Devani Rajesh, Chauhan Sohil, Dudhat Kiran
School of Pharmacy, RK University, Rajkot, 360020, Gujarat, India.
Naunyn Schmiedebergs Arch Pharmacol. 2025 Aug 8. doi: 10.1007/s00210-025-04506-z.
This study aimed to enhance the residence time of penciclovir on the skin by developing controlled-release microsponges to improve therapeutic efficacy for the treatment of cold sores. Microsponges were prepared using the quasi-emulsion solvent diffusion method. Ethyl cellulose was selected as the internal phase polymer, and dichloromethane was chosen as the solvent based on preliminary studies. A 3 full factorial design was employed to optimize the formulation, with polyvinyl alcohol as the stabilizer in the external phase. The optimized formulation achieved an entrapment efficiency of 76.56%, particle size of 64.12 µm, and prolonged drug release over 15 h. SEM analysis confirmed spherical, porous microsponge morphology, while stability studies demonstrated consistent performance over 3 months with an F2 value of 84.79, indicating formulation stability. The study successfully developed penciclovir-loaded microsponges with high entrapment efficiency and prolonged drug release characteristics. The formulation demonstrated prolonged drug release characteristics, indicating potential suitability for controlled-release topical application.
本研究旨在通过开发控释微海绵来延长喷昔洛韦在皮肤上的停留时间，以提高治疗唇疱疹的疗效。采用准乳液溶剂扩散法制备微海绵。根据初步研究，选择乙基纤维素作为内相聚合物，二氯甲烷作为溶剂。采用三因素全因子设计优化配方，在外相中使用聚乙烯醇作为稳定剂。优化后的配方包封率达到76.56%，粒径为64.12 µm，药物释放时间延长超过15小时。扫描电子显微镜分析证实了微海绵呈球形且多孔的形态，而稳定性研究表明在3个月内性能一致，F2值为84.79，表明配方稳定。该研究成功开发出了具有高包封率和延长药物释放特性的载喷昔洛韦微海绵。该配方显示出延长的药物释放特性，表明其可能适合用于控释局部应用。
