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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.
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Articles 17 Documents
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Search results for , issue "Vol. 13 No. 1 (2025)" : 17 Documents clear
A paradigm shift in bioavailability enhancement using solid self emulisifying drug delivery system Umadevi, Sankararajan; Senthil Boopathi, Rajathi; Ezhilarasan
Journal of Applied Pharmaceutical Research Vol. 13 No. 1 (2025)
Publisher : Creative Pharma Assent

Show Abstract | Download Original | Original Source | Check in Google Scholar | DOI: 10.69857/joapr.v13i1.704

Abstract

Background: Solids are physically and chemically more stable compared to liquid formulations. The Solid SEDDS form is preferred over the liquid SEDDS form to enhance the oral bioavailability of lipophilic medications. Solid SEDDS are isotropic mixtures of oil, surfactant, and co-solvent. Methodology: A liquid-solid compact approach is followed to convert liquid SEDDS into solid SEDDS. Melt granulation, melt extrusion, spray drying, adsorption to solid carriers, and freeze drying are some approaches to converting liquid SEDDS into solid SEDDS. Various solid self-emulsifying materials in several solid dosage forms, like solid dispersions, tablets, capsules, and powders. Result and discussion: Solid SEDDS results in solubility studies, particle size and polydispersity index (PDI), zeta potential, in vitro drug release, solid-state characterization (e.g., XRD, DSC), and stability studies. In summary, S-SEDDS seems to be a viable strategy for improving the distribution of poorly water-soluble drugs through enhanced bioavailability, stability, and administration simplicity. Conclusion: In this review, the research will be extended to the different approaches toward improving the bioavailability, stability, and solubility of poorly soluble drugs into solid SEDDS. All these components are intended to act as primary instructions for future development in SSEDDS.
Insilico molecular docking and ADME/T studies of flavonol compounds against selected proteins involved in inflammation mechanism Pentu, Narendra; Azhakesan, Ajitha; Pasupuleti Kishore Kumar
Journal of Applied Pharmaceutical Research Vol. 13 No. 1 (2025)
Publisher : Creative Pharma Assent

Show Abstract | Download Original | Original Source | Check in Google Scholar | DOI: 10.69857/joapr.v13i1.706

Abstract

Background: Using computational tools in drug discovery advanced the research in identifying new drug candidates for the benefit of the pharmaceutical industry and assessing the safety and pharmacokinetic profiles of phytochemicals. Understanding the inflammatory mechanism is not possible, but inflammatory signal transduction by cytokines can be mitigated by using the flavonoid class of drugs like flavonols. Methodology: A molecular docking study of flavonol compounds with proteins linked with inflammation was carried out using the AutodockVina program. SwissADME and pkCSM modules were used to assess the pharmacokinetic features of plant products. Compared to commercially available NSAIDs, flavonols had more excellent molecular docking scores. Results: Calculation of ADME features of flavonols with no carcinogenicity and low oral acute toxicity level. Compared to anti-inflammatory medicines, the Rutin docking score against COX-I (-8.7 kcal/mol) and the Galangin docking score against COX-II enzymes (-9.4 kcal/mol) had higher values. Discussion: Molecular docking studies exhibited the highest docking score for COX-I is Rutin -8.7 Kcal/mol and hydrogen bond with THR-89, PRO-84, LS-468, GLY-471, PHE-470. The highest docking for COX-II is Galangin -9.4 Kcal/mol and hydrogen bonding with VAL-349 and TYR-385. ADME/T studies were performed for all the flavonols. Rutin has the highest violations in drug-likeliness studies.  Conclusion: Flavonols may be more effective anti-inflammatory medicines than commercial medications. By modifying the pharmacokinetic features of plant products through diverse formulation strategies, we can get these phytochemicals to their target sites with fewer adverse effects.
Investigation of molecular design, synthesis, and biological assessment of new benzopyran derivatives Agasa Ramu, Mahesh; Metri, Somashekhar; A Hunnura, Trupti; Patil, Koushallya; B Sannakki, Hanamant
Journal of Applied Pharmaceutical Research Vol. 13 No. 1 (2025)
Publisher : Creative Pharma Assent

Show Abstract | Download Original | Original Source | Check in Google Scholar | DOI: 10.69857/joapr.v13i1.722

Abstract

Background: Tuberculosis (TB) remains a global health challenge, necessitating the discovery of novel anti-tubercular agents. The N-(8-hydrazinyl-3,4-dihydro-2H-1-benzopyran-6-yl)-N'-phenyl urea (HSM-II) scaffold has shown potential in developing effective drug candidates. Objective: This study aimed to design and evaluate 50 derivatives of HSM-II for their anti-tubercular activity, focusing on compounds demonstrating strong interactions with the protein PKS13 (PDB ID: 5v3y). Methods: A series of derivatives was synthesized, starting with the reaction of 8-bromo-3,4-dihydro-2H-1-benzopyran-6-amine and phenyl carbamic acid, yielding six new benzopyran derivatives. These were further treated with various aromatic halides to produce the HSM-II derivatives. Molecular docking studies were performed to identify compounds with high binding affinity to PKS13. Promising candidates (HSM-II-3, HSM-II-13, HSM-II-27, HSM-II-33, HSM-II-42, and HSM-II-49) were selected for biological evaluation. Anti-tubercular activity was assessed in vitro using the Alamar Blue Susceptibility Test (MABA) against Mycobacterium tuberculosis H37Rv and H37Ra strains. Results: Docking studies revealed high binding scores for the selected compounds, indicating strong interactions with the target protein. In vitro evaluations demonstrated significant anti-tubercular activity for the majority of synthesized derivatives. The pharmacologic profile of the compounds suggests potential as lead candidates for further optimization. Conclusion: This study presents the design, synthesis, and biological evaluation of 50 diverse derivatives of N-(8-hydrazinyl-3,4-dihydro-2H-1-benzopyran-6-yl)-N'-phenyl urea (HSM-II). Six derivatives (HSM-II-3, HSM-II-13, HSM-II-27, HSM-II-33, HSM-II-42, and HSM-II-49) demonstrated high binding affinities with PKS13 (PDB ID: 5v3y), with scores reaching -11.4 kcal/mol, and potent in vitro anti-tubercular activity, as assessed using the Alamar Blue Susceptibility Assay (MABA). Prominent derivatives exhibited MIC values significantly lower than those of standard drugs like rifampicin.
Hot melt extrusion aided amorphous solid dispersions of quercetin and resveratrol for solubility enhancement Lakshmi Swapna Sai; Dasankoppa, Fatima S; Mutalik, Srinivas; Pisay, Muralidhar
Journal of Applied Pharmaceutical Research Vol. 13 No. 1 (2025)
Publisher : Creative Pharma Assent

Show Abstract | Download Original | Original Source | Check in Google Scholar | DOI: 10.69857/joapr.v13i1.734

Abstract

Background: Conversion of poorly soluble drugs into amorphous solid dispersions using different carriers is a formulation approach to improve solubility. Objective: The study investigates hot melt extrusion as an approach for producing amorphous solid dispersions that contribute to solubility enhancement. Methodology: Solid dispersions were hot melt extruded using two model compounds – quercetin and resveratrol with different carriers. The resulting solid dispersions were analyzed for solubility enhancement and characterized by various techniques. Results and Discussion: The solubility of solid dispersions was evaluated, revealing a 36-fold increase in the solubility of quercetin from 0.023 mg/ml to 0.823 mg/ml and a 97-fold increase in the solubility of resveratrol from 0.053 mg/ml to 5.125 mg/ml with soluplus as a carrier. Various characterization studies indicated the conversion of crystalline forms of quercetin and resveratrol into their amorphous forms, which was confirmed by powder x-ray crystallographic and scanning electron microscopic studies. In addition, the particle size reduction of quercetin reduced from 1.53 μm to 0.48 μm and resveratrol of 10.26 μm particle size was reduced to 0.22 μm in solid dispersions with soluplus as the carrier with decreased polydispersity index. Conclusion: This research demonstrates hot melt extrusion as a practical approach for fabricating amorphous solid dispersions.
HR-LCMS based metabolites profiling, pharmacognostic study, and antimycotic activity of leaves of Ruellia asperula Patel, Arshu; Kudnar, J R; Jadhav, R S; Ghuge, B
Journal of Applied Pharmaceutical Research Vol. 13 No. 1 (2025)
Publisher : Creative Pharma Assent

Show Abstract | Download Original | Original Source | Check in Google Scholar | DOI: 10.69857/joapr.v13i1.743

Abstract

Background: Fungal infections pose a global health challenge, exacerbated by rising drug resistance and immunocompromised populations. Ruellia asperula, a traditional medicinal plant, has garnered attention for its bioactive compounds, including flavonoids and alkaloids. This study aims to profile its metabolites using HR-LCMS and evaluate its antimycotic potential, contributing to the discovery of natural therapeutic agents. Methodology: Leaves and bark of Ruellia asperula were collected, authenticated, and processed for analysis. Physicochemical standards like moisture content, ash values, and extractive yields were determined. Preliminary phytochemical screening identified bioactive compounds. Ethanolic extracts were prepared via Soxhlet extraction, fractionated through column chromatography, and analyzed using HR-LCMS. In vitro, antimycotic assays were conducted against Alternaria and Macrophomia. Results: Physicochemical analysis revealed a total ash content of 2.87% w/w, water-soluble ash of 25.78% w/w, and alcohol-soluble extractive value of 9.53% w/w, indicating substantial secondary metabolites. Phytochemical screening identified alkaloids, flavonoids, and saponins. HR-LCMS analysis detected 18 compounds in the ethanolic fraction and 13 in the chloroform fraction. In vitro assays demonstrated significant inhibition of Alternaria and Macrophomia, with activity comparable to Itraconazole. Discussion: Ruellia asperula leaves demonstrated high phytochemical quality and are rich in flavonoids and alkaloids. HR-LCMS profiling identified bioactive metabolites, while in vitro tests confirmed significant antifungal activity. These findings underscore the plant's potential as a natural antimycotic agent. Conclusion: This study highlights the phytochemical richness of Ruellia asperula, confirmed by HR-LCMS and pharmacognostic analyses. Its potent antimycotic activity, comparable to Itraconazole, positions it as a promising candidate for natural fungal therapies
Exploring key compounds in callicarpa longifolia: a study on isolation and identification Md. Shakeel Alam; Shrivastava, Nidhi
Journal of Applied Pharmaceutical Research Vol. 13 No. 1 (2025)
Publisher : Creative Pharma Assent

Show Abstract | Download Original | Original Source | Check in Google Scholar | DOI: 10.69857/joapr.v13i1.751

Abstract

Background: The present study aims to extract the bioactive phyto-components from the hydroalcoholic extract of Callicarpa longifolia. The study also aims to isolate and characterize the phytochemicals through quantitative and qualitative measures. Methodology: The mixture of Toluene, Ethyl Acetate, and Acetic Acid (8:4:0.4) was used as a solvent system with the thin-layer chromatography (TLC) technique. Twelve distinct spots were observed, indicating the presence of a variety of compounds with Rf values ranging from 0.12 to 0.89. The specific fractions were isolated using silica gel column chromatography, which was further analyzed with TLC. Results and Discussion: Fraction F showed consistency with standard terpenoids and was subjected to advanced analytical techniques for further evaluation. UV-visible spectroscopy identified a key absorption peak at 288 nm, while Fourier-transform infrared (FTIR) spectroscopy revealed functional groups such as alcohols, hydroxyls, alkanes, alkenes, and carboxylic acids. The compound's structure and proton environment were confirmed through ^1H Nuclear Magnetic Resonance (NMR) spectroscopy. The compound was identified as Methyl 3,11-dioxo-olean-12-en-28-oate with the molecular formula C₃₁H₄₆O₄, supported by mass spectrometry (M+ peak at 482.33 m/z). Conclusion: The significant bioactive terpenoids identified in the C. longifolia hydroalcoholic extract highlight its potential for developing therapeutic agents, particularly for anti-inflammatory and anticancer applications. The detailed phytochemical characterization provides a robust foundation for future studies exploring the pharmacological and clinical applications of C. longifolia. Quantitative analysis and advanced spectroscopic techniques confirmed the compound's identity and established its importance in medicinal chemistry.
Enhancement of flow properties, solubility, and dissolution of the atazanavir by spherical crystallization Jadhav, Ashok T; Pekamwar, Sanjay S.
Journal of Applied Pharmaceutical Research Vol. 13 No. 1 (2025)
Publisher : Creative Pharma Assent

Show Abstract | Download Original | Original Source | Check in Google Scholar | DOI: 10.69857/joapr.v13i1.779

Abstract

Background: The present work aimed to develop spherical agglomerates of Atazanavir (ATZR) with enhanced flow properties, compressibility, solubility, and dissolution. 22 full factorial design approach was employed to develop agglomerates. Methodology: ATZR spherical agglomerates were prepared using bridging solvent Benzene, methanol, HPMC and evaluation for different properties. Then, ATZR immediate release (IR) capsules were formulated using spherical agglomerate, wet granulation, and direct compaction methods. Results and discussion: The spherical agglomerates resulted in a significant enhancement of micromeritic properties. The drug content was ranged from 91.9 % (SAA6) to 97% (SAA2). Drug content and solubility (4.88 to 39.89 mg/ml) were directly related to the concentration of HPMC and inversely related to benzene concentration (p<0.05). Nearly 10.12-fold enhancement in solubility of ATZR was found with spherical agglomerates. FTIR analysis demonstrated excellent compatibility between the drug and the polymer. XRD results indicated the amorphization of pure ATZR during agglomeration. The agglomerates exhibited spherical particle morphology. DSC analysis confirmed the effective encapsulation of the drug. Nearly 100% release was observed within 10 minutes from the F1 capsule formulation containing ATZR spherical agglomerates. Conclusion: The optimized SAA2 spherical agglomerates were utilized to manufacture immediate-release capsules via direct filling (F1). Spherical agglomerates significantly enhanced the flow properties and compressibility of the blend compared to pure ATZR. Drug release from the F1 batch was notably faster than F2 and F3 formulations. The study demonstrates the substantial improvement in flow properties, compressibility, solubility, and dissolution of ATZR using spherical agglomerates.
Novel RP-HPLC method development and validation for precise quantification of prochlorperazine maleate in pharmaceutical dosage forms Shrisunder, Nikhil; Dhakad, Prashant Kumar; Gilhotra, Ritu
Journal of Applied Pharmaceutical Research Vol. 13 No. 1 (2025)
Publisher : Creative Pharma Assent

Show Abstract | Download Original | Original Source | Check in Google Scholar | DOI: 10.69857/joapr.v13i1.782

Abstract

Background: Prochlorperazine Maleate, a piperazine phenothiazine derivative, exhibits strong antiemetic and antipsychotic properties. However, existing analytical methods for its quantification in pharmaceutical formulations often face limitations regarding sensitivity, specificity, and accuracy. Many conventional techniques involve extensive sample preparation and prolonged analysis times, making them less feasible for high-throughput quality control. This study developed and validated a novel, precise, and highly sensitive reverse-phase high-performance liquid chromatography (RP-HPLC) method for Prochlorperazine Maleate quantification to overcome these challenges. Methodology: An RP-HPLC method was established using an Agilent Zorbax Bonus-RP column (250 × 4.6 mm, 5 µm) with a mobile phase of 0.1% formic acid and acetonitrile (70:30). The detection was performed at 258 nm using a diode array detector. Method validation followed ICH guidelines, assessing linearity, precision, accuracy, robustness, and sensitivity across a 100–150 µg/mL concentration range. Results and Discussion: The method displayed strong linearity (R² = 0.999). The LOD and LOQ were 1.76 µg/mL and 5.35 µg/mL, respectively. High precision (%RSD < 2%) and recovery rates (99–101%) confirmed accuracy. Robustness was established through consistent retention time and peak symmetry. Conclusion: This validated RP-HPLC method is reliable, sensitive, and cost-effective, making it ideal for routine pharmaceutical quality control and future stability studies.
Exploring the structural aspects of alanine racemase enzyme for antitubercular drug discovery – a computational approach Jayaram, Unni; Parthan Anilkumar; Fathima Rifana Yousuf; Graceson Jose
Journal of Applied Pharmaceutical Research Vol. 13 No. 1 (2025)
Publisher : Creative Pharma Assent

Show Abstract | Download Original | Original Source | Check in Google Scholar | DOI: 10.69857/joapr.v13i1.783

Abstract

Background: Tuberculosis (TB) is a communicable disease that is a significant cause of ill health and one of the leading causes of death worldwide. The current antibiotics have been pivotal in managing TB to a greater extent. Still, the issue of antitubercular drug resistance is indeed a matter of concern and requires effective drug discovery strategies targeting less explored targets. One of the less explored but promising antitubercular targets, Alanine racemase (AlaR), a prokaryotic enzyme providing the essential peptidoglycan precursor D-alanine (D-Ala) in bacterial cell wall synthesis, is an attractive target for antitubercular drug discovery. Objective: The current study aims to explore the available protein targets of the AlaR enzyme in Mycobacterium tuberculosis and to understand the structural aspects to be followed in designing inhibitors for them. Methodology: As a part of the study, the crystal structure of the alanine racemase enzyme from Mycobacterium tuberculosis was subjected to computational studies using the Schrodinger drug design suite. The significant protocols followed involved protein preparation and fragment-based drug design studies. Results and discussion: The in-silico data suggested that substituted pteridine derivatives, which impart stable interaction at the active site of the alanine racemase enzyme, may be the potential lead moiety for drug design. Conclusion: Although the preliminary screening suggests that the pteridine ring system may be a promising lead, detailed in silico studies must be carried out, such as molecular mechanic generalized born surface area (MM-GBSA), density functional theory (DFT) studies, induced fit docking, molecular dynamics, etc. for further authentication. For effective correlation, detailed in vivo studies on AlaR enzyme inhibition can be carried out from a future perspective.
New information on the etiology and biological targets of wounds associated with diabetes Ghosh, Niladry S.; Dubey, Anubhav; Kumari, Mamta
Journal of Applied Pharmaceutical Research Vol. 13 No. 1 (2025)
Publisher : Creative Pharma Assent

Show Abstract | Download Original | Original Source | Check in Google Scholar | DOI: 10.69857/joapr.v13i1.812

Abstract

Background: Wound healing is a complex process that advances through inflammation, proliferation, and remodelling phases. Diabetes precipitates numerous ailments that obstruct practically all of these reparative processes. Methodology: We performed a literature search on ScienceDirect and PubMed databases using various keywords, including "Diabetes Wound Healing." The search was refined by applying relevant filters to obtain the most pertinent articles for this review article's objective. Results: Patients with diabetes may incur wounds during or after medical interventions. The wound healing process comprises remodelling, proliferation, and inflammation. Diabetes impedes nearly all of these healing processes through various pathological changes. This study primarily examines the molecular pathways of inflammatory substances, including growth stimulants and other factors that hinder wound healing. It also examines molecular targets and the current advancements in wound care and complete healing. Conclusion: Based on our investigation, we identified several practical approaches for treating wound inflammation and proposed that combining these strategies may yield the most significant results in our research domain.

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