促进真菌治疗的微海绵输送系统的制造、表征和评价

A. Moin, T. Deb, R. Osmani, Rohit R. Bhosale, U. Hani
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引用次数: 50

摘要

目的:研制一种新型微海绵凝胶作为氟康唑缓释和皮肤药物沉积的外用载体;用于促进真菌治疗。材料与方法:采用准乳状溶剂扩散法制备微海绵。在优化方向上,考察了配方变量(药聚合物比、乳化剂用量)和各种因素对微海绵物理特性的影响。采用差示扫描量热法、傅里叶变换红外、扫描电镜(SEM)、粒度分析等方法对制备的微海绵进行了表征,并对其药物含量、包封效率、体外释药和体外抗真菌活性进行了评价。结果:相容性研究结果反映没有任何迹象表明药物和聚合物之间的化学相互作用。而不同的药聚合物比和乳化剂浓度对产率、药物含量、包封效率、颗粒大小和药物释放度均有显著影响。微海绵呈球形,表面多孔,平均粒径为29.327±0.31 μm。体外释药结果显示,F1配方在8 h时释药率达到85.38%,而常规配方仅在4 h时释药率就达到了83.17%。此外,微海绵凝胶具有良好的铺展性和挤压性,并具有良好的抗真菌活性。结论:制备的微海绵是一种潜在的药物外用FLZ载体,是一种有效、安全、易于根除真菌感染的替代方法。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
Fabrication, characterization, and evaluation of microsponge delivery system for facilitated fungal therapy
Objective: The rationale behind present research vocation was to develop and investigate a novel microsponge based gel as a topical carrier for the prolonged release and cutaneous drug deposition of fluconazole (FLZ); destined for facilitated fungal therapy. Materials and Methods: Microsponges were prepared using quasi-emulsion solvent diffusion method using Eudragit S-100. In the direction of optimization, the effect of formulation variables (drug-polymer ratio and amount of emulsifier) and diverse factors affecting physical characteristics of microsponge were investigated as well. Fabricated microsponges were characterized by differential scanning calorimetry, Fourier transform-infrared, scanning electron microscopy (SEM), particle size analysis, and also evaluated for drug content, encapsulation efficiency, in vitro drug release and in vitro antifungal activity. Results: Compatibility studies results reflected no sign of any chemical interaction between the drug and polymers used. Whereas, varied drug-polymer ratios and emulsifier concentration indicated significant effect on production yield, drug content, encapsulation efficiency, particle size and drug release. Spherical microsponges with a porous surface and 29.327 ± 0.31 μm mean particle size were evident from SEM micrographs. In vitro release outcomes, from microsponge loaded gels depicted that F1 formulation was more efficient to give extended drug release of 85.38% at the end of 8 h, while conventional formulation by releasing 83.17% of drug got exhausted incredibly earlier at the end of 4 h merely. Moreover, microsponge gels demonstrated substantial spreadability and extrudability along with promising antifungal activity. Conclusions: Fabricated microsponges would be impending pharmaceutical topical carriers of FLZ and a leading alternative to conventional therapy for efficient, safe and facilitated eradication of fungal infections.
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