this study suggest that the kojic acid nanoemulsion holds great promise as an effective means for delivering kojic acid within the upper layers of the skin for treating of facial dyschromia.
5. Preparation and Evaluation of Rebamipide Ophthalmic Nanosuspension for Dry Eye Therapy
Reena Tyagi, Vijay Bhalla
Abstract
Dry eye syndrome poses a therapeutic challenge due to the limited residence time of traditional treatments on the ocular surface. The commercially available rebamipide (REB) ophthalmic suspension, though approved for clinical use in dry eye patients, suffers from rapid drainage through the nasolacrimal duct, limiting its effectiveness. In this study, rebamipide nanosuspension was successfully developed by solvent-diffusion methodology and investigated for measurement of particle size, shape, surface charge, fourier-transform infrared (FTIR), differential scanning calorimetry (DSC), percentage entrapment efficiency, dissolution studies and release kinetics,
ex-vivo permeability study. Results demonstrate that the optimized formulation has 196 nm particle size, surface charge of +32.5 mV, and low polydispersity. FTIR studies revealed that the drug exhibits compatibility with the excipients integrated into the formulation. DSC and X-ray diffraction (XRD) analysis revealed a decrease in the crystalline nature of the drug. Transmission electron microscope (TEM) findings indicate that rebamipide nanosuspension possesses a spherical shape, and
in-vitro studies demonstrate a slower and sustained release of REB.
Ex-vivo studies performed on excised goat corneas demonstrated significantly improved drug permeation compared to the suspension without inducing corneal damage.
6. Molecular Docking, Synthesis, Antiproliferative Activity against MCF-7, and
In-vitro Alpha Amylase Activities of Newer Generation Pyrimidino Hydroxamic Acid Derivatives
Samiya, Supriyo Saha, Vikash Jakhmola, Nidhi Gairola, Mahipal Singh
Abstract
A set of newer generation pyrimidine hydroxamic acid derivatives were designed, synthesized, and evaluated for antiproliferative activity against breast cancer cell line and
in-vitro alpha-amylase activity. The design of the molecules was fully dependent upon the structural features of suberoyl anilide hydroxamic acid. Then all the designed molecules (S1-S100) were docked with 4LXZ HDAC2 enzyme and S1, S2, S16 showed good docking interaction scores as compared to SAHA. The interacting residues of (S1, S2, S16) and 4LXZ showed similar amino acid lining as present in the active site. The synthetic procedure of the molecules (S1, S2, S16) was divided into three parts such as synthesis of chalcone derivative using aromatic aldehyde and acetophenone, the reaction between chalcone and thiourea to form substituted pyrimidine-2-thiol, then finally substituted pyrimidine-2-thiol and 2-chloro-N-hydroxyacetamide reacted in the presence of dimethylformamide to obtain the best-docked molecules. All the molecules showed characteristic peaks in fourier-transform infrared (FTIR), proton nuclear magnetic resonance (1H-NMR) and mass spectrometry with sharp melting points and single peak in thin layer chromatography (TLC) plate. Finally antiproliferative activity against MCF-7 and
in-vitro alpha amylase activity data confirmed that S1 was the best molecule among all the synthesized molecules.
7. Retracted
8. Formulation and Evaluation of Naringin Loaded Transdermal Patches using 3
2 Full Factorial Design
Namrata Singh, Surya Prakash Gupta
Abstract
The main goal of the current study was to maximize the bioavailability of naringin by prolonging the drug’s release using transdermal patches. Ethyl cellulose (EC) served as the lipophilic component and hydroxy propyl methyl cellulose (HPMC) as the hydrophilic matrix in the preparation of transdermal patches. A 32-complete factorial technique was used to build the optimal design matrix, altering the ratio between the hydrophilic and lipophilic matrices. To create the best optimum formulation, three alternative ratios of EC and HPMC were employed. The patches had pH values ranging from 5.28 ± 0.006 to 5.62 ± 0.015. The transdermal patches had thicknesses ranging from 0.514 ± 0.004 to 0.697 ± 0.004 mm. The average weight of the prepared transdermal patches ranged from 194.67 ± 0.578 to 241.67 ± 1.528 mg. The transdermal patches’ moisture content ranged from 7.23 ± 0.158 to 10.33 ± 0.158%. Tensile strength values of the prepared transdermal patches ranged from 9.59 ± 0.006 to 10.41 ± 0.035 kg/cm2, while the drug content varied from 94.7 ± 0.6 to 97.33 ± 0.208%.
9. Incorporating Kappa-carrageenan in Liposomes Facilitates Development of Lipopolysaccharide Hybrid Nanoplatform
Suvaasni Prasad, Kiruthigaa Krishnan, Sivaramakrishnan Venkatabalasubramanian
Abstract
Sulfated polysaccharides (kappa-carrageenan) integration in lipids provides diverse structural and physicochemical properties in nanotechnology. Such a lipopolysaccharide hybrid (LPHS) system offers superior applications in the food and pharmaceutical industry. This study investigates the synthesis and characterization of sulfated polysaccharide (kappa-carrageenan: κ-CG) integrated smart liposomes (cubosomes) for establishing cubic tendency in the LPHS system. The κ-CG integrated smart liposomes were prepared using the modified thin film hydration approach. Characterization studies (liposomes and smart liposomes) were performed using dynamic light scattering (DLS), scanning electron microscopy (SEM), and transmission electron microscopy (TEM). DLS studies confirmed the nano-range of both delivery systems. The SEM and TEM investigation revealed the formation of classical cubic morphology of the smart liposomes. Sulfated polysaccharide (κ-CG) integrated smart liposomes exhibited an enhanced κ-CG release profile compared to the liposome-free κ-CG alone. This was due to improved entrapment efficiency (68%) and better overall stability established by the κ-CG incorporation.
10. Exploring Antipsoriatic Potential of
Aloe vera Gel
Swapnil Shinde, Shrinivas Mohite
Abstract
Research centers on conducting a phytochemical analysis of
Aloe vera Linn leaf extracts, with an investigation into the existence of lead acetate solution, proteins, alkaloids, carbohydrates, flavonoids, cardiac glycosides, steroids, sulfur tests, and tannins. The gel formulation was tested for color, appearance, and homogeneity, and all batches produced gels that were easy to spread. Scores of 90% for the gel’s extrudability, 80% for its quality, and 70% for its fairness were given. Inhibitory effects against HaCaT cell lines were observed with the synthetic herbal component
Aloe vera Linn. These effects were minor when compared to the positive control 5-FU. Several aqueous plant extracts were tested for antipsoriatic activity using the Perry scientific mouse tail method. When compared to retino A cream, the aqueous extract of
Aloe vera Linn gel (500 mg/kg) improved ortho keratotic regions by 59.26%. Results suggest that
Aloe vera Linn leaf extracts may have a variety of functions, including antipsoriatic and therapeutic. To completely grasp the versatility of these plant extracts, additional research is necessary.
11. The Physical Stability of Ciprofloxacin and Levofloxacin Parenteral Dosage Forms in the Polypropylene Plastic Container
Dewi Isadiartuti, Retno Sari, Dini Retnowati, Violyta Ade Gunawan, Risma D Yanti, Oki Yudiswara
Abstract
Polypropylene (PP) plastic container is often used as alternatives to glass containers in the primary packaging of parenteral dosage forms, but the usage poses a risk of interaction with the preparations during moist heat sterilization. Therefore, this study aimed to evaluate the physical stability of ciprofloxacin and levofloxacin parenteral dosage forms packaged in PP container after moist heat sterilization. Parenteral preparations were produced by dissolving the active ingredient ciprofloxacin lactate or levofloxacin hemihydrate in water for injection solvent. The solution obtained was then packaged in a 100 mL PP container and subjected to moist heat sterilization at 115°C for 30 minutes. The physical stability of the samples was then tested, including the weight, pH, clarity, number of particles, and sterility. The physical quality parameters before and after sterilization were compared. Data were analyzed using the paired t-test with significance at α 0.05. The results showed that parenteral preparations were sterile and maintained consistent physical stability after being sterilized, except for the number of particles. Furthermore, the number of particles in the sample met the standard requirements. Based on the results, ciprofloxacin or levofloxacin parenteral preparations in PP containers fulfilled the physical stability requirements after moist heat sterilization.
12. Formulation and Evaluation of Electrospun Nanofiber Mats of Curcumin and Leaf Extract of Tinospora cordifolia: Designed for Accelerating Diabetic Wound Healing
Nagansurkar SB, Hemant KS Yadav, Raizaday Abhay
Abstract
Traditional herbs like
Tinospora cordifolia and curcumin have many therapeutic benefits. However, curcumin’s limited bioavailability is a problem. Electrospun nanofibers are an answer because they increase the effective surface area greatly, and make drug delivery better in almost all aspects. The combination in the form of nanofibers can be greatly useful in the treatment of diabetic wound healing, where curcumin, the known antibacterial and anti-inflammatory element, plays an important role. It is observed that when combined with extract of leaves of
T. cordifolia, which has known antidiabetic and wound healing actions, blended in the chitosan polymer, which is itself a weak antibacterial compound hence can be one of the solutions to the menace of bacterial resistance which is very common in diabetic wound healing. This research aims to create and test electrospun nanofiber mats of curcumin and
T. cordifolia leaves extract blended in chitosan as a base polymer in the treatment of diabetic wound healing. Leaves of the plant
T. cordifolia, which were collected from the institute’s botanical garden, were subjected to drying and then prone to solvent extraction using methanol and acetone, resulting in the production of bioactive extracts. The curcumin was obtained as a gift sample from Sanjay Chemicals, Mumbai. Nanofibers were electrospun from chitosan,
T. cordifolia leaf extract and curcumin. Characterization included scanning electron microscope (SEM), water contact angle measurement, TGA/DSC analysis, drug release studies, fourier-transform infrared (FTIR) analysis, swelling tests and
in-vitro release profiling. The nanofiber mats of curcumin and leaves extract of
T. cordifolia using chitosan as a base polymer were prepared and evaluated at various parameters. The results we found are very promising. The nanofibers formed by using electrospinning techniques show good content uniformity as well as good diameter which was checked using SEM. The study confirmed no component interactions using differential scanning calorimetry (DSC). The good hydrophilicity of mats was found to ensure good retention time. The study concluded with the formation of a novel formulation that can fight the menace of bacterial resistance, which is very common in the diabetic wound healing process. The formulation will ensure not only countering bacterial resistance but also the faster healing of diabetic wounds, as
T. cordifolia leaves extract is known to improve angiogenesis and tissue remodeling.
13. Calendula Oil Associated Dexibuprofen Nanoformulation Transdermal Patches: Formulation and Characterization
Sharan Babu RS, Sowmya C, Rohith S, Mahalakshmi K, Monisha K
Abstract
Objectives: To prepare and characterize the nanoparticle-based topical formulations of dexibuprofen in combination with calendula oil to enhance the topical anti-inflammatory effect.
Methods: Chitosan and tri poly phosphate (TPP) were used to prepare nanoparticles developed utilizing the ionotropic gelation technique and analyzed by scanning electron microscope (SEM) and the ZS. Solvent casting was used to prepare the transdermal medication delivery system for the chitosan nanoparticle formulation.
Results: Results revealed that nanoparticles were between the sizes of 267.3 nm. This particle size may enhance the drug’s solubility and penetration through the skin. These patches containing chitosan nanoparticles were produced utilizing polymer combinations – HPMC, chitosan, and PEG400 with tween80 as plasticizers. Accompanying the rise in hydrophilic polymer content came an increase in the rate of medication release via the patch.
Conclusion: Transdermal patch – F3 released the drug reasonably well.
14.
In-vitro Study on Anthelmintic and Insecticidal Activity of Macrolichens Collected from South Karnataka
Kavana NL, Rashmi S
Abstract
In the present study, lichen samples were collected from the southern Karnataka state and were used for
in-vitro anthelmintic and insecticidal activity. The three lichen samples
Parmotrema tinctorum (Nyl.) Hale,
Roccella montagnei Bèl. Emend. Awas,
Everniastrum cirrhatum (Fr.) Hale was subjected to the extraction with solvents. The prepared extracts from the lichen species were evaluated for anthelmintic activity against
Pheretima posthuma. 100% mortality was obtained from all the samples and it was compared with the reference drug albendazole for positive control.
P. tinctorum methanolic extract showed the fastest result but on the other side, the slowest result was observed in the hexane extract. The insecticidal activity of the crude extracts of the lichens was tested against two insects
Macrosiphum rosae (L.) and
Sitophilus oryzae (L.). There was a 100% mortality rate observed in
R. montagnei and E.
cirrhatum methanolic extracts against
M. rosae. In
S. oryzae the methanolic extracts of
P. tinctorum and
E. cirrhatum with 75 and 50% mortality rates at 42 and 48 hours was observed. The promising results of lichen extracts towards insecticidal and anthelmintic activity were found to be a potential candidate for drug discovery and development against biopesticides.
15. Development of a Robust and Reliable RP-HPLC Method for the Estimation of Finerenone in Tablet Dosage Form
Sumalatha Chepyala, Srinivas Medidi, Jitender Kumar Malik
Abstract
An advanced analytical method was explored, specifically tailored for estimating finerenone, a vital drug found in tablet formulations intended to reduce the risk of chronic kidney disease in patients with type-2 diabetes. This sophisticated technique employs an Inertsil ODS 3V C18 column (5 μm particle size x 250 x 4.6 mm) for precise separation of analyte. The mobile phase consists of an ammonium dihydrogen phosphate buffer (pH 4.5) and acetonitrile (60:40), which is a carefully balanced mixture that flows consistently at 1.0 mL/min. UV detection is achieved at a wavelength of 238 nm. Finerenone’s characteristics are unveiled with a brief retention time of 4.06 minutes, highlighting the efficiency of the method. The method demonstrates linearity within the concentration range of 2.5 to 15 μg/mL, offering a comprehensive scope for accurate analysis. This robust reversed-phase high-performance liquid chromatography (RP-HPLC) method undergoes thorough validation following International Council for Harmonisation (ICH) guidelines, ensuring its reliability. Notably, the accuracy is impressive, with a mean recovery falling comfortably within the acceptable range of 99.76 to 101.09%. In summary, our analytical approach stands out for its simplicity, precision, sensitivity, rapidity, and robustness in estimating finerenone in tablet formulations.
16. Lipid Nanoemulgel Therapy for the Treatment of Keratoconjunctivitis Sicca: Cyclosporine Formulation Characterization and
In-vitro Evaluation
Phadatare Suvarna P, Kurumkar Pritish P, Wanegaonkar Anjali M, Jadhav Varsha M
Abstract
Nanoparticulate carrier systems play a significant part in enhancing ocular bioavailability. Emulgels are a potential new delivery method for the administration of lipophilic drugs like cyclosporine A (CsA). In the present research work, CsA, the immunomodulatory drug with a wide safety profile, has been formulated into nanoemulgel for treating vision-threatening ocular surface disorder
viz. Keratoconjunctivitis sicca. The objective of this study was to prepare lipid-based nanoemulsion gel of CsA aiming to prolong corneal residence time and increase ocular bioavailability. Ophthalmic nanoemulgel was prepared using suitable vehicles, preservatives, hydrophilic and lipophilic emulsifiers
viz croduret 40, poloxamers, spans, polyethylene glycol, polyoxyethylene 40 stearate, etc., by probe sonication method. It was evaluated for physical appearance, particle size, pH, viscosity, drug release, assay, and stability, etc. using appropriate methods. The pH and osmolarity of transparent ocular liquigel were 7.2 and 155 mOsm/L respectively. The particle size analysis and cryo scanning electron microscopic images of ocular nanoemulgel showed a monodisperse system containing a globule mean size of 190.2 ± 8.93 nm. The drug content was 99.5% w/w and the
in-vitro diffusion studies showed that the medication was released for 6 hours; followed first-order kinetics with a high regression coefficient (r2) of 0.982. The lipid carrier-based topical cyclosporine ophthalmic liquigel was developed and evaluated. The
in-vitro study has shown uniform, smooth-surfaced globules of size < 200 nm and prolonged drug release up to 6 hours; thus indicating increased corneal residence by nanocarrier-based gel system.
17. Formulation and Evaluation of Herbal Hair Serum
Yashshree N Yenurkar, Rahul G Ingle
Abstract
In daily life, there is a rising demand for cosmetics and are used by a large number of individuals annually. Humanity employs a variety of goods to accentuate elegance and attractiveness in order to appear youthful and endearing. Therefore, cosmetics are essential to human survival. Because of the perception that herbal cosmetics are safer and have fewer adverse effects, they are utilized extensively these days. One of the main bodily components that serve as a protective appendage is hair. The spreadability test and stability test results were all assessed. It was the development of a daily-use herbal hair serum is the main objective of this study. To achieve this, a range of herbs will be employed, and the ideal formulation will be determined by evaluating the cosmetic serum’s qualities. Three different cosmetic serum formulations (H1, H2, and H3) with different excipient concentrations have been developed. Physical properties, pH, homogeneity test, and viscosity ensured that every parameter fulfilled the norms and was in good condition. Herbal compositions have been shown to be useful in improving hair consistency.
18. Formulation Optimization and Evaluation of Herbal Films Containing Ethanol Leaves Extract of
Cassia auriculata to Treat Chronic Constipation Disorder
Brahmaiah Bonthagarala, Seetha Devi Alla, Sudarshan Rao Nagineni, Rama Rao Vadapalli, Sri Rekha Malakapurapu
Abstract
An intriguing trend in recent years has been the designing of oral films containing extracts from medicinal plants. Therefore, efforts were made in the current work to create fast-dissolving herbal films using
Cassia auriculata ethanol leaf extract in order to create a dosage form that would be more convenient to administer and treat chronic constipation disorders in the elderly. Varying ratios of hydroxy propyl methyl cellulose as polymer, propylene glycol as film softener, and a solvent-casting approach were utilized to create the quickly dissolving herbal films of
C. auriculata leaf extract. A number of quality control measures, including weight fluctuation, thickness variation, surface pH, percentage moisture uptake, percentage moisture loss, disintegration time and folding endurance, were assessed. According to the findings, every film had a decent appearance, a smooth texture, was free of particle matter, and had excellent folding endurance. According to a content uniformity analysis, the drug is dispersed evenly across the entire film, and each one dissolves in less than 95 seconds.
In-vitro dissolving studies using Paddle type apparatus in pH 6.8 phosphate buffer pH 6.8, which is simulated saliva, were performed for each film composition. Out of all nine formulations, formulation F5, which is an herbal film with 10% propylene glycol and 40% HPMC, exhibited complete drug release (99.6%) in 30 minutes and had a strong folding endurance value. The release of medication from films was found to follow a first-order kinetics. Overall, studies indicate that the most feasible dose form that can be used in medical settings for the treatment of chronic constipation disorder is fast-dissolving herbal films containing
C. auriculata leaves extract. This is especially true for patients who have difficulty swallowing.
19. Estimation of Imeglimin in Pharmaceutical Tablets by RP-HPLC
Shubham Jahagirdar, Rahul Godge, Sneha Vikhe, Snehal Bornare
Abstract
Objective: This study’s primary goal is to create a novel, sensitive and comprehensive reverse phase-high performance liquid chromatography (RP-HPLC) procedure. The computation of Imeglimin’s dose and dosage is the primary goal.
Method: Chemicals and impurities were separated chromatographically using a C18 (AGILENT) chromatographic column. Methanol and 0.1% OPA are present in the mobile phase in a 40:60 v/v ratio. A 240 nm ultraviolet light detector was employed for the purpose of detection. With a retention time of 4.718 minutes, the results demonstrated the effectiveness of meglimin. After adjusting the flow rate to 0.7 mL/min, there was good separation. There are several imeglimin doses planned, ranging from 10 to 50 μg/mL. 101.46 to 101.12% in yield.
Results: This method’s validation has good accuracy, sensitivity, precision, linearity, specificity, and robustness, and it satisfies the requirements of the International Conference on Harmonization.
Conclusion: In conclusion, imeglimin was predicted and the construction method was isolated. In conclusion, it’s feasible for daily use.
20. Development and Validation of New LC-MS/MS Bioanalytical Method of Tremelimumab in Rat Plasma by Using Nivolumab as Internal Standard and Its Application with Pharmacokinetic Studies
Alapati Sahithi, Asha Deepti
Abstract
Nivolumab was decided to be used as the IS. To separate the drugs, an isocratic mobile phase of acetonitrile (ACN): Ammonium formate containing formic acid (70:30) was adopted and delivered at 1-mL/min, along with a 150 x 4.6 mm x 3.5 μm Alliance, e2695 Luna Phenyl Hexyl column. Drug and IS, both of which display proton adducts approximately m/z 146.3685 to 120.0638 and m/z 143.7695 to 76.7964, might be detected simultaneously using MRM-positive modalities. Over a linearity level of 2.00 to 40.00 ng/mL, the method had a correlation value (r2) of 0.99977. The accuracy and precision of this method during the day ranged from 89.85 to 102.89% and 0.19 to 2.81%, respectively. Tremelimumab was reported to remain stable during three freeze-thaw cycles, benchtop tests, and postoperative stability studies. Cmax and Tmax values were acquired directly from experimental data. Cmax and Tmax averaged 18.024 ng/mL and 6 hours, respectively. At t1/2 of 18 hours, plasma levels began to fall. The obtained AUC024 and AUC0 values were 257 and 257 ng h/mL, respectively.
21. Characterization and Evaluation of Anti-inflammatory Melinjo Seed Extract Nanoparticles
Iwan Setiawan, Dwi Saryanti, Hazrina, Miftakhul Sholikhah
Abstract
Melinjo seed extract is rich in various active compounds, including trans-resveratrol, commonly known as “melinjo resveratrol,” with antioxidant and antimicrobial pharmacological functions. However, a comprehensive exploration of the anti-inflammatory potential of melinjo seed extract has not been conducted. Converting melinjo seed extract into nanoparticles offers distinct advantages, including the ability to permeate intercellular spaces and higher cell walls through diffusion or opsonification. This flexibility allows for synergies with various technologies, presenting extensive potential for diverse applications and targets. Therefore, this experimental research aimed to obtain an extract from melinjo seed through an extraction process and apply it in nanoparticle dosage forms. Characterization was performed by evaluating the particle size, zeta potential, surface morphology, and anti-inflammatory activity. The results showed that the nanoparticles were successfully prepared using the ionic gelation method, yielding a particle size of 267.5 nm, a stable potential zeta, and well-defined spherical morphology. Additionally, the nanoparticles produced the highest anti-inflammatory activity compared to treatments with conventional melinjo seed extract and sodium diclofenac.
22. A Novel Process for Improving the Drug Loading of Highly Water-Soluble High-Dose Drug in FDM 3D Printed Tablets
Adarsh Malgave, Rajkumar Malayandi, Anumol Joseph, Sideequl Akbar, Vinod Gaikwad, Subramanian Natesan, Ravichandiran V
Abstract
Background: 3D printing technologies, also known as additive manufacturing technologies, are gaining importance in pharmaceutical research and manufacturing. These technologies are widely used in automobile, plastic, and material fabrication industries. In the recent past, pharmaceutical industries are actively working to increase the applicability of these technologies in commercial manufacturing. On the other hand, clinics and hospitals are ready to adopt these technologies due to their versatility such as flexibility, individual customization, and low-cost investment. FDM 3D printing technology is one of the widely used technologies for the manufacturing of finished products. However, this technology has limitations such as drug loading, scale-up issues, and regulatory requirements. The present study focused on developing a suitable solvent system along with a drug-loading method to increase the industrial applicability of this technology.
Methods: Metformin, a high-dose, highly soluble drug, was selected as a model. Solvents such as water, ethanol, and methanol and their combinations were explored. Saturation solubility and drug loading in both PVA filaments and printed tablets were tested for drug loading. The solvent ratio of ethanol/methanol/water (8:1:1) was selected. The different infills of 10, 25, 50, 75, and 100% were printed using PVA filaments and were subjected to drug loading using soaking and solvent curing methods.
Results: The soaking method has resulted in poor drug loading as well as layer separation and swelling of the polymer. The solvent curing method has a maximum drug loading of 91.9% w/w without physical deformities of the tablets. Moreover, the solvent curing method is a scalable process with less process time, and hence this method could be useful for both large-scale commercial manufacturing as well as customized formulations for personalized therapies.
Conclusion: This method could be used for manufacturing thermoliable drug products and moderate-dose drug substances. Based on the research outcomes, we propose a novel, scalable, and rapid solvent-curing method for drug loading in the FDM 3D printing technique.
23. Design Formulation Ointment and Wound Healing Effectiveness of Onchidiid Slug (
Onchidium typhae) Extract Ethanolic Assisted by Design Expert Software
Bambang Wijianto, Liza Pratiwi
Abstract
Research on onchidiid slugs has been conducted regarding their antibacterial activity and wound healing abilities. Objective: This study aims to design the ointment formula as an effective drug delivery base for wound healing. The formula design was obtained using the mixture design method using Design Expert software version 13.0. The proposed and optimum formulas were then evaluated for their physical properties (organoleptic, homogeneity, spreadability, adhesion, and pH). The incision wound was made with a wound length of 1.5 cm with a depth of 0.2 cm on the mouse’s back. The assay group was divided into several groups. Group I is the positive control treated with betadine ointment. Group II is the negative control treated with an ointment base without active extract. Group III is the group given crude extract. Groups IV, V, and VI are the treatment groups’ optimum formula of onchidiid slug ethanol extract ointment: 1, 3, and 5%, respectively. The intervention for each group was carried out for ten days with smearing once a day. The design results in optimal formulas with the composition of adeps lanae and vaseline album (9,566:70, 344) with a desirability value of 0.934. Tests for adhesion power, spreadability, and optimum formula pH meet the requirements for a good ointment. An ointment containing 1% onchidiid slug extract showed the best wound-healing effectiveness. This formula is 88.31% effective in wound healing. Onchidiid slug ethanol extract can be designed into an effective ointment for wound healing assisted by the mixture design method using Design Expert software.
24. Study of Total Phenols, Flavonoids, Antioxidant and Antibacterial Activities from
Dioscorea hispida Tubers
Masfria1, Syahputra H, Samosir VC, Manalu E
Abstract
The tubers of
Dioscorea hispida Dennst., a Dioscoreaceae plant, contain flavonoid molecules and plant secondary metabolites that are antioxidants and antibacterials. In this study, the total phenolic content and flavonoids from the ethanol extract and fraction (n-hexane and ethyl acetate) of
Dioscorea tuber were investigated for their antioxidant and antibacterial properties. Fractionation with n-hexane and ethyl acetate followed by diffusion with 96% ethanol. The Folin-Ciocalteau reagent measured total phenol at 765 nm, and the AlCl3 method measured total flavonoid at 440 nm using a visible spectrophotometer. The DPPH assessed the antioxidant activity, whereas the antibacterial activity against
Staphylococcus aureus and
Escherichia coli was determined using agar diffusion on paper discs. The extract, n-hexane fraction, and ethyl acetate exhibited total phenolic content of 33.02, 5.95, and 156.33 mg GAE/g extract, respectively. Similarly, the total flavonoid content was measured at 20.26, 14.31, and 74.02 mg QE/g extract. The extract, n-hexane fraction, and ethyl acetate of the
Dioscorea tuber exhibited minimum inhibitory concentrations (MICs) of 8.25, 7.76, and 10.30 mg/mL against
S. aureus and 8.51, 8.31, and 12.05, against
E. coli, respectively. The findings of this study indicate that the ethanol extract and n-hexane fraction derived from
Dioscorea tubers exhibited comparatively diminished antioxidant and antibacterial properties in comparison to the ethyl acetate fraction. Furthermore, the ethyl acetate fraction exhibited elevated concentrations of total phenols and total flavonoids in comparison to the remaining fractions.
25. Development and Assessment of a Nutritional Supplement Formulation for Diabetes Mellitus
Ajay G Pise, Harshita Ghuse, Sanskruti Zade, Gayatri H Tiwaskar
Abstract
Diabetes, a major global health issue, affects 424.9 million people worldwide, with a significant portion undiagnosed, leading to severe health and economic impacts. Effective management of diabetes includes dietary interventions, among which nutraceuticals play a crucial role. Nutraceuticals are food-derived compounds that offer health benefits, including disease prevention and treatment. This study focuses on the development of an antidiabetic nutraceutical instant soup powder formulated with ingredients like fenugreek seed, finger millet, tomato, curry leaves, garlic, black pepper, black salt, stevia, and oyster mushrooms.
The raw materials were sourced from local markets and processed to create a fine powder mix. The soup powder’s physicochemical parameters, including pH, viscosity, moisture content, and ash levels, were measured. Nutritional analysis, sensory evaluation, and heavy metal content determination were conducted following standard protocols. The soup powder exhibited significant antimicrobial, antioxidant, and antidiabetic properties, demonstrating potential as a dietary supplement for diabetes management. The sensory evaluation indicated high acceptability among the panelists, highlighting the product’s feasibility for consumer use.
26. Effect of Inhaler Technique Health Education in Improving Symptoms and Lung Function in COPD Outpatient in a Private Hospital in Gresik, Indonesia: Pilot Studies
Amelia Lorensia, Soedarsono, Rivan Virlando Suryadinata, Havida Ainin Badri
Abstract
Inhalers are the most effective therapy in the treatment of Chronic obstructive pulmonary disease (COPD). Research shows that a large number of COPD patients do not use inhalers properly. Incorrect inhaler use technique can reduce drug delivery and poor disease control. Education on how to use inhalers is an important part of COPD management. The study was conducted to determine the effect of education on symptom assessment, lung function assessment and inhaler use skill assessment in COPD patients. The research was in the form of a pre-experimental one-group pre-test post-test. The results showed that there was a significant difference in the effect of education on how to use the inhaler on the assessment of symptoms (
p = 0.000), a significant difference in the assessment of lung function (
p = 0.001) and a significant difference in the assessment of skills in using the inhaler (
p = 0.000). Education on how to use inhalers has an influence on the assessment of symptoms, lung function and skills in using inhalers in COPD patients.
27. Ibuprofen Release from Poly(L-Lactic Acid)/Cellulose Blend Tablets: Box-Behnken Design for Optimization of the Influenced Parameters
Azouz L, Sadoun-Daikha O, Rezgui F
Abstract
According to the literature, blending PLA with cellulose, a natural polymer, can improve their use in the field of drug delivery systems. This work aimed to prepare a ternary mixture of ibuprofen, poly(L-lactic acid) (PLLA), and cellulose by the physical mixing method and to determine the effect of three selected factors (PLLA/cellulose blend ratio, percentage of the blend, and time of contact) on the amount of IBF released as a function of time. A Box-Behnken experimental design created using Minitab 17 software was used to study and optimize the selected factors. The percentage of IBF released significantly decreased with increasing PLLA/cellulose blend ratio (X1) and percentage of blend (X2). No significant interactions between the three factors were observed for Y1 (30 minutes), Y2 (60 minutes), and Y3 (120 minutes). A significant interaction between the PLLA/ cellulose ratio and the percentage of the blend was observed only for Y4 (180 minutes). ANOVA revealed that the refined mathematical model equations for Y1, Y3, and Y4 were more adequate than Y2 to explain the investigated total variations.
28. Formulation and Characterization of Gabapentin-Loaded Bigel For Transpinal Delivery to Brain
Basavesh, Manjula D, Premakumari KB, Josephine Leno Jenita
Abstract
In this research, the focus was on the design and evaluation of novel two-phase systems known as bigels (BGs) for the transpinal (TS) drug delivery of gabapentin. BGs combine the advantages of hydrogels and organogels while mitigating the drawbacks of individual gels. The formulation involved preparing hydrogels and organogels using carbopol 940 in varying concentrations, which were later combined in a 1:1 ratio to produce BGs. The Fourier-transform infrared spectroscopy (FTIR) analysis indicated the interaction between the drug and polymer was nil. The formulated BG formulations underwent comprehensive characterization, including assessments of physical appearance, pH, viscosity, swelling index, spreadability, drug content,
in-vitro release,
ex-vivo permeation, skin irritation, and antiepileptic activity. Formulation B5 emerged as the optimized formulation based on various evaluation parameters. Skin irritation studies demonstrated compatibility with the skin, showing no adverse reactions. In antiepileptic activity, rats receiving gabapentin BG
via the TS route exhibited a significant reduction in convulsion duration compared to control groups that received BG without the drug or free drug solution orally. Conclusively, the study suggests that the developed BGs containing gabapentin, when applied through the TS route on the back of the neck, hold promise for reaching the brain effectively. This method presents a potential avenue for enhanced drug delivery in the control of epilepsy.
29. Lornoxicam Solid Lipid Nanoparticle-Enriched Transdermal Gel: Development and Characterization
Vaibhav Dagaji Aher, Rajesh V, Renukaradhya Chitti, Boi Basanta Kumar Reddy
Abstract
To develop antiinflammation and analgesic effects, scientists introduced lornoxicam (LRX) nanoemulsion, nanostructure lipid carriers, and solid lipid nanoparticles. After six months of testing at different temperatures, SLN, NLC, and NE were determined to be stable. The most prominent mechanism that was identified in case I was the diffusional release of drugs from nanoparticles and nanoemulsion, which is consistent with Fickian drug diffusion. After NE, NLC, and SLN, a gel formulation achieved the greatest rate of drug penetration
via rat skin. When contrasted with the gel, nanoformulations considerably enhanced the drug’s penetration into the skin of rats. Therefore, SLN, NLC, and NE of LRX could be recommended for the relief of skin disorders characterized by inflammation and pain.
30. Design and Development of Simvastatin Loaded Liposomes Sujit Desai, Arehalli Manjappa, Preeti Khulbe
Abstract
Liposomes containing simvastatin were the focus of recent research. A process called thin film hydration was used to create simvastatin (SVN) liposomes. Method optimization was accomplished with the help of the BBD model. Drug content, vesicle size, surface shape, and
in-vitro drug release were evaluated in the generated liposomes. There was no liposome that did not meet the criteria for appropriate drug content and mean vesicle size. Liposomes that did not combine and had a spherical or nearly spherical shape were seen in the surface morphology. The produced liposomes have demonstrated significant drug release. Liposomes loaded with SVN were successfully manufactured and tested.
31. Optimization of Slugging and Compression Process for Bicalutamide Tablets
Santanu Roy, Naresh Kalra, Gurpreet Singh
Abstract
The critical nature of pharmaceutical dosage forms necessitates the optimization of manufacturing process variables to achieve the desired product quality. In this study, slugging (Dry granulation) was selected as an appropriate granulation method to mitigate poor flow properties in the final bicalutamide blend. The chosen process variables include slug hardness, mill screen size, and mill speed. A 23-factorial design was employed to investigate these variables. Process parameters were reproducible, with minimal impact on tablet properties, even when roller speeds varied. Response surface models effectively examine the relationship between response variables and quantitative parameters. The input and process variables for the compression process were predetermined based on the desired quality attributes of bicalutamide tablets. Notably, the
p-value for the slugging process was not more than 0.05, indicating their insignificance in tablet content uniformity. Product quality attributes affected by the compression process step include content uniformity, disintegration time, and dissolution. The optimal hardness range was found to be 2.0 to 7.0 kp.
32. Formulation Optimization and Preparation of Amlodipine and Telmisartan Double-layer Tablets (5/40Mg) using Wet Granulation Method
Duyen Thi My Huynh, Huynh Thien Hai, Tran Huu Loc, Minh-Ngoc T Le, Phuoc-Vinh Nguyen
Abstract
The two-layer tablet of amlodipine and telmisartan is an effective strategy to manage hypertension disease through a combination of various treatment mechanisms. However, the spray-drying method is currently used to prepare telmisartan tablets due to its extremely low solubility, which requires sophisticated equipment. In this study, wet granulation was applied to fabricate this two-layer tablet. Furthermore, design of experiments were deployed to design and optimize the formulation in order to obtain an
in-vitro equivalence with the reference drug. As a result, a formulation of the two-layer table using the wet granulation method was successfully developed and optimized. The obtained tablet showed an
in-vitro equivalence with the reference drug (with f2 superior to 50 for both amlodipine and telmisartan). Furthermore, the obtained tablet also met a set of in-house standards, including appearance, identification, assay, and dissolution rate. This study provided not a novel but effective and simple method of fabrication for amlodipine-telmisartan tablets using wet granulation. Furthermore, the obtained results also highlighted the significant contribution of a well-established design of experiments in the development of a complex tablet formulation.
33. Pharmacological Evaluation of Ayurvedic
Nicotiana tobacum Formulation for Accelerated Wound-healing: An Experimental Study
Aarti Shastri, Arti Swami, Sachin Bhusari, Satish Polshettiwar
Abstract
Background: The need for pharmacognostic-based compounds with various medicinal actions is increasing to address issues such as drug resistance, new diseases, and the toxicity of already utilized chemical compounds. The plant kingdom provides numerous bioactive molecules that have great promise to help solve these challenges, resulting in the rise of innovative solutions in the pharmaceutical sector. Ayurvedic preparations, including tobacco (
Nicotiana tabacum) are considered a viable method due to their long history in herbal therapy and several medical advantages.
Methods: The study aims to investigate the wound-healing properties of the tobacco plant. Tobacco leaves were utilized in the production of a traditional ayurveda formulation, which included mashi formulations such as anterdhum padhati mashi, bahirdhum padhati mashi, and muffle furnace mashi, in accordance with traditional ayurvedic methods. Aqueous and alcoholic extracts of tobacco leaves were also produced. The effectiveness of these formulations in wound-healing was evaluated using an Excision model in mice.
Results: The bahirdhum padhati mashi with methanolic discharge showed significantly greater wound-healing capacity compared to a standard medication formulation, as indicated by comparative study.
Conclusion: Ultimately, the bahirdhum padhati mashi made from tobacco shows potential for healing wounds and could be a useful agent for wound-healing. The results of this experimental study suggest that ayurvedic formulations could be effective in treating wound-healing difficulties. Additional research and clinical studies are needed to confirm the safety, effectiveness, and possible use in wound treatment.
34. Investigating Bael Fruit Gum Powder as Natural Polymer for Pharmaceutical Drug Delivery
Dipak P Mali, Dhanashri R Patil, Ravina D Sutar, Dinanath T Gaikwad
Abstract
Nowadays, the use of natural products is crucial in pharmaceuticals. Currently, natural products made with natural polymer offer various biomedical applications. The objective of the present research was to characterize the bael fruit gum (
Aegle marmelos L.) as a natural polymer and investigate its potential in pharmaceutical drug delivery. Extraction of bael fruit gum was carried out by simple maceration technique. Further, the extract was subjected to different phytochemical analysis. The characterization part was studied with sophisticated techniques such as fourier-transform infrared (FTIR) and X-ray diffraction (XRD). Additionally, swelling and viscosity behavior were estimated as per the reported methods. Phytochemical analysis confirms the existence of major secondary metabolites like tannins, flavonoids, saponins, alkaloids, and triterpenoids. FTIR results showed identical peaks of phytochemicals, which confirmed the presence of identical functional groups. XRD study indicates that extract nature is amorphous. The swelling behavior and viscosity study resulted in the rheological performance at an optimum and desired level. In conclusion, this research indicates the potential of bael fruit gum as a natural polymer for pharmaceutical applications, contributing to the discovery of new natural products and promoting their industrial use.
35. Effect of Magnesium Stearate and Fines on Delivery of Dry Powder for Inhalation using Sucrose as a Carrier
Ganesh Jadhav, Milind Wagh, Nazma Inamdar
Abstract
Typically, lactose is utilised as carrier in Dry Powder Inhaler commercially. However, with the widening scope of DPI in therapeutic categories other than COPD and asthma, a need for the alternate carrier is arising. In this study, we used sucrose, a non-reducing sugar, as an alternate carrier. Effect of addition of fines and magnesium stearate was studied on powder flow properties and aerosolization performance. The air jet milling technique was used to generate sucrose fines. DSC and XRD studies showed no change in sucrose polymorph upon micronization. Levosalbutamol sulphate was used as a model drug, powder blends were prepared by low shear tumbling type blender. Powder formulations were studied for PSD, blend homogeneity, and flow properties. The percentage of particles smaller than 5 microns rose when fines were added as indicated by PSD data. SEM study revealed that the added fines get adsorbs on the coarse carrier, thus minimizing the adhesive interactions between drug and coarse carrier.
In-vitro deposition was studied using low and high resistance devices on glass Twin Stage Impinger (TSI). Addition of fines and the magnesium stearate improves aerosolization performance showing higher Fine Particle Fraction (FPF) by almost 2 folds than the formulation containing coarse carrier alone.
36. Development of a Bioanalytical Assay for the Selective RET Inhibitor Pralsetinib in Plasma Samples Utilizing Liquid Chromatography-Tandem Mass Spectrometry
Vijetha Pendyala, Susmitha Priyadarsini Addanki, Vidyadhara Suryadevara
Abstract
Pralsetinib is a potent and specific tyrosine kinase inhibitor targeting the RET receptor, used in treating various cancers. This study developed and validated a bioanalytical assay for pralsetinib in plasma using liquid chromatography-tandem mass spectrometry (LC-MS/MS). The internal standard was erlotinib, and protein precipitation with acetonitrile was used for sample preparation. The analytes were separated on an Ultimate® XB-C18 column using gradient elution with ammonium acetate in water and methanol. Both are acidified with 0.1% formic acid. Detection was performed using positive electrospray ionization in the chosen reaction monitoring mode. The assay was validated over a linear range of 2 to 2000 ng/mL, achieving accuracies greater than 90% and precision values below 2%. The method was stable under all tested conditions without significant matrix effects or extraction losses.
37. Development and Evaluation of Polyherbal Phyto-phospholipid Complexes (Phytosomes) for PCOD Treatment
S Prema, Firoj A Tamboli, Bhupinder Bhyan, Hanish Singh Jayasingh Chellammal
Abstract
Polycystic ovary disorder (PCOD) is a common endocrine condition affecting women of reproductive age that is distinguished by hyperandrogenism, ovulatory failure, and polycystic ovaries. It is still not entirely apparent what causes polycystic ovary syndrome (PCOS), and the treatments that are currently available tend to focus more on alleviating symptoms than on addressing the underlying causes. The bioavailability and effectiveness of bioactive chemicals can be improved by the use of phytosomes, which are sophisticated delivery methods. Phytosomes for the treatment of polycystic ovary syndrome (PCOS) are the primary focus of this study. Materials such as milk thistle (
Silybum marianum), curcumin (
Curcuma longa), and
Ginkgo biloba were utilized with the purpose of highlighting the potential benefits of these substances in the treatment of PCOD. A fourier-transform infrared (FTIR) analysis was carried out, and the results of the
ex-vivo analysis confirmed that the formulation PS3 with a ratio of 2:1 exhibited a greater release profile.
38. Development and Validation of Analytical Method for Estimation of Sildenafil Citrate in Swab Samples
Dushyant Gaikwad, Gayatri Dhobale, Rushikesh Kakade, Harshal Tare
Abstract
Among the most significant issues with pharmaceutical production in shared facilities is the risk of cross-contamination, which lowers product quality and costs the business a lot of money. This work set out to evaluate a cleaning approach by creating and testing a straightforward UV spectrophotometric method for estimating sildenafil citrate in swab samples. To get a good recovery from a stainless steel surface utilising a sterile cotton swab stick, the swabbing technique was fine-tuned. A wavelength of 292.20 nm was chosen for detection. Linearity, precision, accuracy, detection limit, and quantification limit were the criteria used to validate the suggested approach. A correlation coefficient of 0.9993 was determined for the regression line after studying linearity throughout a concentration range of 5 to 25 μg/mL. An average of 88.23% was recovered.
39. Formulation and Evaluation of Tablets Using the Solvent Evaporation Method to Increase the Solubility of Lansoprazole
Shankar Dhobale, Suresh Jadhav, Mayur Hase, Harshal Tare
Abstract
The inability to determine sufficient and repeatable bioavailability and/or desirable pharmacokinetic features in humans is one of the biggest obstacles to the oral administration of new medicines. The solubility and absorption of a medicine determine its bioavailability, which in turn determines its therapeutic efficacy. Achieving the target drug concentration in the systemic circulation and ensuring drug biological activity in humans are both affected by solubility. A stomach ulcer has the potential to rip through the stomach lining, the initial section of the small intestine, and possibly even the lower esophagus. Distinct ulcers form in different parts of the intestines; one forms in the duodenum and one in the stomach. Duodenal ulcers are most commonly characterized by upper abdominal pain at night that subsides after eating.
Eating might exacerbate the discomfort from a stomach ulcer. Preparing and assessing the pills will yield optimal outcomes. The active component content is 99.90%, as is the active ingredient release rate. Compared to other formulations, solid dispersion tablets performed better in in-vitro tests (98.85%). The optimized formulation (lansoprazole solid dispersion tablets) outperformed the labeled formulation (conventional lansoprazole tablet) in terms of drug-releasing capacity within 6 hours, outperforming both formulations.
40. Formulation and Evaluation of Immediate Release Tablets of Antimalarial Drug Hydroxychloroquine
Dushyant Gaikwad, Priyanka Dhainje, Sachin Kadam, Harshal Tare
Abstract
The goal of the study was to develop and evaluate an immediate-release antimalarial tablet formulation for the effective management of malaria, an antimalarial drug as an active pharmaceutical ingredient using excipients. Appropriate pharmaceutical products and evaluate their properties in relation to the innovative product. The study was to develop an antimalarial formulation with
in-vitro solubility properties equivalent to or better than the improved formulation. Therefore, an orally administered immediate-release tablet with a robust and reproducible formulation technique was developed. According to the study, the number of F3 definitions decreased the most and F8 had the most important medicinal properties. At 20 minutes, F4 appeared to lead the first high decay rate (98. 56%), followed closely by F5 (93.48%). The expansion of F1, F2 and F3 shows high decay rates at this time. Based on this information, one can analyze and compare the decay profiles of unmistakable definitions. Things such as composition, excipients used, and manufacturing geometry can influence degradation behavior, and this information may be necessary to optimize concentrations of substances of interest for drug delivery. It is then concluded that the definition number F5 may be an optimized detail.
41. Stability Indicating Force Degradation Study of Nintedanib in Bulk and Pharmaceutical Dosage Form
Sachin Kadam, Rohit Bhalerao, Sonali Pawar, Harshal Tare
Abstract
Assay of the nintedanib drug substance can be determined using a newly designed and verified reverse-phase high-performance liquid chromatography (RP-HPLC) method, even when degradation products from forced degradation experiments are present. By using gradient elution, the mobile phase was a mixture of 70% acetonitrile and 30% water by volume. Acid, base, peroxide, thermal, and photolytic degradation were among the stress conditions that the product was subjected to. During the thermal and photolytic breakdown processes, no extra contaminants were detected. Using validation criteria such as specificity, linearity, limit of quantitation (LoQ), accuracy, precision, robustness, and ruggedness, the developed technique was validated in accordance with International Council for Harmonization (ICH) recommendations. At a concentration of 12.4 ng/mL, the LoQ value was attained. The results showed good linearity (r2 > 1.00) across doses ranging from 2 to 10 μg/mL. Verification of recovery was done by adding concentrated solutions of 5, 10, and 15 μg/mL. So, newly developed RP-HPLC technology can separate Nintedanib from its main degradation products, and it can also estimate the drug substance’s concentration.
42. Development of Enteric-Coated Tablet with a Unique Combination of Therapeutic and Nutraceutical Actives to Treat Colitis
Manish Kumar Gupta, Ketaki Dhane, Chandraprabhu Jangme, Abhinandan Patil
Abstract
The primary objectives of the current investigation were to design and characterize enteric-coated oil of ginger tablets in coconut water powdered form as a therapy for ulcerative colitis. One source that is both anti-inflammatory and high in electrolytes is a combination of ginger oil and powdered coconut water. By reducing inflammation and improving electrolyte and water balance, this combination will hasten the healing process. Starch 1500, microcrystalline cellulose, and ethyl cellulose were used to create enteric-coated tablets of ginger oil alone and in combination with coconut water powder. The results corroborated the findings that there were no unique interactions between any of the substances, as demonstrated by the examination of both tablets, which included morphology, micrometric features, and fourier transform infrared (FTIR) spectroscopic capabilities. We studied the dissolving characteristics of coated tablets at pH 1.2, 6.8, and 7.4 in a buffer. Quantification of gingerol was accomplished by use of reverse-phase high-performance liquid chromatography (RP-HPLC) technology. The selected formulation’s therapeutic efficacy was lastly confirmed using a colitis model generated by 2,4,6-trinitrobenzene sulfonic acid. Tablets containing either ginger oil or a powdered combination of ginger oil as well as coconut water were compared in the research. Myeloperoxidase, lipid peroxidase, and histological assessment were calculated using the colitis model. The colon/body weight ratio was also measured. Research on animals has shown that a combination of the coated oil of ginger and the oil of coconut tablets, as opposed to ginger oil tablets alone, considerably improved the sick conditions in Wistar rats. The gain in weight and clinical improvements in the macroscopic and microscopic factors of induced colitis served as evidence of this. These results demonstrate the potential of coated tablets formulated with coconut water powder for the targeted delivery of ginger oil to the colon as well as for the improvement of colon health through the balance of micronutrients and water content. It is not practical to increase the dosage to compensate for metabolic loss while using ginger oil because of its strong taste and strength. Therefore, the formulation of choice is enteric coating. As enteric coating tablets target the intestine as the site of action, it is possible to use less potent ginger oil. Due to the inclusion of coconut water powder, the formulation not only helps cure the illness state but also promotes and supports a speedy recovery.
43. Antifungal Niosomal Nail Lacquer for Enhanced Transungual Delivery of Efinaconazole in the Treatment of Onychomycosis
V Chatur, S Dhole, N Kulkarni
Abstract
Niosomes, multilamellar vesicles, efficiently transfer active substances into the epidermis or systemic circulation. Topical medication delivery techniques increase skin permeability to active compounds. Onychomycosis, a common nail ailment caused by fungus, requires efficient topical therapies due to the risks of systemic antifungal therapy. This research aimed to make a nail polish with efinaconazole (EFN) to treat onychomycosis. The spherical Niosomes contained efinaconazole and had a 100 to 130 nm diameter. In the 24-hour
in-vitro experiment, drug trapping ranged from 40 to 90% and release from 25 to 86%. The 1:2 mixtures of efinaconazole niosomes, Span 60, and CHO produced nail paint with good results. Efinaconazole-loaded niosomal nail polish had better drug release, antifungal effectiveness, and smoothness over other formulations. Topical nail polish can help low-bioavailability medicines. This method helps the medication enter the body through the nail. The ENNL can deliver onychomycosis drugs topically.
44. Bioanalytical Method Development and Validation for Determination of Nirmatrelvir in Human Plasma using LC-MS/MS
Nameera Jabeen, M Akiful Haque
Abstract
The term “antivirals” has been associated with COVID-19 during the period when the usage of this specific class of medications has increased. Nirmatrelvir, a protease inhibitor, is used to treat mild to moderate COVID-19 symptoms by stopping SARS-COV-2 reproduction. With deucravacitinib serving as the internal standard, liquid chromatography-tandem mass spectroscopy in human plasma was used to provide a quick, simple, innovative, trustworthy, and sensitive approach. Liquid-liquid extraction was used to separate nirmatrelvir and the internal standard. The extracted sample was then run through a chromatographic system with ACE-C18 column (4.6 × 100 mm, 5 μm); and mobile phase with methanol and 2 mM ammonium formate in a ratio of 80:20, and a flow rate of 1.00 mL/min. The system operates for three minutes in multiple reaction monitoring mode at the ABSCIEX API 4000 mass spectrometer using electron spray ionization. Nirmatrelvir ion transitions are 500.10 to 110.10, while deucravacitinib are 426.30 to 358.20. The validation was conducted using a concentration range of 5.00 to 4000 ng/mL, and the results showed that the selectivity, accuracy, precision, linearity, and selectivity were all within the acceptability limits.
45. Formulation Development and Evaluation of Ticagrelor Oral Dispersible Tablets by Using Co-processed Superdisintegrants
Gayatri Dhobale, Soham Chavan, Shankar Dhobale, Harshal Tare
Abstract
Ticagrelor is a contemporary anti-platelet drug that inhibits the aggregation of platelets by blocking the adenosine phosphate (ADP) receptors of the subtype P2Y12; generally utilized in patients who have a previous history of myocardial infarction or with acute coronary syndrome to prevent occurring of myocardial infarction, cardiovascular death and stroke in future. This study focuses on the development of formulation development & assessment of an oral dispersible tablet of ticagrelor, a Biopharmaceutical Classification System (BCS) class 4 drug, by using the co-processed superdisintegrants to enhance drug dissolution and bioavailability. Wet granules with different concentrations of co-processed superdisintegrants developed the tablets. This study includes seven formulations that were formulated using the different selected excipients. The various batches were assessed for physical characteristics, disintegration, dissolution studies, hardness and friability.
In-vitro dissolution investigations were conducted for formulations. S1 to S7 at time points 5, 15 and 30 minutes. According to the results of the formulation S7 was discovered to be the optimum formulation, as shown 102.89% drug release at 5 minutes and a disintegration time of 16 seconds. Thus, it appears that S7 is the most suitable formulation of ticagrelor oral dispersible tablet in order for enhanced bioavailability.
46. The Development of an Innovative Ophthalmic
In-situ Gel Containing Posaconazole
Kumbhar ST, Salunke MA, Mane PT, Wakure BS
Abstract
The goal of this study was to create and test various
in-situ gel formulas for administering posaconazole to the eye to treat fungal keratitis. They used an
in-situ gelling method to help posaconazole stay in the eye mucosa longer, which made it easier for the body to use. To make
in-situ gel preparations, polymers such as sodium alginate, poloxamer 407, and poloxamer 188 were used in a cold method. Finally, there was 0.2% (w/w) posaconazole in the mixtures. The pH, drug content, viscosity, gelling capacity, and temperature at which the solution turns into a gel were all checked on the recipes. It was between 32 and 34℃ when each blend turned into a gel. There was about the same amount of drugs in all of them. It was also worked out how much of the antifungal and
in-vitro drugs these mixtures would release. Everyone in the drug release study showed signs of long-lasting release. To sum up,
in-situ gels that contain posaconazole could be a good way to use optical drug delivery to change how fungus diseases act.
47. Formulation and Characterization of Isoconazole Loaded Invasomal Gel for Effective Antifungal Activity
Dhananjay Chavan, Manish Kumar
Abstract
The characterization of isoconazole invasomal gel formulations (IG1–IG5) aimed to evaluate their physical attributes, drug content, and drug release kinetics for topical application. All formulations exhibited transparency and smooth texture, indicating uniform drug dispersion. While IG1 had an easily pourable consistency, IG4 displayed very good consistency, suggesting viscosity differences. Despite these variations, all formulations showed good homogeneity and high drug content, with IG4 leading in drug content percentage. Spreadability and viscosity varied among formulations, influencing ease of application and adherence to the skin. Cumulative drug release profiles revealed sustained release over 12 hours, with notable differences in release rates and extents among formulations. IG4 exhibited the most sustained release, aligning with pharmacokinetic requirements for antifungal therapy. Its release profile followed a diffusion-controlled mechanism, with a high cumulative drug release percentage of 98.95 ± 0.32% over 12 hours. Antifungal activity against
Candida albicans was comparable to Isoconazole, suggesting IG4’s effectiveness in treating fungal infections. Stability studies confirmed the formulation’s stability under tested conditions, supporting its potential for further development and clinical use.
48. Potential of Native Cyclodextrins and L-Lysine for Enhancing Ellagic Acid Aqueous Solubility
Isaïe Nyamba, Charles B Sombie, Anna Lechanteur, Rasmané Semde, Brigitte Evrard
Abstract
This study aimed to examine the influence of β cyclodextrin (βCD) and γ cyclodextrin (γCD) alone and in combination with L-lysine on ellagic acid (EA) solubility. Indeed, complexation with cyclodextrins can be used to improving the solubility of drugs poorly soluble in water such as EA. EA is a Biopharamceutical Classification System (BCS) IV bioactive polyphenol with numerous therapeutic activities, including antimalarial activities. However, its unfavorable physicochemical properties limit its therapeutic use. Therefore, after a phase solubility study, we successfully prepared EA-βCD and γ CD binary solid complexes using the freeze-drying technique. Methods including proton nuclear magnetic resonance (1H-NMR) analysis and fourier-transform infrared (FTIR) spectroscopy were used to characterize the inclusion behaviors of the complexes of EA with cyclodextrins both in solution and solid forms. The results of the phase solubility study indicated Ap-type diagrams of EA with the two cyclodextrins (CDs). The solubility of EA was multiplied by 9.92 and 2.98 in the presence of γCD and βCD respectively. Moreover, the complexes characterization by FTIR spectroscopy revealed the involvement of the C=O and EA OH groups in the interaction with the CDs. The results of NMR spectroscopic characterization revealed that the formation of EA inclusion complexes with βCD was partial. However, these results did not indicate the appearance of EA inclusion complexes with γCD. These relatively modest results in terms of increased EA solubility, obtained with cyclodextrins, prompted us to use a third compound, l-lysine, to enhance CDs complexation. Thus, the formation of ternary complexes led to a very significant increase EA solubility. Indeed, the incorporation of EA into EA-L-lysine-βCD and γ CD complexes increased its water solubility at pH 7.4 by a factor of 555 and 663, respectively.
49.
In-vivo Toxicity Profile of 2-Butyl-3-(3, 5-Diiodo-4-Hydroxybenzoyl) Benzofuran on Different Experimental Models
Sowjanya Akula, Gubbiya Shiva Kumar
Abstract
The anti-cancer properties of 2-butyl-3-(3, 5-Diiodo-4-Hydroxybenzoyl) benzofuran have been determined in earlier
in-vitro studies, but safety and efficacy still need to be resolved. This research investigates the acute oral toxicity of 2-butyl-3-(3, 5-diiodo-4-hydroxybenzoyl) benzofuran on female Wistar rats, zebrafish, and brine shrimp. The present study was conducted on rats to evaluate the compound acute oral toxicity, following the protocols established by the Organization for Economic Cooperation and Development (OECD) 423. After 14 days of duration, histopathological changes were observed in the liver and heart of animals that received a dosage of 2,000 mg/kg. The compound was tested at a limit test concentration of 100 mg/L in zebrafish for period of 96 hours. During this time, sub-lethal clinical signs and mortalities were observed at 24, 48, 72, and 96 hours. Brine shrimps were exposed to various concentrations for 24 hours to evaluate their cytotoxicity and calculate the percentage of mortality. Histopathological changes are primarily observed in the liver (multifocal necrosis of hepatocytes), heart (myocardial inflammation) and lung (low alveolar/interstitial inflammation). There are no recordings of mortalities at 300 and 2,000 mg/kg treated rats. Behavioral patterns remained unchanged, whereas food intake and body weight decreased significantly. The oral administration of the test chemical to rats would result in an LD50 greater than 2,000 mg/kg, ranking it in the fifth category of the GHS. The LC50 (322.96 μg/mL) for the brine shrimp lethality assay was calculated using a plotted graph. The test compound’s LC50 value in the zebrafish model would be higher than 100 mg/L. The acute toxicity profile of 2-butyl-3-(3, 5-diiodo-4-hydroxybenzoyl) benzofuran has been demonstrated using rodents, zebrafish, and brine shrimp lethality assay. This study will guide subsequent chronic toxicological assessments.
50. Biosynthesis of Platinum Nanoparticles PlNPs by Bacterial Strain
Rhodococcus erythropolis
Prabir Kumar Pal, Naveen Kumar Choudhary
Abstract
The biosynthesis of platinum nanoparticles (PlNPs) using the bacterial strain
Rhodococcus erythropolis offers a greener alternative to conventional chemical and physical synthesis methods. This study explores the potential of
R. erythropolis to produce PlNPs by leveraging its biological machinery to reduce platinum ions and stabilize the resulting nanoparticles. The biosynthesis was conducted under varying conditions of pH, temperature, and sodium platinite concentrations to optimize yield and particle characteristics. The nanoparticles were characterized. The outcome reflects that PlNPs exhibit distinct size-dependent optical properties and crystallinity, with extracellular proteins from
R. erythropolis playing a crucial role in nanoparticle stabilization. The optimized biosynthesis process produced PlNPs with high colloidal stability and significant potential for applications in catalysis and environmental remediation. This study advances the understanding of microbial nanoparticle production, highlighting a sustainable pathway for the synthesis of biocompatible and catalytically active platinum nanoparticles.
51. Formulation and Evaluation of Brucine Sulphate Transdermal Patch for Anti-Inflammatory Activity
Gayatri Dhobale, Shankar Dhobale, Rupali Hande, Harshal Tare
Abstract
This study was designed to develop and evaluate a transdermal patch containing brucine sulphate, a herb-based ingredient. Because of its potential to treat a wide range of illnesses with fewer side effects and higher efficacy, herbal medicines are gaining popularity in today’s society. Researchers in the field of phytoformulation have shown that there are a lot of benefits to enhancing the pharmacological activity of herbal drugs by creating nano dosage forms such as nanoparticles, nano-capsules, liposomes, nano-emulsion, and transdermal patches. Drugs can be delivered to patients in a regulated manner through transdermal drug delivery systems. It decreases systemic side effects and, in some cases, provides efficacy compared to other dose forms by enabling a consistent blood level profile. Patch preparation done by using naturally occurring polymers. Thickness, moisture content, folding endurance, and content homogeneity are some of the evaluation measures that are carried out. The transdermal patches evaluated successfully. Average weight of patch was 2.65 g, having folding endurance 94 times and pH of patch was 5.69, moisture content was 7.9%.
52. To Synthesize and Characterize Metabolite Enalapril: PKPD and Toxicity Predictions by Computational Approaches
Parag Pathade, Vinod Bairagi, Shraddha Vaishnav, Shraddha Dingare
Abstract
Enalapril is a prodrug that facilitates the transformation of angiotensin I to angiotensin II, an ingredient that brings constriction of blood vessels by action of the enzyme angiotensin-converting enzyme (ACE). Reversed-phase high-performance liquid chromatography (RP-HPLC) method is the focus of this work, which also includes its characterization, optimization, and synthesis. The objective is to correctly, precisely, and sensitively determine both enalapril and its synthesized metabolite, enalaprilat, when present as an impurity. The paper also forecasts the ADME and toxicity characteristics of ENLP by utilizing several ADME databases, including SWISS ADME and molesoft. The laboratory synthesized enalaprilat, the metabolite derived from enalapril, and characterized. The Kinetex C18 stationary phase was employed in the analytical approach. Flow rate was 1.0 mL/min, and the injection volume was 20 μL. With a wavelength of 244 nm, the run lasted for 10 minutes. The mobile phase used was an 80% acetonitrile: 20% pH 3 phosphate buffer. The HPLC technique validation, which involved the identification of the enalapril metabolite, followed the parameters outlined in ICH Q2B (R1). The analysis exhibited a range of accuracy and precision between 98.75 and 102.5% for all substances being tested. This approach is appropriate for identifying and measuring the metabolite in enalapril bulk or formulations. The method for assessing enalaprilat in biological fluids has the potential to be further refined and applied in clinical and bioequivalence research. The study furthermore presents an evaluation of toxicity utilizing computational methods such as the Swiss tool, with the objective of aiming to mitigate potential risks.
53. Characterization and
In-vitro Study of Polyethylene Glycol as Coating Material used as Drug Carriers on Coronary Stent for Treatment of Cardiac Diseases
Jayashri V Chopade, Deepak Hujare
Abstract
Background: The way coronary artery disease is treated has changed dramatically with the use of coronary angioplasty and stenting. Nowadays, acute coronary syndromes brought on by coronary artery disease are frequently treated using drug-eluting stents. A review of the literature reveals that the polymer coating’s thickness affects the stent’s safety; moreover, current computational studies suggest that larger coatings increase the risk of stent deformity. Polyethylene glycol is the preferred polymer coating material for coronary artery stents.
Objectives: Characterization of polyethylene glycol as a medication carrier coating for coronary stents used in cardiac disease therapy
Methods: Using UV-visible spectrophotometer, differential scanning calorimetry (DSC), fourier-transform infrared (FTIR), X-ray diffraction, thermogravimetric analysis, and surface morphology, polyethylene glycol was characterized.
Results: The calibration curves’ linear regression results, as revealed by the UV-visible spectrophotometer investigation, showed a significant linear association between the concentration range of 10 to 60 μg/mL for polyethylene glycol Y = 0.0354X + 0.0212 (r2 = 0.999), was found. Polyethylene glycol’s molecular miscibility, recrystallization, and phase separation were investigated using a DSC analysis. It was found that the material was physically stable because no recrystallization peaks were visible. According to the results of the thermogravimetric study, a ceramic sample cup with 4 to 6 mg of sample was heated to 400°C at a rate of 5°C every minute. Nitrogen gas was continuously supplied at a rate of 20 mL/min into the sample chamber during the analysis. The results of each batch were measured, and an average was determined. The study of surface coatings to examine the microstructure of the coatings produced both before and after the use of polymers is known as surface morphology. Within analytical imaging is the subset of surface morphology. Pure polyethylene glycol’s morphology showed broad plate-shaped structures. Additionally, a strong band is detected between 1362 and 1287 cm-1, which is comparable to the C-O stretching vibration seen in primary alcohol.
Conclusion: On base of the characterization results above shows that polymers were stable and included functional groups and structures throughout a range of conditions. It is possible to use polyethylene glycol as a coating material for coronary stents.
54. Formulation, Development and
In-vitro Characterization of Modified Release Tablets of Curcumin
Vikrant Nikam, Sachin Suryawanshi, Nikita Rathod, Shruti Kadam
Abstract
Objective: The current study set out to design and test a cost-effective system for developing modified-release tablets of curcumin in an effort to increase the duration of drug release. Because curcumin has a shorter elimination half-life, reducing the frequency of doses can increase its bioavailability.
Methods: For improved drug retardation in the stomach environment, modified-release tablets were made utilizing the wet granulation method with various grades of high-potassium chloride (HPC) as the extended-release matrix-forming agent and katira gum as the viscosity-modifying agent. Combining the use of HPC and katira gum slows the drug’s release in the stomach. The sustained-release tablets had the highest rate of medication release for up to 24 hours with almost no stomach absorption. The medication and excipients did not interact, according to the fourier-transform infrared spectroscopy (FTIR) spectra. There was no evidence of drug-excipient incompatibility, according to differential scanning calorimetry (DSC) tests. Optimal formulation batch F2 modified release tablets showed no outward signs of deterioration after three months of storage, according to stability analysis. Further evidence that F2 was steady is the lack of variation in drug content and percentage of drug release.
Conclusion: This study accomplished its stated goal of creating a modified-release tablet formulation that is both cost-effective and does not make use of coating technology.
55. Integration of UV Spectrophotometry Method For Simultaneous Estimation of Fluconazole and Efinaconazole in Nanoparticle Loaded Hydrogel
Fiza Farheen, Hemant Kumar Yadav, Abhay Raizaday
Abstract
The goal of this study was to create and validate a UV spectrophotometric method for fluconazole and efinaconazole. Ultraviolet spectroscopy was employed at 255 nm for fluconazole and 268 nm for efinaconazole, using samples prepared in a DMF and phosphate buffer solution with a pH of 4.9. The method demonstrated strong linearity with a correlation coefficient of 0.999. Following ICH guidelines, the validity of the method was assessed for various parameters, including accuracy, precision, limit of detection (LoD), limit of quantification (LoQ), recovery study, and range. The simplicity, time efficiency, and cost-effectiveness of UV spectroscopy were key factors in its selection over HPLC technique, which is known for being expensive and time-consuming with potential susceptibility to various factors affecting determination. Through repeated experiments and meticulous sampling, the method exhibited linearity, accuracy, repeatability, and lack of errors. It was also found to be selective, specific, and cost-effective, affirming its reliability. Moreover, the use of a consistent solvent throughout the experimental work ensured that the method was free from interference by any excipients. Overall, the proposed UV spectrophotometric method was deemed simple, rapid, precise, accurate, and sensitive, making it suitable for routine analysis of fluconazole in both single and combined forms.
56. Anastrozole and Paclitaxel Loaded Nanocrystals: Evaluation of Anticancer Activity
Pavan Kumar V, Narayanaswamy Harikrishnan
Abstract
To study the cytotoxic study of anastrozole and paclitaxel-loaded nanocrystals on MDA-MB-231 cell lines for enhanced anticancer activity. Paclitaxel is a tubulin-targeting cytoskeletal drug that interferes with microtubule structures, and anastrozole’s mechanism of action is apoptosis in living cells. Methylthiazol tetrazolium (MTT) assay was used to determine anticancer activity. After 24 hours of treatment, the highest ALN and PLN concentrations (100 μg/mL) showed a cytotoxic effect. The inhibition rate of doxorubicin (standard) was found at 24 hours with 89.6. The viability values of Anastrozole loaded nanocrystals (ALN) were 14.03 (100), 22.76 (80), 28.23 (40), 34.9 (20), 40.26 (10), 50.13 (5), 60.53 (2), 80.66 (1), and 99.11 (0) μg/mL. When compared to the standard, viability was 38.23% and drug unloaded nanocrystal was 86.06% (100 μg/mL) 24 hours after anastrozole (100 μg/mL) administration to MDA-MB-231 cells. All experimental groups showed significantly from the control group. The cytotoxicity effect was determined with low dose of anastrozole and paclitaxel-loaded nanocrystals. The cell viability and toxic effects of the ALN and PLN also tested. As ALN and PLN concentrations grew, so did the harmful effect on MDA-MB-231 cell viability. Cell count was significantly reduced (
p < 0.05) at high ALN and PLN concentrations (100 μg/mL). Finally, the MTT assay revealed that ALN and PLN cytotoxic to MDA- MB-231. Exposure to dose-dependently hazardous doses of ALN and PLN nanocrystal formulations resulted in increased nuclear intensity, cytochrome c, and permeability of the cell membrane in the MDA-MB-231 cell line.
57. Preparation and Characterization of Sustained Release Risperidone Loaded Eudragit Microparticles by Spray-Drying Technique
Arindam Chatterjee, Amrita Pandey, Ashutosh Sharma, Mayank Bansal, Rakesh Kumar Gupta
Abstract
The goal of this work was to create novel risperidone-containing spray-dried microparticles using Eudragit® L100, a methacrylic polymer. Microparticles were designed with controlled release and enhanced
in-vitro effects in mind and were meant to be taken orally. Spray-drying was used to create Eudragit® L100 microparticles loaded with risperidone. Risperidone-loaded Eudragit® L100 was successfully prepared to treat mental/mood disorders, according to an investigation into its physicochemical properties
in-vitro. Spray-drying was an effective method for producing Eudragit® L100 microparticles loaded with risperidone. Formulations displayed a suitable drug entrapment percentage or nearly 89.94%. The mean diameter of the nearly spherical and spherical microparticles ranged from 30 to 50 μm, and they had a smooth surface. The distinctive peak of risperidone loaded with Eudragit L100 was visible in the fourier-transformed infrared (FTIR) spectra, indicating that the medication was fully encapsulated in the polymer. The dissolution rate of risperidone-loaded microparticles was slower than that of the pure medication. The use of spray-dried risperidone microparticles as a practical oral drug delivery method for more effective and regulated risperidone release is supported experimentally by our results.
58. Development of Unique Pyrazoline Analogues for Screening Anticancer and Anti-inflammatory Studies
Susmita Basakand, Ishwar Bhat K
Abstract
Cancer is a major threat to human society in the world, which results in a maximum probability of death. In the present scenario, chemotherapy is the main cancer treatment, but still, it has its limitations. Hence, cytotoxic and chemotherapy medicines are the main focus of research for medicinal chemists. So, it is the need of the hour to explore the possibility of effective and safe anticancer drugs. The current research involves the synthesis of pyrazoline derivatives (PYR1-PYR8), which are novel cytotoxic agents developed from recently formulated chalcones (CHL1-CHL8). Title compounds were prepared by subjecting the chalcones with by hydrazine hydrate in ethanolic acetic acid. The purified synthesized compounds were characterized by IR, 1H-NMR, and mass spectroscopic evaluation. Using
in-vitro models, cytotoxicity evaluations were conducted on cell lines associated with lung cancer by MTT and SRB methods using doxorubicin as standard, which revealed differing levels of cytotoxic effects among the compounds. The egg albumin denaturation and protein denaturation methods were used to access
in-vitro anti-inflammatory activity. Compound PYR4 and PYR6 showed significant anti-inflammatory efficacy in relation to diclofenac sodium as the reference drug. Compound PYR3, PYR4, and PYR6 displayed noteworthy anticancer activity matched to doxorubicin, which is a reference drug. The current research asserts that the newly developed pyrazoline derivatives exhibit high levels of cytotoxicity and anti-inflammatory effects. However, their preclinical and clinical significance needs a thorough evaluation.
59. Investigation of the Molecular Mechanisms of
Sanguinaria canadensis in Treating Lung Cancer Using Network Pharmacology and Molecular Docking Techniques
Vaibhavkumar Jagtap, Shital Bidkar, Manoj Shinde, Jayprakash Suryawanshi
Abstract
This study examines the molecular mechanism that underlies the possible therapeutic benefits of
Sanguinaria canadensis in the treatment of lung cancer. Through network pharmacology and molecular docking techniques, we identify 15 bioactive compounds from
S. canadensis, with sanguinarine and chelerythrine being the most prominent. These compounds interact with key proteins involved in lung cancer progression, including IL-6, IL-1β, ICAM1, TNF, and MMP-9. Pathway enrichment analysis reveals significant involvement of pathways such as homologous recombination, p53 signaling, and cell cycle. GO and KEGG analyses elucidate the molecular mechanisms underlying cancer pathogenesis and highlight potential therapeutic targets. STING enrichment analysis uncovers crucial biological processes associated with STING-regulated genes, suggesting their involvement in cancer-related functions. Molecular docking studies demonstrate strong binding affinities between bioactive compounds and target proteins, indicating potential efficacy in impeding cancer-related processes. This comprehensive investigation provides insights into the therapeutic potential of
S. canadensis in lung cancer treatment, warranting further experimental validation and exploration of novel therapeutic strategies.
60. Formulation and Evaluation of Soap Containing Extracts of Various Ethnomedicines
Shubham Wankhade, Manish Bhise, Manoj Shinde, Jayprakash Suryawanshi, Harshal Tare
Abstract
The herbal soap’s formulation includes neem leaf; all herbal ingredients are easily obtained from the local herbal market. Use of cosmetics is part of caring for the skin and other body parts due to the damaging effects of modern pollution and UV rays on human health; aloe plants produce a material used in cosmetic goods to treat burns, psoriasis, acne, and other skin disorders; preparation of herbal soap is a medication or therapy with therapeutic benefits for the skin, including antibacterial and antifungal qualities; the raw material used to make soap has a number of properties that make it a good medicinal or cosmetic. The plant used to manufacture soap has properties that can help eliminate acne, soften the skin’s epidermis, increase penetration, and hasten healing and resolution. Natural remedies like aloe vera are used to both prevent and cure a range of skin conditions. The medicinal properties of aloe vera soap include antiseptic, antimicrobial, antiviral, antioxidant, and antifungal properties. The aloe vera plant features tubular yellow blossoms, many-seeded fruits, and triangular, fleshy leaves with serrated edges. Each leaf consists of three layers: an inner, transparent gel that contains 99% water and glucomannans, amino acids, lipids, sterols, and vitamins in the remaining 2%. The intermediate layer of latex is composed of a bitter-yellow sap. Neem provides additional medicinal benefits. Studies have demonstrated the anti-inflammatory, anti-hyperglycemic, anti-ulcer, antimalarial, antifungal, antibacterial, antimutagenic, and anticarcinogenic properties of neem and its chemical components. Tulsi provides many skin-benefiting qualities, such as beep-clean skin. Turmeric and vitamin C are also used to help tone the skin when treating breakouts. Homegrown cleaning solutions with medicinal or sedative qualities, such as antimicrobial and antifungal qualities, can benefit the skin. The rough material used in the cleanser formulation has multiple prescription drugs or cosmetics attached to it. The plant used in cleanser formulations has the ability to smooth out skin imperfections, enhance skin texture, prevent breakouts, and hasten healing and resolution.
61. Development and Characterization of Olmesartan Medoxomil-Loaded Microspheres for Hypertension Management
Dipak Mali, Sandip Bandgar, Indrayani Bandgar, Dinanath Gaikwad
Abstract
Our aim is to develop and assess microspheres loaded with olmesartan medoxomil, the antagonist of angiotensin II receptor which is used in hypertension treatment, for their efficacy. The microspheres were fabricated through a solvent evaporation process employing eudragit L100 and chitosan as the inner phase and liquid paraffin as the outer phase. Optimization was done according to the results of entrapment efficiency and
in-vitro drug release. Fourier-transform infrared (FTIR) analysis indicated negligible interaction, which clarifies the suitability of the drug and excipients. The resulting microspheres exhibited a pale yellow hue and free-flowing characteristics, as confirmed by micromeritics experiments. Scanning electron microscopy (SEM) revealed smooth and spherical microspheres. Particle size, ranging from 187.44 to 358.75 μm, increased with polymer concentration, as determined by optical microscopy. Formulation F9, with a ratio of eudragit L100 to chitosan at 7:1, demonstrated the highest drug entrapment percentage (97.82%).
In-vitro release studies demonstrated a reduction in olmesartan medoxomil release with increasing polymer content, with formulation F9 sustaining release for 12 hours. Furthermore, short-term accelerated stability testing indicated the physicochemical stability of the microsphere formulations throughout the stability period.
62. Mebendazole Suppresses Tumor Growth and Hinders the Invasion of Triple-Negative Breast Cancer in Model Systems by Disrupting RAN-GTP Regulation
Rahmeh Saad Al-Ramamneh, Mohamed El-Tanani, Frezah Muhana, Moath Alqaraleh
Abstract
Due to the lack of targeted therapies, triple-negative breast cancer (TNBC), one of the most aggressive types of cancer, has a poor prognosis and a high death rate. TNBC frequently metastasizes to the brain, bones, and lungs. Studies have demonstrated a correlation between the metastatic behavior of A594 lung cancer cells and MDA-MB-231 breast cancer cells and the overexpression of the RAN GTP (RAN) gene. Using a variety of biological assays, this study sought to investigate mebendazole’s potential as an anticancer agent by specifically targeting the RAN gene. Both MDA-MB-231 breast cancer cells (IC50 7.5 μM) and A549 lung cancer cells (IC50 48.5 μM) were shown to be resistant to mebendazole’s ability to promote cell growth. The cytotoxic effect of mebendazole via the apoptotic pathway was confirmed by Annexin V assays on both cell lines. Furthermore, mebendazole demonstrated enhanced efficacy against TNBC by halting the cell cycle, preventing colony formation, invasion, and migration, and reducing RAN GTPase expression in both cell lines.
63. Enhancing Anticancer Potential: Optimization of Allicin Extraction from Regular Garlic and Characterization of Allicin-Loaded Copper Oxide Nanoparticles
Tufail Dana, Amjad Khan Pathan, Sufiyan Ahmad
Abstract
This research aimed to optimize the extraction and purification processes of allicin from regular garlic (
Allium sativum) and to evaluate the potential of allicin-loaded copper oxide (CuO) nanoparticles for anticancer applications. Initially, various solvents, including MilliQ water, 25% methanol, and phosphate buffer pH 2.5 in 60% methanol, were tested to determine the most effective conditions for extracting allicin. Among these, MilliQ water and 25% methanol demonstrated the highest extraction efficiencies, as evidenced by their absorbance values. The extracted allicin underwent purification and was subsequently characterized using fourier-transform infrared spectroscopy (FTIR) and high-performance liquid chromatography (HPLC). These techniques confirmed the identity and high purity of the allicin. Following purification, the allicin was encapsulated into copper oxide (CuO) nanoparticles using an optimized nanoprecipitation protocol. The physicochemical properties of the allicin-loaded nanoparticles were thoroughly characterized. Dynamic light scattering (DLS) analysis revealed a mean particle size of 123 nm, indicating a uniform and nanoscale particle distribution. Zeta potential measurements indicated a surface charge of -28.34 mV, suggesting good stability of the nanoparticles in suspension. Scanning electron microscopy (SEM) was employed to further analyze the particle size, surface charge, and morphology, providing detailed insights into the structural attributes of the nanoparticles. The successful encapsulation of allicin into CuO nanoparticles not only enhances the stability and bioavailability of allicin but also leverages the unique properties of CuO nanoparticles, which are known for their anticancer, antioxidant, and antimicrobial activities. This study underscores the potential of allicin-loaded CuO nanoparticles derived from regular garlic as a promising formulation for pharmaceutical applications, particularly in the field of oncology. These findings warrant further investigation into their clinical efficacy and safety to fully harness their therapeutic potential.
64. Repurposing Existing FDA-Approved Medications by Virtual Screening for Combatting
Pseudomonas aeruginosa Infections
Vaibhavkumar Jagtap, Nayana Baste, Manoj Shinde, Jayprakash Suryawanshi
Abstract
Pseudomonas aeruginosa, a notorious pathogen, poses significant challenges due to its resistance to multiple antibiotics. This study aims to identify potential FDA-approved drugs that could be repurposed to combat
P. aeruginosa infections through virtual screening. The target protein, DNA gyrase B 24kDa ATPase subdomain (PDB ID: 7PTF), was refined using PDB-REDO, improving geometric parameters despite a slight increase in R and R-free values. The virtual screening revealed several promising candidates with high binding affinities, including acetyldigitoxin (-9.9), digoxin (-9.5), digitoxin (-9.4), posaconazole (-9.3), venetoclax (-8.8), and itraconazole (-8.7). These top hits, primarily comprising cardiac glycosides and antifungal agents, exhibited large molecular weights, numerous hydrogen bond donors and acceptors, and significant molecular flexibility. The findings suggest potential repurposing opportunities for these drugs in treating
P. aeruginosa infections, warranting further
in-vitro and
in-vivo investigations to validate their antimicrobial efficacy.
65. Effect of Lyophilization on Characteristics of Iloperidone Nanosuspension
Shivraj Popat Jadhav, Prashant Kumar Dhakad, Tapasvi Gupta, Ritu Gilhotra
Abstract
Objective: The primary objective of this study is to develop the nanosuspension formulation of iloperidone and to check the effect of lyophilization on different characteristics of iloperidone nanosuspension.
Methods: Solvent-antisolvent method with probe ultrasonication was used for the formulation of nanosuspension. The nanosuspension was then converted into lyophilized form by using mannitol as a cryoprotectant and then evaluated for various parameters, including particle size, saturation solubility, scanning electron microscopy (SEM), thermal analysis, fourier-transform infrared (FTIR), in-vitro drug release study.
Result: From the study it was observed the increase in concentration of cryoprotectant while lyophilization has increased the particle size of nanosuspension. As there was an increase in particle size after lyophilization, there was a decrease in saturation solubility. In-vitro drug release also indicates a slight decrease in drug release after lyophilization. Overall, lyophilization might be used in the improvement of stability of nanosuspension, parameters must be chosen carefully for the process of lyophilization in order to obtain nanosuspension with good characteristics.
66. Formulation, Optimisation and Evaluation of Levodopa and Entacapone Loaded Transdermal Patches for the Treatment of Parkinson’s Disease
Akanksha Ghodke, Surabhi Taose, Priyanka Rathore, Neha Joshi, Aakash Singh Panwar
Abstract
Parkinson’s disease is an extrapyramidal motor disorder leading to progressive degeneration of neurons in substantia niagra, pars compacta and the dopaminergic tract. The most promising drugs used to treat Parkinson’s disease, i.e., levodopa and entacapoe have very low oral bioavailability because of first-pass metabolism, therefore to increase the bioavailability of levodopa and entacapone, these were incorporated in transdermal patches. Different formulations of the levodopa and entacapone drugs were prepared with different polymeric ratios, by using the solvent casting method and the formulations were evaluated for
in-vitro and
in-vivo tests, which focus on drug release and drug excipient compatibilities. Various models were applied to ascertain the kinetics of drug release by using
in-vitro release data
. Nine formulations were prepared and evaluated out of which F6 was found to be the best formulation, which contained HPMC and ethyl cellulose in the ratio of 2:3. It showed drug release of 99.11% in about 12 hours.
67. Synthesis, Pharmacological Study of 3,5-Di- Substituted Isoxazole Derivatives as Anticancer Drug Against Breast Cancer Cell Line Followed by Computational Study
Sonali Waghmare, Ramesh Sawant
Abstract
Objective: Cancer has remained a challenge to the healthcare system due to changes in eating habits and lifestyle, tremendous side effects of chemotherapy, and resistance to existing treatment due to mutations, which creates difficulty in identifying specific targets.
Chemistry and Methodology: In this study, equimolecular amounts of reagents were used to synthesize substituted isoxazoles from alpha-beta unsaturated intermediates.
Result: Compounds were collected in varying amounts of yield. Spectroscopic data supports the formation of compounds.
Compound Id shows GI50 of 46.3 μg/mL against MDA-MB-231.
Conclusion: The effective synthesis of novel derivatives has opened up exciting new avenues for medicinal research; one of these compounds has moderate anticancer properties.
68. Application of PCR and ELISA for Investigation the
Helicobacter pylori in Stool Specimens of Infected Patients
Saja A Al-Jumaili, Amina N Althwani, Ahmed Dawood Ahmed, Ahmad Abd alraheem Ibrahem Dahy, Zina Najim, Nawal M Al Khalidi
Abstract
Background: Infection with
Helicobacter pylori is a global health issue, and non-invasive and accurate testing is a promising diagnostic method. Because
H. pylori antibodies collapse quite gradually even after effective treatment. So, the tests for identifying the antibody of
H. pylori are missing specificity and sensitivity. Instead, the tests of stool antigen for
H. pylori are described as an alternative method because they have more reliability and simplicity.
Aim: The study was aimed to assess the performance of enzyme-linked immunosorbent assays (ELISA), for the detection of H. pylori antigen in stool and compare it to molecular tests by using two housekeeping genes.
Methods: Stool samples were collected from patients (85) who attended the Gastroenterology and Hepatology Teaching Center in Baghdad, Iraq, and underwent esophagogastroduodenoscopy (EGD) for biopsy in a period extended from November 2020 to July 2021. PCR and ELISA were used to Investigate H. pylori in stool specimens of infected patients.
Results: The result revealed that 74/85 (87.88%) of specimens were positive by ELISA, whereas 49/85 (57.6%) were positive for the 16 SrRNA gene related to Helicobacter genus and 35/85 (41.1%) were positive for amiA gene related to H. pylori species, and that means the ELISA test is more accurate than PCR analysis for detection of H. pylori bacteria in stool specimen.
Conclusion: Detection H. pylori Ag using the ELISA test was superior to the molecular test. Therefore, the ELISA test might replace other methods and could be used for the detection of active H. pylori infection before the inauguration of treatment between dyspeptic patients.
69. Preparation and Evaluation of
Ficus racemosa Extract Transdermal Gel for Antimicrobial and Anti-inflammatory Activity
Monika Sharma, Jyoti Gupta, Prabhjot Singh
Abstract
Background: Ficus racemosa (FR) belongs to the Moraceae family having different pharmacological activities. The primary aim of the researchers was to examine how varying polymer concentrations affect the outcome, additionally nature of penetration enhancers on microbial growth inhibition, and the protein denaturation inhibition capability of
F. racemosa extract (FRE).
Method: FRE has been prepared by a simple maceration process. By performing an antimicrobial assay procedure and in-vitro protein denaturation inhibition method, the antimicrobial and protein denaturation capability of the extract has been confirmed. Furthermore, 12 formulations of transdermal gel were developed with polymer (carbopol 934), which was used at non-identical concentrations (1, 1.5, 2, 2.5%) along with three dissimilar kinds of penetration enhancers, i.e., Tween 80, oleic acid, thioglycolic acid at the same concentration (1%). Transdermal gels have been prepared by a dispersion method & evaluated by physical parameters, viscosity, spreadability, pH, skin irritation, drug content, and in-vitro study with Franz diffusion cell.
Result: Formulation B3 showed the best results, having a polymer concentration of 1.5% and Tween 80 as a penetration enhancer.
70. Chemical Composition and Antioxidants of
Senecio vulgaris (Asteraceae)
Karzan Omer Qader
Abstract
The study included the antioxidant and chemical compounds of methanolic extract of
Senecio vulgaris in Iraq.
S. vulgaris has a rich history in traditional medicine for treating different health problems. The results gas chromatography-mass spectrometry (GC-MS) chromatogram of
S. vulgaris extract showed 19 peaks, which indicates the presence of 19 compounds (phytochemical constituents). Most of the chemical components extracted from
S. vulgaris include oleic acid (40.46%), n-Hexadecanoic acid (23.40%), 5,9-dimethyl-2-(1-methylethyl)-1-cyclodecanone (6.52%), octadecanoic acid (3.57%) and 1,2-benzenedicarboxylic acid, bis(2-methylpropyl) ester (3.27%).
The antioxidant activity of overall methanol extract contents of S. vulgaris was determined by adding different concentrations of methanol extract to 2,2-diphenyl-1-picrylhydrazyle (DPPH). The inhibitory activity was evaluated by using five different concentrations of methanol extract of S. vulgaris. The results showed that the antioxidant activity in concentration 3 μL/mL was 41.23%, while the highest antioxidant activity was 98.33% in 25 μL/mL compared with vitamin C, which was 16% in 3 μL/mL and recorded 91.97% in 25 μL/mL. The total antioxidant capacity of S. vulgaris methanol extract was evaluated as vitamin C equivalents per gram. The DPPH radical scavenging potency with a minimum IC50 value in S. vulgaris was5.64 μL/mL, while vitamin C was 3.09.
71. Synthesis and Method of Nanoparticles and Their Applications- An Exhaustive Review
Abhishek Singh, Tarun Parashar, Arbaz Khan, Vikash Jakhmola
Abstract
Nanoparticles are tiny little particles, going from 1 to 100 nm in size. They stand out enough to be noticed because they have unique properties that are not quite the same as bigger particles. Researchers can make nanoparticles utilizing various techniques like combining synthetic compounds as one, utilizing actual cycles like crushing, or, in any event, utilizing living organic entities like microbes. These minuscule particles have a ton of purposes since we have some control over their properties definitively. They’re utilized in things like conveying drugs inside the body, assisting responses with happening quicker in science (called catalysis), making sensors to identify things, working on clinical imaging, and tidying up contamination. Controlling how nanoparticles are made is significant because it assists us with ensuring they have the right properties for what we need to involve them. For instance, in the event that we’re making nanoparticles to convey drugs, we believe they should be a sure size and shape so they can go through the body successfully. Nanotechnology is assisting us with tracking down better approaches to battle against illnesses, like malignant growth and contaminations, by utilizing extraordinary nanoparticles that are ok for the body but can target and treat these sicknesses.
72. A Comprehensive Review of Advances in Nanoparticle-Based Cancer Therapy
Abdellateif Okkod, Sunith Reddy
Abstract
A promising method for treating different kinds of cancer is cancer therapy based on nanoparticles. The goal of this thorough analysis is to present a summary of the most current developments in cancer treatment using nanoparticles and discuss the different kinds of nanoparticles and how they might be used to enhance therapeutic efficacy and deliver anticancer medications. These include mesoporous dendritic silica nanospheres, gold nanoparticles, and chitosan nanoparticles. The review stresses the significance of stability and dynamic interfaces in attaining effective drug administration and addresses the difficulties related to medication release and degradation in nanoparticle-based therapy. Moreover, it investigates the immune reactions, such as dendritic cell maturation and immune response activation, that are brought on by nanoparticle-based therapy. Overall, this thorough analysis highlights the promise of these cutting-edge strategies for enhancing the effectiveness of cancer treatment and offers insightful information about the developments in nanoparticle-based cancer therapy. The information provided in this study contributes to the growing corpus of information in the field of nanomedicine and suggests future avenues for investigation and development of treatments utilizing nanoparticles to treat cancer.
73. Nanosuspensions in Breast Cancer Therapy: A Comprehensive Overview
Sebastine, Mohamed Zerein Fathima
Abstract
Nanosuspensions offer a promising avenue for enhancing breast cancer treatment through improved drug delivery, solubility, and targeting. These colloidal dispersions contain submicron drug particles, significantly increasing surface area and enhancing drug solubility and dissolution rates. This improvement can lead to increased drug bioavailability, enabling lower doses and reduced side effects. It is also possible to engineer nanosuspensions so that they are controlled-release drugs, providing sustained therapeutic levels at the tumor site. Nanosuspensions facilitate targeted drug delivery, which is one of their key advantages. In order to minimize systemic toxicity, nanosuspensions contain targeting ligands or antibodies that adhere to the surface of nanoparticles in order to deliver drugs specifically to breast cancer cells. The nanosuspension platform also allows a combination therapy approach to be used, allowing multiple drugs to be delivered simultaneously in order to achieve synergistic effects and combat drug resistance. Nanosuspension treatments can be beneficial both therapeutically and for imaging and diagnostic purposes. Using nanoparticles labeled with imaging agents, it is possible to visualize tumors and monitor treatment responses. Nanosuspensions may reduce side effects associated with traditional chemotherapy by improving drug targeting and reducing systemic exposure. A nanosuspension represents a promising treatment option for breast cancer. Nanosuspensions must be fully exploited for their full potential to improve outcomes and quality of life for patients.
74. Irinotecan Resistance Mechanisms in Cancer: Challenges and Opportunities
Bindu Ghodeswar, Santosh Chhajed
Abstract
Irinotecan, a topoisomerase I inhibitor, has been widely used in the treatment of various solid tumors, including colorectal, lung, and pancreatic cancers. However, its efficacy is often limited by the development of resistance mechanisms within cancer cells. Understanding these resistance mechanisms is crucial for improving treatment outcomes and developing effective therapeutic strategies. This review article provides a comprehensive overview of the mechanisms underlying irinotecan resistance in cancer. Key resistance mechanisms discussed include the overexpression of drug efflux pumps, activation of DNA repair pathways, altered drug metabolism, and microenvironmental factors. Clinical implications, challenges, and emerging opportunities in overcoming irinotecan resistance are also explored, including the identification of biomarkers predictive of response/resistance, combination therapies targeting multiple resistance pathways, and advancements in drug delivery systems. By elucidating the complexities of irinotecan resistance, this review aims to inform future research directions and facilitate the development of personalized treatment approaches for patients with resistant cancers.
75. A Review on Phytochemical Analysis and
In-vitro Antioxidant Activity of Curcumin from
Curcuma longa L. Rhizomes
Udayakumar N, Reefa Fathima K, Umme Hani PS, Mounika N
Abstract
This study focused on investigating the phytochemical composition and evaluating the antioxidant capability of an extract obtained from the rhizomes of
Curcuma longa (turmeric). Preliminary screening tests revealed the presence of various bioactive compounds like alkaloids, flavonoids, phenolic substances, saponins, terpenoids, cardiac glycosides, and fixed oils/fatty acids in the methanolic rhizome extract. The antioxidant potential of the extract was assessed using the widely employed 1,1-diphenyl-2-picryl-hydrazyl (DPPH) free radical scavenging assay. The findings indicated a concentration-dependent enhancement in radical scavenging activity, reaching a maximum of around 81% at the highest concentration evaluated (3 mL). The remarkable antioxidant capacity can be attributed to the unique structural features of curcumin, the principal bioactive compound present, which contains methoxy, phenoxy, and carbon-carbon double bonds that enable efficient neutralization of free radicals and reactive oxygen species. Furthermore, curcumin has been reported to modulate the activity of transcription factors like Nrf2, thereby upregulating the expression of antioxidant enzymes and bolstering the body’s defense against oxidative stress. These findings offer empirical support for the historical use of
C. longa and underscore the diverse potential uses of curcumin as a natural antioxidant across different sectors, including food, pharmaceuticals, and cosmetics.
76. Herbal Hair Serum – A Promising Nourishing Agent for the Hair Growth
Yashshree N Yenurkar, Rahul G Ingle
Abstract
With their promise of nourishing properties, improved scalp health, and stimulation of hair growth, herbal hair serums have become increasingly popular as natural substitutes for traditional hair care products. An overview of herbal hair serums is given in this abstract, with particular attention to their composition, effectiveness, safety, and possible advantages for hair health to the assertion of reduced hair loss and improved hair growth. Alopecia is a common issue among metropolitan dwellers who are subjected to stress, environmental issues, and other issues. Thus, we deduce from this review paper that alopecia may be effectively treated with numerous herbal remedies without any adverse effects. There are several allopathic medications kinds for treating hair loss, however they all have a lot of adverse effects. The foundation of any medical research is its herb collection. About 80% of residents suggested using herbal medications since they had fewer negative effects and more positive effects than the animal system. Our article shows that herbal hair serum contains a number of vital ingredients that are necessary to maintain the correct operation and self-defense. It also offers excellent protection from extreme heat. Many factors have contributed to the severe hair loss issues that the younger generations are now experiencing. Generally speaking, hair loss is not transient. Known to be the most significant organ in the mammalian system, the hair follicle has a variety of roles in self-defense, extreme temperature protection, and attractiveness and gender differentiation. The younger generations are facing severe hair loss issues as a result of several lifestyle changes, including worry, weariness, and overindulgence in junk food and hair colouring and styling products.t alopecia is the outcome. To encourage the production of new hair and prevention of hair loss, hair roots must be activated which is why many individuals experiencing hair loss are seeking different treatments. The anti-dandruff and hair care properties of
Citrus sinensis are employed.
77. Development of Inhaled Tuberculosis Microparticle using Polysaccharide Polymers Containing Rifamycin Groups:
In-vitro and
In-vivo Study
Finisha Prigestiya Dinanti, Tristiana Erawati, Dewi Melani Hariyadi
Abstract
Tuberculosis (TB) is one of the urgent global health problems. TB therapy involves the use of antibiotics, but unwanted side effects often accompany the treatment of TB with high doses and long periods of time. In an effort to increase the effectiveness of TB treatment and reduce side effects, direct drug delivery to the lungs is the focus of research. One of the approaches used is the development of drug delivery systems that use natural polymers in dry powder inhalation (DPI) formulations. Natural polymers, especially polysaccharides, have various advantages, such as biodegradability, biocompatibility and non-toxicity. This review discusses the use of rifamycin microparticle tuberculosis inhalation using polysaccharide polymers and reviews relevant
in-vitro and
in-vivo studies. The use of natural polymers, especially polysaccharides, is expected to increase the efficiency of TB therapy by reducing drug doses and systemic side effects and increasing direct drug delivery to infected organs.
78. Current Updates on the Therapeutic Potential of Diosgenin
Sowmya C, Thirumal V, Preetika S, Epsiba A
Abstract
Diosgenin (DG) is a naturally occurring steroid saponin that can be obtained from several plants. A lot of the artificial steroidal drugs that are used extensively in the pharmaceutical industry come from diosgenin for the treatment of various disease conditions. DG has various intriguing pharmacological effects, including anticancer, antidepressant, and anti-inflammatory and anti-infectious capabilities. Apart from its health advantages, DG is challenging to utilize in therapeutic applications due to its poor water solubility, bioavailability, and rapid physiological change. The DG nanotechnology for medicine formulations has been tested as a possible therapy for a variety of disorders employing a broad range of
ex-vivo, in-vitro, and
in-vivo models and delivery methods. Based on this analysis, it is possible to infer that DG is a viable therapeutic alternative for the management of numerous ailments, such as diabetes, cancer, neurological conditions, inflammatory diseases, and skin conditions.
79. Revolutionizing Brain Tumor Therapy: Unleashing the Potential of Phytosomal Nanoparticles
Hitesha Gole, MS Manjusha Bhange, Gunjan Rathod, Heena Mahurkar, Gaurav Kubde
Abstract
Unleashing the potential of phytosomal nanoparticles in brain tumor therapy. This article discusses the transforming potential of phytosomal nanoparticles in the fight against brain tumors, delving into this novel field. When the complex problems of traditional medicine are considered, the special qualities of phytosomal nanoparticles show great potential. Because of the nanoparticles’ ability to cross the blood-brain barrier, it is possible to transport drugs specifically to the brain, which solves a long-standing issue with current treatments. This accuracy reduces off-target effects, providing a crucial therapeutic benefit in a sensitive brain environment.
Phytosomal formulations are further distinguished by their lower toxicity and biocompatibility, which establishes them as a safer substitute for several traditional medicines. These natural compound-based nanoparticles fit in with the medical paradigm shift towards personalized and integrative care. The versatility of phytosomal formulations opens up new avenues for personalized medicine in the treatment of brain tumors by enabling customized approaches based on the molecular profiles of individual tumors.
Phytosomal nanoparticles provide a unique combination of natural pharmacopeia and state-of-the-art nanotechnology, which presents opportunities for novel therapeutic approaches beyond their clinical usefulness. The consequences could change the way brain tumors are treated as research and clinical trials are conducted. In order to overcome obstacles related to scalability, legal frameworks, and long-term safety assessments, cooperation between researchers, physicians, and legislators is essential. The full potential of phytosomal nanoparticles in the fight against brain tumors will be realized through ongoing research into how they might work in concert with current therapies and the creation of evidence-based guidelines. This article essentially presents a paradigm shift that will have a significant impact on cancer therapy in the future. It is the result of the convergence of innovative ideas inspired by nature with state-of-the-art nanotechnology.
80. From Gut to Brain: Targeting Probiotics in Neurodegenerative Health
Jain Sanidhya, Mazumder Avijit, Das Saumya
Abstract
Probiotics have evolved from a dynamic and living culture that enhances the composition of the GI tract microbiota to encompass more specific benefits, notably the immunomodulatory ability of well-defined strains. The most prevalent sources of beneficial strains, or potential probiotics, are commonly found within the
Bifidobacterium and
Lactobacillus genera, and certain strains among them possess remarkable capabilities in reducing inflammation, preventing ulcers, alleviating diarrhea, and even combating autism. Recent evidence further emphasizes the essential part of GI microbiome dysbiosis in neurodegenerative disorders. These conditions may manifest through the intricate network of interconnections amongst the microbiota, gut, and brain, facilitating bidirectional transmission
via pathways involving neuroimmune responses, neuroendocrine signaling, and direct neural connections like the vagus nerve. The present focus of probiotic research aims to provide suitable and secure bacterial stimulation to counteract abnormal immune reactions linked to allergic inflammation and various neurodegenerative diseases. Nonetheless, additional careful scientific efforts are essential to completely clarify the immune-modulating potential of certain probiotic types regarding these particular goals.
81. Liposomes in Medicine: An In-depth Analysis of Preparation Methods and Applications
Diptee Gupta, Suruchi Agarwal, Kavitha Komire, Vishal Kumar
Abstract
Liposomes are the targeted drug administration system that offers the potential to improve the medicinal value of drugs by boosting the concentration of medication the duration of time in intended cells, thereby reducing side effects. Liposomes, which are sphere-shaped vesicles built from phospholipids and cholesterol, are being investigated extensively as a means of increasing the bioavailability and delivery of therapeutic medications. Liposomes have both hydrophilic head and hydrophobic tail and exhibit eminent properties, including reduced toxicity, better biocompatibility, easily biodegradable, easy to function and enhanced sustained release of drugs with increased therapeutic efficacy. Liposomes are said to be an ideal drug-carrier system as they enhance the delivery of anticancer drugs at the tumor site. Since liposomes are amphiphilic carriers that may be modified to have various functional characteristics, they are seen as a potential technology for a range of pharmacological and industrial uses. As a potential way to carry drug delivery across cell membranes, liposomes help medications to target specific disease sites. Liposomes are employed to deliver genetic material, such as DNA fragments, to specified cells so they may synthesize certain proteins. Thus, liposomes are investigated as adaptable nano-vesicular vehicles with potential medical applications for medicinal and diagnostic purposes. The future of liposomal formulations is projected to be a multipurpose use of imaging capabilities and medicinal components in a single liposome for diagnostic and actual-time therapy. The most promising approach for topical administration is liposomal drug delivery since it is compatible with living systems and can accommodate simultaneously hydrophobic and hydrophilic medicated substances because of the amphipathic feature of phospholipids.
82. Nanotechnology in Ankylosing Spondylitis: Advancements in Drug Delivery and Targeted Therapy
Anuj Kumar, Jitendra Singh Chaudhary, Anubhav Dubey, Shubham Sanjay Pachorkar
Abstract
Ankylosing spondylitis is a chronic inflammatory disorder primarily affecting the spine and the sacroiliac joints, although it is now considered for new drug target possibilities. It is an area in which nanotechnology has shown significant potential. This report offers an extensive review of the formulation design, clinical utility, and current development in the use of nanotechnology for treating AS. The rational design principles of nanotherapeutics, created to modify the myriad processes implicated in AS pathophysiology, were examined. It comprises drug delivery systems, targeting approaches, and release processes. Clinical and preclinical evidence of nanomedicines’ tolerability and effectiveness in AS therapy is reported. In conclusion, this document reflects the recent state of these nanotechnology-based treatments for AS and discusses the author’s future goals in developing novel, powerful treatment strategies that generate strong patient outcomes.
83. Unlocking Dithranol’s Potential: Advanced Drug Delivery Systems for Improved Pharmacokinetics
Pankaj Kumar, Kuldip Kumar Savita, Anubhav Dubey, Sandeep Singh Gaur
Abstract
Dithranol is a therapeutic agent mainly used for psoriasis; however, its clinical use is limited by poor stability, skin irritation, and low patient compliance with conventional formulations. This paper reviews the various advanced drug delivery systems that have been formulated to bypass the above limitations and improve the pharmacokinetics of dithranol. In this context, we describe the problems of the current formulations, which are the instability of the drug and adverse reactions to the skin. Further, we present the advantages of advanced delivery systems, including nanoparticles, nanosuspensions, liposomes, niosomes, solid lipid nanoparticles and nanostructured lipid carriers, for drug stabilization and delivery to target tissues. We elaborate on the working of polymeric systems, including hydrogels, microparticles, micelles, and prodrugs, with which drug solubility is improved and drug release is sustained. Finally, through
in-vitro and
in-vivo studies and clinical procedures, details are given regarding the drug release kinetics, pharmacokinetics, and biodistribution of such formulations. The text elaborates on future directions and new technological approaches toward the delivery of dithranol. These advanced delivery systems will help to overcome the limitations of the existing formulations and achieve a higher therapeutic impact of the drug on psoriasis and other skin diseases.
84. Revolutionizing Arthritis Care: Cutting-Edge Nanogel Formulations for Targeted, Long-Lasting Relief and Enhanced Mobility
Saurabh Gupta, Jitender Kumar Malik, Gyan Singh
Abstract
Arthritis, which impacts individuals all over the globe, is characterized by severe pain and a high prevalence rate. Current treatments for the illness come with a number of obstacles and difficulties. It is necessary to explore alternative paradigms, as systemic medications aren’t necessarily the greatest choice. The new discipline of nanotechnology has the potential to significantly alter several aspects of arthritis treatment. Therefore, the work provides strong support for developing novel therapies employing compositions of topical nanogels. Traditional systemic narcotics have their limitations, and the evolution of arthritis treatments has to take that into consideration. Thus, novel nanogel formulations offered as a nanotechnology solution may out to be quite advantageous. Applying nanogels to product design has been a significant administrative step. Nanogels offer unparalleled precision and efficiency, whether you’re dealing with simple concepts, cutting-edge techniques for surface modification, or intricate strategies for drug encapsulation. New data from pain evaluations, clinical studies, and comparisons to traditional therapies have supported their revolutionary potential and effectiveness. However, the patient’s health must always come first. While we strive to mitigate adverse effects and evaluate long-term ramifications, the positive outcomes of our biocompatibility testing offer reassurance regarding the safety profile of nanogels. For regulatory and ethical considerations, there must be transparency, informed permission, and equitable access for nanotechnology-powered arthritic treatments. This study calls for additional research into the use of nanotechnology in the treatment of arthritis because recent advances in nanogel technology have the ability to completely transform the current approach to treating this debilitating disease, bringing about a new era of precision medicine.
85. Kinetics Aspects in Design and Release of Nasal Drug Delivery Systems
Shubham Choudante, Priya Deshmukh, Vaishali Kadam, Harshal Tare
Abstract
The traditional school of Indian medicine includes a sort of nasal therapy known as Nasya karma. There is a lot of recent interest in using the nasal route for administering difficult medications including tiny polar compounds, vaccines, hormones, peptides, and proteins. Nasal drug molecules are highly suited for systemic distribution and the absence of hepatic first-pass metabolism. Vaccination through the nose is thought to be a straightforward and economical method with improved patient compliance, and it may also provide immunity at numerous distant mucosal locations. Microparticle, nanoparticle, and liposomal nasal vaccination delivery technologies are now in development and show protection in animal models. Both pharmacokinetics & pharmacodynamics of nasal administration devices have been studied
in-vivo by a number of different research organizations. The purpose of this review was to summarise these studies and bring attention to the work done on nasal-based formulations to better treat conditions like epilepsy, schizophrenia, and neurodegenerative diseases.
86. Drug-Coated Central Venous Catheters – A Comprehensive Review of Strategies in the Development to Overcome Biofilm Formation and Related Infections
Nissara Ahammed, Revathi Sundaramoorthi, Venkatesh Dinnekere Puttegowda
Abstract
Central venous catheters (CVCs) are implantable medical instruments regularly used in intense care units for the easy introduction of medical drugs and medicaments, to give fluids intravenously, nutriments, transfusion of blood and also to withdraw blood samples. Bloodstream infections associated with the usage of catheters are the most recurrent, harmful as well as expensive impediment. This is the omnipresent reason for the introduction of bacteria and related infections. Among the various types of medical devices, the rate of infection, morbidity and mortality are higher with the usage of CVCs than any other types of medical instruments. Biofilm developed due to contamination by microorganisms. The biofilm is a bunch of microorganisms accumulated on the surface of CVCs. These biofilms contribute to the proliferation of microbes and increase antimicrobial resistance against antibiotics, affect the host’s immunity and get spread to the various body parts. Numerous approaches have been evolved to overcome the above mentioned issues associated with the usage of CVCs. In the said review, the authors have summarized the usage of CVCs, biofilm formation, development of infection, strategies and innovations in the modification of CVCs aiming to avoid the CRBSI and subsequent resistance to antimicrobial drugs.
87. Cutting-Edge Developments in Microemulsion Technology: Diverse Applications, Formulation Innovations, and Future Horizons
Niranjan D Chivate, Anuradha N Chivate, Akshay R Yadav, Shubhangi J Patil
Abstract
Microemulsion technology has emerged as a versatile and dynamic solution with widespread applications across various industries. This review delves into the diverse applications, formulation innovations, and anticipated future trends in microemulsion technology. From pharmaceuticals and food to cosmetics and enhanced oil recovery, the unique properties of microemulsions have paved the way for numerous breakthroughs. We explore the formulation strategies that contribute to their stability and efficiency, shedding light on the key factors influencing their success. Additionally, the article highlights the current landscape of microemulsion applications and discusses how ongoing research is shaping the future of this promising technology.
88. Formulation, Characterization and Stability Aspects of Mesoporous Silica Nanoparticles
Neha Padiyar, Nidhi Nainwal, Yogita Ale, Deepika Galwan
Abstract
Mesoporous silica nanoparticles are a type of inorganic nanoparticles having mesopores of 2 to 50 nm in size. The nanosized mesoporous particles of silica facilitate endocytosis in drug targeting without any side effects. Mesoporous silica nanoparticle (MSN) can be used to deliver a variety of therapeutic agents or gene delivery through active or chemical adsorption. MSNs can be used in the field of biomedical for the detection and treatment of various diseases like cancers, infection, inflammation, diabetes, bone-related disorders, cardiac diseases, neurodegenerative diseases, etc. The unique characteristics of MSNs in the form of easily adjustable pore size, surface area, particle size, pore volume, and surface morphology are advantageous not only in the biomedical field but also in the fields of biosensors, imaging, agriculture, thermal energy, and catalysis, etc. MSNs provide high surface area, easy surface functionalization, and controlled drug release. MSNs are formulated after condensation of silica in the presence of molecular templates like surfactants and polymers. This review article focused on giving in-depth knowledge about formulation techniques. Various types of excipients, such as catalysts, silica, solvents and surfactants utilized for the formulation of silica-based nanoparticles, have been summarized. The characterization of MSNs using suitable techniques was also reviewed. The stability of MSNs and factors affecting their stability is a crucial part of formulation development that is discussed here.
89. Polymeric Nanoparticle-Mediated Targeted Drug Delivery System: A Promising Approach for Breast Cancer
Naimish Nanda, Chozharajan Tharmaraj, M Akiful Haque, Swapna S
Abstract
After lung cancer, breast cancer (BC) is the second most frequent malignancy in women globally. Surgery followed by chemotherapy is the conventional treatment plan for BC. However, both are unsuccessful in treating BC because of the harmful effects that these treatments have on healthy tissues and organs. Many polymeric nanoparticles (PNPs) have been discovered and created recently to selectively aim cancer cells without harming normal cells. As an outcome, drug delivery systems (DDS) mediated by NPs have developed as a possible method to treat BC. PNPs have several special qualities that make them ideal for cancer treatment due to their tunable surface functions and choosiness to target tumor cells and minimize side effects.
90. Solid lipid Nanoparticles and Nanostructured Lipid Carrier: A Novel Approach for Lipid-Based Drug Delivery System
Naimish Nanda, Chozharajan Tharmaraj, Saswati Panigrahi, Mandadi Sandhya Rani
Abstract
Lipid nanoparticles, or LNPs, including nanostructured lipid carriers (NLCs) and solid lipid nanoparticles (SLNs), attracted a lot of attention lately. SLNs were formed to circumvent the confines of the most common colloidal carriers because of their benefits, which include a favorable profile of release and precise administration of the drug with great physical stability. NLCs are the succeeding group of lipid nanoparticles with better capacity loading and durability. There are three possible NLC structural models. These LNPs may find usage in clinical medicine, research, cosmetics, and drug delivery.
91. A Panoramic Review on Gastro-Retentive Floating Drug Delivery System
Latika Bisht, Tarun Parashar, Mansi Butola, Vikash Jakhmola
Abstract
Floating drug delivery has been demonstrated to be the most efficacious of the numerous gastroretentive drug delivery mechanism strategies. The concept behind this system has drawn substantial interest in recent decades. Several strategies are currently implemented to prolong the stomach residence durations, such as floating drug delivery systems, swelling and expansion systems, polymer bioadhesive systems, deformation systems, high-density, etc., systems, and various delayed emptying gastric devices. From a formulation and technology standpoint, floating drug delivery equipment is a rather simplistic and straightforward approach. Floating delivery of drug systems is one of the GRDFs used to increase stomach residence duration. The floating medication delivery device can persist in the gastrointestinal region for several hours due to its floating action on the stomach contents, extensively enhancing the gastrointestinal residence period of drugs. The main thrust of this review is on the design, factors, characterization, applications, evaluation criteria, and prospective future gastro-retentive floating medication delivery techniques.