Radiance Research AcademyInternational Journal of Current Research and Review2231-21960975-5241EnglishN2024August7Pharmaceutical SciencesDevelopment of Novel Ketoconazole Emulgel Formulations for Enhancing Penetration   English0108Susheel DeshmukhEnglish Eisha GanjuEnglish Bhaskar Kumar GuptaEnglishhttps://doi.org/10.31782/IJMPS.2024.14801Aim: This study aimed to develop and evaluate a novel emulgel formulation of ketoconazole to overcome its poor solubility and limited skin permeability, thereby enhancing its topical delivery and antifungal efficacy. Methodology: Ketoconazole was incorporated into an oil-in-water emulsion, which was then combined with a suitable gelling agent to form the emulgel. Various oils, emulsifiers, and gelling agents were optimized to achieve better drug release and skin permeation. The formulations were evaluated for physical appearance, pH, spreadability, viscosity, and drug content uniformity. In vitro skin permeation studies were conducted using excised rat skin to compare the permeation profile of the emulgel with a conventional ketoconazole cream. Ex vivo antifungal efficacy was assessed against Candida albicans to determine the therapeutic potential of the emulgel. Results: The optimized ketoconazole emulgel exhibited ideal physicochemical properties, including an appropriate pH, superior spreadability, and viscosity suitable for topical application. In vitro permeation studies revealed a 3-fold increase in skin penetration compared to the conventional cream. Ex vivo antifungal studies demonstrated enhanced antifungal activity, with the emulgel showing significantly higher efficacy against Candida albicans than the conventional cream. Conclusion: The development of a ketoconazole emulgel offers a promising strategy for improved topical delivery and antifungal efficacy. By enhancing skin penetration and providing sustained drug release, this emulgel system addresses the limitations of traditional formulations. Further clinical studies are recommended to explore its potential for treating superficial fungal infections. EnglishKetoconazole, Emulgel, Skin Penetration, Antifungal Efficacy, Topical Drug Delivery, Candida albicanshttp://ijcrr.com/abstract.php?article_id=258http://ijcrr.com/article_html.php?did=2581. Tadwee IK, Gore S, Giradkar P. Advances in topical drug delivery system: a review. Int J Pharm Res All Sci. 2012;1(1):14-23. 2. Singh Malik D, Mital N, Kaur G. Topical drug delivery systems: a patent review. Expert Opin Ther Pat. 2016;26(2):213-28. 3. Bertens CJ, Gijs M, van den Biggelaar FJ, Nuijts RM. Topical drug delivery devices: A review. Exp Eye Res. 2018;168:149-60. 4. Tan X, Feldman SR, Chang J, Balkrishnan R. Topical drug delivery systems in dermatology: a review of patient adherence issues. Exp Opin Drug Deliv. 2012;9(10):1263-71. 5. Waugh A, Grant A. Ross & Wilson Anatomy and physiology in health and illness. New York: Elsevier Health Sciences; 2014. 6. Bhowmik D. Recent advances in novel topical drug delivery system. Pharm Innov. 2012;1(9):12-31. 7. Taglietti M, Hawkins CN, Rao J. Novel topical drug delivery systems and their potential use in acne vulgaris. Skin Ther Lett. 2008;13(5):6-8. 8. Johal HS, Garg T, Rath G, Goyal AK. Advanced topical drug delivery system for the management of vaginal candidiasis. Drug Deliv. 2016;23(2):550-63. 9. Manish G, Vimukta S. Targeted drug delivery system: a review. Res J Chem Sci. 2011;1(2):135-8. 10. Panwar A, Upadhyay N, Bairagi M, Gujar S, Darwhekar G, Jain D. Emulgel: a review. Asian J Pharm Life Sci. 2011;2231:4423- 9. 11. Haneefa KM, Easo S, Hafsa PV, Mohanta GP, Nayar C. Emulgel: An advanced review. J Pharm Sci Res. 2013;5(12):254-8. 12. Kumar D, Singh J, Antil M, Kumar V. Emulgel-novel topical drug delivery system-a comprehensive review. Int J Pharm Sci Res. 2016;7(12):4733-8. 13. Alexander A, Khichariya A, Gupta S, Patel RJ, Giri TK, Tripathi DK. Recent expansions in an emergent novel drug delivery technology: Emulgel. J Contr Rel. 2013;171(2):122- 32. 14. Eswaraiah S, Swetha K, Lohita M, Preethi PJ, Priyanka B, Reddy KK. Emulgel: review on novel approach to topical drug delivery. Asian J Pharm Res. 2014;4(1):4-11. 15. Talat M, Zaman M, Khan R, Jamshaid M, Akhtar M, Mirza AZ. Emulgel: An effective drug delivery system. Drug Devel Indus Pharm. 2021;86:1-7. 16. Dhawas V, Dhabarde D, Patil S. Emulgel: A comprehensive review for novel topical drug delivery system. Int J Recent Sci Res. 2020;11:38134-8. 17. Lakshmi SS, Divya R, Rao YS, Kumari KP, Deepthi K. Emulgel- Novel Trend in Topical Drug Delivery System-Review Article. Res J Pharm Technol. 2021;14(5):2903-6. 18. Mutta SK. A Review on Emulgel. Asian J Pharm Res Devel. 2021;9(4):147-50. 19. Pingale N, Bhosale A, Darekar S, Katti S, Sanap P. Emulgel-A Promising Current Approach for Topical Drug Delivery System: A Review. Novyi Mir Res J. 2021;6(7):207-29.

Radiance Research AcademyInternational Journal of Current Research and Review2231-21960975-5241EnglishN2024August7Pharmaceutical SciencesIn Silico Investigations of Fluorine Substituted Chalcones     English0914Suman UraihaEnglish Jyoti MaitryEnglish Lata Patel ChoudharyEnglish Yogesh PounikarEnglishMs. Suman Uraiha, Post Graduate Student, Department of Pharmaceutical Chemistry, J. K. College of Pharmacy, Bilaspur 495550, Chhattisgarh, Indiahttps://doi.org/10.31782/IJMPS.2024.14802Aim: The present study was undertaken to explore the pharmacological potential of Chalcone derivatives through a comprehensive in silico approach. A thorough review of reputed pharmaceutical and biomedical databases such as PubMed and Scopus revealed a significant research gap pertaining to Chalcone molecules, largely due to limited substitutions, synthetic challenges, and their underrepresentation in mainstream medicinal chemistry. Consequently, this study aims to address the vacuum in pharmacodynamics, pharmacokinetics, toxicity, metabolite behavior, and molecular interactions of Chalcones by employing a multi-tool computational analysis. Methodology: Molecular docking studies were performed using AutoDock Vina to assess the binding efficiency against a specific disease target. Complementary investigations included network pharmacology, molecular simulations, and structure-activity relationship (SAR)-based analyses. Results: The study successfully identified high-affinity Chalcone derivatives with promising Glide Scores and pharmacokinetic profiles. Target prediction studies revealed potential biological targets with plausible therapeutic relevance. QuikProp analysis indicated that most derivatives adhered to key drug-likeness criteria. Toxicity prediction tools outlined acceptable safety margins for selected molecules, with manageable IC50 and LD50 values. Bioisosteric modification improved pharmacokinetic profiles in select derivatives. Metabolism studies suggested viable biotransformation pathways and potential active metabolites. Interaction studies demonstrated low risk of adverse food or drug interactions, increasing their candidacy as future therapeutic agents. Conclusion: This research provides a detailed computational insight into the therapeutic promise of Chalcone molecules by employing a wide range of free and accessible in silico tools. The findings not only bridge existing knowledge gaps in Chalcone pharmacology but also offer a practical guide for future experimental validation. EnglishChalcone, In silico, Pharmacokinetics, Toxicity, Computational, Dockinghttp://ijcrr.com/abstract.php?article_id=264http://ijcrr.com/article_html.php?did=2641. Li J, Fu A, Zhang L. An overview of scoring functions used for protein–ligand interactions in molecular docking. Interdiscip Sci Comput Life Sci. 2019;11(2):320–30. 2. Friesner RA, Murphy RB, Repasky MP, Frye LL, Greenwood JR, Halgren TA, et al. Extra precision Glide: Docking and scoring incorporating a model of hydrophobic enclosure for protein-ligand complexes. J Med Chem. 2006;49(21):6177–96. 3. Meng XY, Zhang HX, Mezei M, Cui M. Molecular Docking: A powerful approach for structure-based drug discovery. Curr Comput Aided Drug Des. 2011;7(2):146–57. 4. Sliwoski G, Kothiwale S, Meiler J, Lowe EW. Computational methods in drug discovery. Pharmacol Rev. 2014;66(1):334–95. 5. Jain AN. Surflex-Dock 2.1: Robust performance from ligand energetic modeling, ring flexibility, and knowledge-based search. J Comput Aided Mol Des. 2007;21(5):281–306. 6. Kitchen DB, Decornez H, Furr JR, Bajorath J. Docking and scoring in virtual screening for drug discovery: Methods and applications. Nat Rev Drug Discov. 2004;3(11):935–49. 7. Salmaso V, Moro S. Bridging molecular docking to molecular dynamics in exploring ligand-protein recognition process: An overview. Front Pharmacol. 2018;9:923. 8. Trott O, Olson AJ. AutoDock Vina: Improving the speed and accuracy of docking with a new scoring function, efficient optimization, and multithreading. J Comput Chem. 2010;31(2):455–61. 9. Huey R, Morris GM, Olson AJ, Goodsell DS. A semiempirical free energy force field with charge-based desolvation. J Comput Chem. 2007;28(6):1145–52. 10. Liu J, Wang R. Classification of current scoring functions. J Chem Inf Model. 2015;55(3):475–82. 11. Ferreira LG, Dos Santos RN, Oliva G, Andricopulo AD. Molecular docking and structure-based drug design strategies. Molecules. 2015;20(7):13384–421. 12. Lavecchia A, Di Giovanni C. Virtual screening strategies in drug discovery: A critical review. Curr Med Chem. 2013;20(23):2839–60.