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Journal of Applied Pharmaceutical Research
Published by Creative Pharma Assent
ISSN : -     EISSN : 23480335     DOI : 10.18231
Core Subject : Health,
Medicine & Pharmacology
Journal of Applied Pharmaceutical Research (JOAPR) is an official publication of Creative Pharma Assent (CPA). It is an open access, peer review online international journal. JOAPR is primarily focused on multiple discipline of pharmaceutical sciences (Pharmaceutics, Pharmaceutical Technology, Biopharmaceutics, Cosmetic Technology, Pharmacokinetics, Pharmaceutical/Medicinal Chemistry, Computational Chemistry and Molecular Drug Design, Pharmacognosy and Phytochemistry, Herbal drugs/ formulations, Pharmacology, Pharmaceutical Analysis, Pharmacy Practice, Clinical and Hospital Pharmacy, Cell Biology, Genomics and Proteomics, Pharmacogenomics, Bioinformatics and Biotechnology of Pharmaceutical Interest) which publish quarterly. JOAPR also includes evaluation of pharmaceutical excipients & their practical application to research & industry based efforts. The aim of the scientific journal, JOAPR is to present a wide area for the current researchers to share their noble works and ideas in terms of the research papers, review articles and short communications. JOAPR only publish the original research works with a definite innovation and novelty after thorough reviewing. The paper must have a suitable and proper scientific background.
Arjuna Subject : -
Articles 459 Documents
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Formulation and evaluation of diclofenac emulgel using natural permeation enhancers Chandra Sekhar Naik D; Shaik Noor Mahammed; Mudigedu Samreen; S. Vamsi; P. Hemalatha
Journal of Applied Pharmaceutical Research Vol. 13 No. 2 (2025)
Publisher : Creative Pharma Assent

Show Abstract | Download Original | Original Source | Check in Google Scholar | DOI: 10.69857/joapr.v13i2.907

Abstract

Background: This study aimed to formulate a stable diclofenac emulgel and determine the penetration rate using different natural penetration enhancers. Methodology: Carbopol (934) and Hydroxypropyl methyl cellulose (HPMC) were utilized as gelling agents due to their favorable viscosity characteristics, which render them widely used for regulating the flow properties of topically administered dosage forms. In the research, diclofenac served as the active ingredient, while Carbopol (934) & HPMC (0.5%) acted as gelling forms to form a proper gel base. Emulsion contains Tween-20 (0.05%), PEG (0.6%), liquid paraffin (0.75%), span-20 (0.1%), along with natural penetration enhancers (0.3%) initially prepared gel base & the emulsion with natural penetration enhancers combine conjointly to shape an appropriate diclofenac emulgel. Results and discussion: According to the study, the improved batch exhibits a 95.08% release in 48 hours and remains stable for about three. The optimized batch exhibits 46.6% suppression in the microbiological assay, whereas the marketed treatment only demonstrates 32.3% inhibition. However, the skin irritation test results have no erythema or edema. The rabbits' skin showed no signs of discomfort. According to stability experiments, the synthesized emulgel's antifungal activity, rheological analysis, in vitro drug release, and physical appearance did not alter after three months of storage. Conclusion: Overall, it was recommended that, in contrast to cream, the emulgel formulation come after the drug release for controlled, long-term drug delivery.
Design, development, and optimization of mucoadhesive buccal films of ganaxolone for enhanced bioavailability Pawar, Onkar; Godge, Rahul; Shinde, Ganesh; Barde, Kailas; Vikhe, Akshay
Journal of Applied Pharmaceutical Research Vol. 13 No. 2 (2025)
Publisher : Creative Pharma Assent

Show Abstract | Download Original | Original Source | Check in Google Scholar | DOI: 10.69857/joapr.v13i2.943

Abstract

Background: CDD disorder affects children mainly during their first three months of life. The buccal route offers advantages over oral administration for ganaxolone by avoiding first-pass metabolism and providing direct systemic absorption. This study aimed to formulate and characterise mucoadhesive buccal films of ganaxolone to increase its bioavailability. Methods: Mucoadhesive buccal films were prepared using a solvent casting technique employing HPMC K4M and Moringa gum as polymers. The formulation was optimized using a 32-factorial design, where polymer concentrations were varied systematically to achieve optimal film properties. Nine batches (OF1-OF9) were formulated and evaluated for various physicochemical parameters, mucoadhesive strength, percentage drug content, goat buccal mucosa permeation study, and stability analysis. Results: Based on the findings, the OF8 batch containing optimal polymer ratio (250mg HPMC K4M and 60mg Moringa gum) emerged as the superior formulation with 94.45±0.34% drug content, 15.37±0.58 N/mm² tensile strength, and 7.8±0.57 N mucoadhesive strength. Permeation studies consequently confirmed 96.37% of the drug at 8 hours with a 13.63 µg /cm² /h permeation rate. There was no evidence of drug-excipient interaction in FTIR and DSC analysis. The formulation was set to be stable for 6 months at accelerated conditions (40±2°C, 75±5% RH) with an average tensile strength above 15 N/mm² and an average ex-vivo drug permeation of 93%. Conclusion: This optimized buccal film formulation demonstrates promising potential for clinical application in CDD treatment by offering enhanced bioavailability, controlled release, and patient-friendly administration, which is particularly beneficial for pediatric patients.
Identification of novel potential benzimidazole derivatives by pharmacophore generation, 3D-QSAR, virtual screening, molecular docking and ADME/ TOX analysis against breast cancer as targeted estrogen alpha receptor Sharma, Aastha; Banga, Nitish; Marwaha, Rakesh Kumar; Narasimhan, Balasubramanian
Journal of Applied Pharmaceutical Research Vol. 13 No. 2 (2025)
Publisher : Creative Pharma Assent

Show Abstract | Download Original | Original Source | Check in Google Scholar | DOI: 10.69857/joapr.v13i2.951

Abstract

Background: The estrogen alpha receptor (ERα) is critical in breast carcinogenesis. Although selective estrogen receptor modulators like tamoxifen are clinically used, their adverse effects highlight the need for safer alternatives. The study uses computational methods to identify potential ERα inhibitors within a benzimidazole scaffold. Methodology: This study employed computational approaches, including pharmacophore generation, 3D-QSAR, virtual screening, molecular docking, and in silico ADME/Tox analysis. The best pharmacophore model (DDRRR_1) identified two hydrogen donors and three aromatic rings as critical features. Moreover, a rigorous external validation was used on decoy databases with optimized metrics (ROC, BEDROC, AUROC). A subsequent atom-based 3D-QSAR model with a high correlation coefficient (R² = 0.9), cross-validated coefficient (Q² = 0.8), and Fisher ratio (F = 80.1) was developed. Benzimidazole scaffolds from PubChem were screened, followed by docking against ERα (PDB ID: 3ERT) and ADMET profiling. Results and Discussion: The pharmacophore model validated the importance of the identified features. The 3D-QSAR model effectively screened benzimidazole scaffolds, with five component PLS factors, supporting the pharmacophore findings. This model effectively screened benzimidazole scaffolds obtained from the PubChem database, followed by molecular docking against the targeted protein ERα (PDB ID: 3ERT) and identified five promising compounds. ADME/Tox profiling revealed PubChem ID 3074802 (2-[2-(1H-indol-3-yl) ethyl]1H-benzimidazole) has favourable pharmacokinetics and a low toxicity profile. Conclusion: These findings indicate that PubChem ID 3074802 is a promising candidate for further therapeutic drug development in breast cancer treatment. It demonstrates the highest binding affinity (-9.842 kcal/mol) compared to the standard drug Tamoxifen (-5.357 kcal/mol) and exhibits a favorable ADME/Tox profile.
A comprehensive review of peptic ulcer disease: epidemiology, experimental models, and mechanistic insights Singh, Laliteswar Pratap; Chatterjee, Sandip; Kar, Sanjeeb Kumar
Journal of Applied Pharmaceutical Research Vol. 13 No. 2 (2025)
Publisher : Creative Pharma Assent

Show Abstract | Download Original | Original Source | Check in Google Scholar | DOI: 10.69857/joapr.v13i2.953

Abstract

Background: Peptic ulcer disease (PUD) is one of the most common gastrointestinal disorders, resulting from an imbalance between aggressive and protective factors, leading to mucosal erosion. Various factors influence its pathogenesis, including Helicobacter pylori infection, NSAID use, and oxidative stress. Objective: We review PUD epidemiology, varying experimental models, and mechanistic insights into PUD and promising therapeutics. Methodology: We systematically reviewed previous literature on PUD, including epidemiological trends, commonly used in vivo, and molecular mechanisms. Results and discussion: The global prevalence of peptic ulcer disease (PUD) follows an epidemiological pattern influenced by geography, lifestyle, and genetic factors. Experimental models using ethanol, NSAIDs, or Helicobacter pylori induction provide valuable insights into disease progression and pathophysiology. Emerging trends:  Recent research in peptic ulcer disease focuses on molecular mechanisms, gut microbiome interactions, personalized therapies, and novel pharmacological agents. Molecular studies explore genetic and epigenetic factors influencing ulcer formation, while microbiome research examines the role of gut bacteria beyond H. pylori. Personalized treatment approaches use genetic profiling and biomarkers to enhance efficacy and reduce toxicity. Additionally, emerging pharmacological agents aim to improve acid suppression, promote mucosal healing, and develop more effective H. pylori eradication strategies. Conclusion: A deeper understanding of PUD pathophysiology through epidemiological studies and experimental models can aid in developing novel, targeted therapies. Future research should focus on alternative treatments, including phytochemicals and probiotics, to enhance ulcer prevention and management.
Development of a stability-indicating UPLC method for quantification of mirvetuximab soravtansine-gynx in pharmaceutical formulations using quality by design (QbD) principles Rao, K. V. Umamaheswara; Shorgar, Neetu
Journal of Applied Pharmaceutical Research Vol. 13 No. 2 (2025)
Publisher : Creative Pharma Assent

Show Abstract | Download Original | Original Source | Check in Google Scholar | DOI: 10.69857/joapr.v13i2.977

Abstract

Background: This study intended to introduce a robust ultra-performance liquid chromatography (UPLC) method for quantifying Mirvetuximab soravtansine-gynx (MSG) in pharmaceutical dosage forms. A systematic approach incorporating the Design of Experiments (DoE) was employed to optimize reliable, sensitive, and efficient chromatographic conditions. Methodology: The finalized method utilized a Waters ACQUITY BEH Phenyl (50 mm) Column with a mobile phase comprising acetonitrile and 0.1% aqueous formic acid in 30:70 (v/v) at 0.2 mL/min and 271 nm and PDA wavelength. Results and discussion: The method validation demonstrates excellent linearity (R² = 0.991, p < 0.05) over 17.50–105 µg/mL. The Intraday and interday precision (%RSD) values were 0.568 and 0.544, respectively, confirming method reproducibility. Accuracy was validated through recovery studies, which produced results within the range of 100.1–100.5%, whereas the robustness test highlights the method's resilience to minor variations. This method detects MSG at a very low concentration of 0.42 µg/mL, confirming method sensitivity. The forced degradation studies were conducted under various stress conditions. The result suggests that moderate degradation of 10.3%, 14.5%, and 9.5 % was noticed in acidic, peroxide, and reduction (9.5%) conditions. Conclusion: The purity analyses confirm the absence of significant impurities in the stress degradation chromatogram, highlighting the stability of MSG and the reliability of the proposed method. In conclusion, the proposed method was rapid, sensitive, precise, robust, and stable for quantifying MSG in pharmaceutical formulations.
Antioxidant and hepatoprotective activity of Nigella sativa alcoholic extract in a CCl4-induced rat A.S. Devadhe; Dighe, Santosh; S.S. Yadav; S. B Bhawar; R D Ghogare
Journal of Applied Pharmaceutical Research Vol. 13 No. 2 (2025)
Publisher : Creative Pharma Assent

Show Abstract | Download Original | Original Source | Check in Google Scholar | DOI: 10.69857/joapr.v13i2.985

Abstract

Background: This study investigated the antioxidant, hepatoprotective, and sedative modulatory effects of Nigella sativa alcoholic extract (NSAE) in CCl4-induced hepatotoxicity in rats. Methods: Male Wistar rats were divided into six groups (n=6): normal control, CCl4 control, silymarin (50 mg/kg), and NSAE (100, 200, and 400 mg/kg). Hepatoprotective effects were evaluated through biochemical parameters, oxidative stress markers, and histopathological examination.  Results: NSAE treatment (400 mg/kg) significantly restored liver function markers, including SGOT (20.95 ± 0.52 IU/L, p = 0.033) and SGPT (28.61 ± 0.67 IU/L, p < 0.001), compared to CCl4 control. Total protein and albumin levels were normalized to 5.68 ± 0.54 mg/dL and 3.84 ± 0.48 mg/dL, respectively. Antioxidant parameters showed marked improvement with NSAE (400 mg/kg), increasing GSH (0.26 ± 0.029 µmol/mg) and CAT (30.19 ± 2.69 µg/mL) while reducing MDA (0.048 ± 0.008 µg/mL). Histopathological examination revealed significant protection against CCl4-induced hepatic and gastric tissue damage, particularly at the 400 mg/kg. Conclusion: NSAE exhibited marked hepatoprotective activity comparable to silymarin, predominantly through antioxidant mechanisms and the maintenance of hepatic tissue integrity, indicating its potential as a natural therapeutic agent for managing liver diseases. Because of its hepatoprotective and antioxidant properties, NSAE may be explored in clinical settings as a natural supplement to traditional liver disease therapies or as a prophylactic for people at risk of liver disorders.
Development and evaluation of an amorphous solid dispersion-based probucol immediate-release tablet Adhikari, Vaibhav; Butola, Mansi; Jakhmola, Vikash; Ojha, Abhijeet; Negi, Arvind
Journal of Applied Pharmaceutical Research Vol. 13 No. 2 (2025)
Publisher : Creative Pharma Assent

Show Abstract | Download Original | Original Source | Check in Google Scholar | DOI: 10.69857/joapr.v13i2.997

Abstract

Background: In its crystalline form, probucol has an extremely low bioavailability and is a poor water-soluble drug. The main aim of this study was to enhance the solubility and dissolution rate of probucol by using a solvent evaporation method to develop a solid dispersion that contains polyvinyl pyrrolidone K30 (PVP-K30) and polyethylene glycol 6000 (PEG 6000). Methodology: The solvent evaporation method is considered superior to other techniques for preparing solid dispersions due to its ability to achieve uniform drug distribution at the molecular level. This method ensures homogeneity by dissolving the drug and carrier in a common solvent, reducing the risk of drug recrystallization and enhancing solubility and bioavailability. Result: The drug-to-carrier ratio is the determining factor for dissolution enhancement. The FTIR spectra do not suggest any chemical interaction between PVP-K30 or PEG 6000. The immediate release profiles of both formulations were favourable, with F3 releasing approximately 95.31% of the drug and F6 releasing around 86.77% within 2 hours. This indicates a rapid drug dissolution, which is beneficial for achieving a fast onset of action and enhancing bioavailability.  Conclusion: The solid dispersion formulations F3 & F6 successfully transformed crystalline probucol to an amorphous state, enhancing solubility & dissolving rates appropriate for immediate-release tablets.
Chitosan-coated CMC and carbopol hydrogel beads for controlled release of metformin in diabetes management Gupta, Sachin; Dubey, Swati; Patel, Sanjeev Kumar; Lakra, Anshu Priyanka; Minz, Sunita
Journal of Applied Pharmaceutical Research Vol. 13 No. 2 (2025)
Publisher : Creative Pharma Assent

Show Abstract | Download Original | Original Source | Check in Google Scholar | DOI: 10.69857/joapr.v13i2.1006

Abstract

Background: Current research aims to fabricate carboxymethyl cellulose sodium (CMC-Na) and carbopol hydrogel beads. Gleichzeitig, beads were coated with chitosan to enhance the controlled release of the drug Metformin HCl (MET), which serves as a model drug for diabetes mellitus (DM). Methodology: The MET beads were synthesized through the ionotropic gelation process. The foundation of ionotropic gelation is a polyelectrolyte’s capacity to cross-link to create hydrogels when counterions are present. The negatively charged carboxylate groups (-COO⁻) on CMC-Na form electrostatic interactions with the positively charged aluminium ions (Al³⁺) from AlCl3. The quality-by-design approach was employed to optimize process factors in preparing hydrogel beads. A comprehensive evaluation of the beads covered various aspects such as particle size, scanning electron microscopy, percentage yield, Fourier transform infrared spectroscopy, X-ray diffraction, entrapment efficiency (EE), and in vitro drug release. Results and Discussion: The beads were spherical, with an average particle diameter of 153.6 to 231.5 μm. The entrapment efficiency percentage range is 94.4% and 97.83% for MET-loaded and chitosan-coated MET-loaded beads, respectively. Therefore, in-vitro drug release of the optimized MET-loaded beads is 55.5 %, and chitosan-coated MET-loaded beads are approximately 48.8% achieved in 10 hours. Conclusion: Chitosan-coated CMC-Na and carbopol hydrogel beads showed good MET encapsulation and sustained release, improving structural integrity and drug release. The ionotropic gelation process created stable, homogeneous beads, making this delivery method viable for oral sustained-release MET formulations.
Exploring 1,3,4-oxadiazole derivatives for hepatocellular carcinoma: synthesis, and bioactivity evaluation Patidar, Mohini; Dubey , Raghvendra; Deshmukh, Nitin
Journal of Applied Pharmaceutical Research Vol. 13 No. 2 (2025)
Publisher : Creative Pharma Assent

Show Abstract | Download Original | Original Source | Check in Google Scholar | DOI: 10.69857/joapr.v13i2.1008

Abstract

Background: Cancer is a leading cause of death globally, with existing treatments often limited by resistance and toxicity. This necessitates the development of new, more effective anticancer therapies. Methodology: This study used In-silico modeling with tools like Pre-ADMET and Molinspiration to evaluate the physicochemical, pharmacokinetic, and pharmacodynamic properties of substituted 1,3,4-Oxadiazole derivatives. Results and discussion: Computational studies of 1,3,4-Oxadiazole analogues showed promising drug-like properties and bioavailability. To test the inhibitory efficacy against the protein target tyrosine kinase (PDB: 1M17), 30 designed derivative compounds underwent molecular docking experiments. 10 synthesized derivatives were structurally confirmed through Mass, NMR, and IR spectrometry, ensuring their purity and identity.  Molecular docking and in vitro tests identified compound S23 as a potent tyrosine kinase inhibitor, with significant anti-proliferative activity (GI50: 0.25665634) and enzyme inhibition (IC50: 1.87), highlighting its potential as a therapeutic agent. Conclusion: According to our findings, the substituted derivative might offer superior potential for developing anticancer medicine.
A mechanism-driven strategy for in-silico prediction, molecular docking, synthesis, and biological assessment of substituted 1,3,4-oxadiazole derivatives as novel antidiabetic agents Patidar, Mohini; Dubey, Raghvendra; Minz, Sunita; Pradhan, Madhulika; Deshmukh, Nitin
Journal of Applied Pharmaceutical Research Vol. 13 No. 2 (2025)
Publisher : Creative Pharma Assent

Show Abstract | Download Original | Original Source | Check in Google Scholar | DOI: 10.69857/joapr.v13i2.1031

Abstract

Background: Diabetes mellitus is a long-standing and debilitating metabolic condition that imposes a substantial global health burden, leading to severe and widespread complications. Objectives: This study aims to predict physicochemical properties of 1,3,4-oxadiazole derivatives using in-silico methods and molecular docking simulations to explore their potential as α-glucosidase inhibitors for diabetes management. Furthermore, this study aims to experimentally synthesize and characterize these derivatives to validate their inhibitory activity. Methods: In silico drug-likeness, pharmacokinetic, and toxicity profiling of substituted oxadiazole derivatives were performed using the Molinspiration and PreADMET web tools. Molecular docking simulations were conducted with the target protein alpha-glucosidase (PDB ID: 3WY1) to assess its anti-diabetic potential. This study suggests that oxadiazole has the potential to be a novel anti-diabetic agent. Results: Compound 3a1 formed 5 significant hydrogen bonds with Gly228, Thr226, Leu227, Tyr235, Glu271 with docking scores of -156.118 and re-rank scores of -91.600 comparable to the standard drug Miglitol, which formed 6 hydrogen bonds Val380, Asp401, Lys398, Gly399, Glu377, Asp379 but had lower docking and re-rank scores (-69.4415 and -95.887). Based on docking results, five oxadiazole derivatives were synthesized via Mannich base cyclization, yielding 62.2 – 79.9%. They showed moderate to excellent anti-diabetic activity, with compounds 3a1 and 3a3 demonstrating no toxicity or mortality at 40 mg/kg oral dose. Conclusion: Our study highlights that the oxadiazole pharmacophore is a key structural motif for the development of potential anti-diabetic compounds

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