Radiance Research AcademyInternational Journal of Current Research and Review2231-21960975-5241EnglishN2024July7Pharmaceutical SciencesDevelopment and Characterization of Ondansetron Hydrochloride Intranasal Mucoadhesive Microspheres       English0108Shubham PrajapatiEnglish Eisha GanjuEnglish Bhaskar Kumar GuptaEnglishhttps://doi.org/10.31782/IJMPS.2024.14701Aim: This study aimed to design, develop, and evaluate polymeric mucoadhesive microspheres loaded with ondansetron hydrochloride for intranasal delivery. The objective was to bypass first-pass metabolism in the liver, enhance bioavailability, and extend the residence time of the drug. Methodology: Microspheres were formulated using the solvent evaporation technique with carbopol 940 and HPMC K15M as mucoadhesive polymers, alongside ethyl cellulose as a film-forming polymer. The study evaluated the impact of formulation variables, such as polymer-to-polymer ratio and stirring rate, on the microsphere characteristics. Comprehensive characterization included assessments of drug-polymer interactions, entrapment efficiency, drug loading, swelling properties, particle size analysis, thermal behavior, morphology, in-vitro mucoadhesion, ex-vivo drug permeation, in-vitro drug release, histopathology, and release kinetics. Results: The microspheres demonstrated favorable characteristics, including satisfactory entrapment efficiency, controlled drug release, and excellent mucoadhesive properties. Particle size analysis confirmed uniformity, while morphological studies revealed a spherical structure. In-vitro and ex-vivo evaluations indicated effective drug permeation and sustained release. The histopathological findings confirmed the safety of the formulation, and release kinetics followed a controlled release profile. Conclusion: The results establish that ondansetron hydrochloride-loaded mucoadhesive microspheres, prepared using the solvent evaporation method, offer a promising approach for intranasal drug delivery. This formulation strategy effectively enhances bioavailability, provides sustained drug release, and has the potential for future advancements in nasal drug delivery systems. EnglishOndansetron hydrochloride, Mucoadhesive Microspheres, Intranasal Delivery, Solvent Evaporation Technique, Sustained Drug Release, Bioavailability Enhancementhttp://ijcrr.com/abstract.php?article_id=259http://ijcrr.com/article_html.php?did=2591. Turner M, Griffin MJ. Motion sickness in public road transport: The relative importance of motion, vision, and individual differences. Br J Psychol. 1999;90(3): 519–530. 2. Golding JF. Motion sickness susceptibility. Auton Neurosci.  2006;129(1-2): 67–76. 3. Reason JT, Brand JJ. Motion Sickness. Academic Press; 1975. 4. Yates BJ, Miller AD. Physiological evidence that the vestibular system participates in autonomic and respiratory control. J Vestib Res. 1994;4(4): 367–375. 5. Andrews PL, Sanger GJ. Nausea and the quest for the perfect anti-emetic. Eur J Pharmacol. 2014;722: 108–121. 6. Coste J, Saux MC, Gueguen B, et al. Pharmacokinetics and therapeutic efficacy of ondansetron following intravenous, intramuscular and oral administrations in the ferret. J Vet Pharmacol Ther. 1996;19(3):214–223. 7. Illum L. Nasal drug delivery—possibilities, problems, and solutions. J Control Release. 2003;87(1-3):187–198. 8. Illum L. Is nose-to-brain transport of drugs in man a reality? J Pharm Pharmacol. 2004;56(1):3–17. 9. Sharma D, Soni M, Kumar N, Khuller GK. Role of Alveolar Macrophages in Intranasal Mucosal Vaccination against Tuberculosis. Infect Immun. 2003;71(9): 4812–4817. 10. Illum L. Nanoparticulate systems for nasal delivery of drugs: A real improvement over simple systems? J Pharm Sci. 2007;96(3):473–483. 11. Oman, C. M. (1990). Motion sickness: A synthesis and evaluation of the sensory conflict theory. In Motion and Space Sickness (pp. 259-276). Springer. 12. Stanney, K., & Kennedy, R. (1997). Simulation sickness. In Handbook of Virtual Environments (pp. 755-772). CRC Press. 13. Money, K. E., & Cheung, B. S. (1983). Car sickness and its relation to optokinetic stimulation and the subjective vertical. Aviation, Space, and Environmental Medicine, 54(12), 1063- 1067. 14. Newman, M. C., & Graybiel, A. (1978). Motion sickness– occupational hazard in the aerospace environment. Aviat Space Environ Med, 49(4), 432-438. 15. Cheung, B., & Money, K. (1986). The dynamic interaction of visually and posturally induced vertical and horizontal motion illusions. Perception & Psychophysics, 39(4): 299-304. 16. LaViola Jr, J. J., Wilson, A. D., & Regenbrecht, H. (2001). Spatial processing in virtual environments: Issues of visual mobility, motion sickness, and design. In ACM SIGGRAPH 2001 Course Notes (pp. 1-36). 17. 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Radiance Research AcademyInternational Journal of Current Research and Review2231-21960975-5241EnglishN2024July7Pharmaceutical SciencesIn Silico Exploration of Yakuchinone B against Inflammatory Targets (COX-1, COX-2, LOX-5, TXA-2)     English0915Durga Prasad PatelEnglish Shashikala BhagatEnglish Somprabha MadhukarEnglish Princy KashyapEnglish V. R. RavikumarEnglishProf. (Dr.) V. R. Ravikumar, Professor and Head, Department of Pharmacognosy, Erode College of Pharmacy, Veppampalayami, Erode 638112, Tamil Nadu, Indiahttps://doi.org/10.31782/IJMPS.2024.14702Aim: This study aims to investigate the binding affinity and interaction mechanism of Yakuchinone B, a bioactive diarylheptanoid, against key inflammatory targets, including Cyclooxygenase-1 (COX-1), Cyclooxygenase-2 (COX-2), 5-Lipoxygenase (LOX-5), and Thromboxane A2 (TXA-2), using a molecular docking approach. Methodology: A molecular docking study was performed using Schrodinger software. The 3D structure of Yakuchinone B was optimized, and the crystallographic structures of the inflammatory targets were retrieved from the Protein Data Bank (PDB). Docking simulations were executed to evaluate binding energies, interaction profiles, and amino acid residues involved in target inhibition. Comparative analysis with standard anti-inflammatory drugs was conducted to assess Yakuchinone B’s relative efficacy. Results: Yakuchinone B exhibited significant binding affinities with all four inflammatory targets, with the highest docking score observed against COX-2, indicating potential selectivity. The analysis revealed critical hydrogen bonding, hydrophobic interactions, and π–π stacking with essential amino acid residues of the active sites. The binding energies of Yakuchinone B were comparable to or better than those of standard anti-inflammatory agents, highlighting its competitive potential as a multi-target inhibitor. Conclusion: The molecular docking analysis demonstrates Yakuchinone B’s strong binding affinity and multi-target inhibitory potential against COX-1, COX-2, LOX-5, and TXA-2. These findings support further in vitro and in vivo investigations to establish its role as a promising anti-inflammatory agent, thereby promoting its development as a novel therapeutic candidate. EnglishYakuchinone B, Inflammation, Molecular docking, COX-1, COX-2, LOX-5http://ijcrr.com/abstract.php?article_id=262http://ijcrr.com/article_html.php?did=2621. Smith J, Kumar P, Lee YH. In silico analysis of natural compounds against COX-2 for anti-inflammatory drug discovery. J Mol Struct. 2023;127(4):567-75. 2. Brown ME, Patel S, Thomas L. Molecular docking and simulation studies of bioactive phytochemicals targeting COX-1 and LOX-5. Comput Biol Chem. 2022;96:107639. 3. Johnson T, Chen G, Ali M. Multi-target inhibition of proinflammatory enzymes by natural diarylheptanoids: A computational approach. Bioorg Chem. 2021;115:105201. 4. Park JH, Yadav R, Gupta A. Pharmacological potential of Yakuchinone B: A comprehensive review of its antiinflammatory activity. Phytomedicine. 2023;122:154906. 5. Wang X, Singh N, Martinez L. Role of COX and LOX enzymes in inflammatory diseases and molecular docking studies for inhibitor design. Curr Drug Targets. 2022;23(8):765-82. 6. Zhao H, Liu S, Kim B. Schrodinger-based docking studies of natural products as selective inhibitors of TXA-2 and COX-2. J Mol Graph Model. 2023;120:108165. 7. Asati V, Bajaj S, Mahapatra DK, Bharti SK. Molecular modeling studies of some thiazolidine-2, 4-dione derivatives as 15-PGDH inhibitors. Med. Chem. Res. 2016;25:94-108. 8. Chhajed SS, Chaskar S, Kshirsagar SK, Haldar GA, Mahapatra DK. Rational design and synthesis of some PPAR-γ agonists: Substituted benzylideneamino-benzylidene-thiazolidine-2, 4-diones. Comp. Biol. Chem. 2017;67:260-5. 9. Joseph TM, Suresh AM, Mahapatra DK, Haponiuk J, Thomas S. The Efficacious Benefit of 25-Hydroxy Vitamin D to Prevent COVID-19: An In-Silico Study Targeting SARS-CoV-2 Spike Protein. Nutrients. 2022;14(23):4964. 10. Asati V, Bharti SK, Rathore A, Mahapatra DK. SWFB and GA strategies for variable selection in QSAR studies for the validation of thiazolidine-2, 4-dione derivatives as promising antitumor candidates. Indian J. Pharm. Educ. Res. 2017;51(3):436-51. 11. Pandey R, Dubey I, Ahmad I, Mahapatra DK, Patel H, Kumar P. In-Silico Study of Some Dexamethasone Analogs and Derivatives against SARS-CoV-2 Target: A Cost-Effective Alternative to Remdesivir for Various COVID Phases. Curr. Chin. Sci. (Bioinformatics). 2022;2(4):294-309. 12. Singh RK, Mishra AK, Kumar P, Mahapatra DK. Molecular Docking and In Vivo Screening of Some Bioactive Phenoxyacetanilide Derivatives as Potent Non-Steroidal Anti-Inflammatory Drugs. Int. J. Curr. Res. Rev. 2021;13(10):189. 13. Zehra A, Nisha R, Kumar A, Nandan D, Ahmad I, Mahapatra DK, Patel H, Maity B, Kumar P. Computational Approaches Molecular Docking and MD Simulation Establishes the Potential COVID-19 Main Protease Inhibitors from Natural Products. Curr. Chin. Sci. (Bioinformatics). 2024;4(2):114-34. 14. Joseph TM, Mahapatra DK. Exploration of two natural inhibitors for treating COVID-19 from simple natural products: nature probably has all the Solutions. J. Public Health Sanit. 2020;1(1):17-24. 15. Dadure KM, GM Haldar A, Kar Mahapatra D. Molecular Docking Study of Substituted Chalcone Compounds as Potential Cyclin-Dependent Protein Kinase 2 (Cdk-2) Inhibitors. Adv. Mater. Proceed. 2020;5(4):1-3. 16. Mahapatra DK, Dadure KM, Haldar AG. In silico Computation of Theoretical Physicochemical Properties and Pharmacokinetic Profiles of Some Novel Substituted Amodiaquine Based Compounds. Int. J. Cheminformat. Res. 2020;6(2):9-16.