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设计和开发用于局部递送抗真菌药物的固体脂质纳米粒。

Design and development of solid lipid nanoparticles for topical delivery of an anti-fungal agent.

机构信息

Pharmaceutics Research Projects Laboratory, Department of Pharmaceutical Sciences, Dr. Hari Singh Gour Vishwavidyalaya, Sagar (M. P.) 470003, India.

出版信息

Drug Deliv. 2010 Aug;17(6):443-51. doi: 10.3109/10717544.2010.483252.

Abstract

Topical application of the drugs at the pathological sites offers potential advantages of delivering the drug directly to the site of action. The main aim of this work was to formulate and evaluate Miconazole nitrate (MN) loaded solid lipid nanoparticles (SLN) for topical application. MN-loaded SLN were prepared by modified solvent injection method and characterized for shape, surface morphology, particle size, and drug entrapment. These solid lipid nanoparticles were spherical in shape with smooth surface and possessed mean average size of 206.39 +/- 9.37 nm. In vitro drug release of MN-loaded SLN-bearing hydrogel was compared with MN suspension and MN hydrogel; MN-loaded SLN-bearing hydrogel depicted a sustained drug release over a 24-h period. Tape stripping experiments demonstrated 10-fold greater retention with MN-loaded SLN-bearing hydrogel as compared to MN suspension and MN hydrogel. The in vivo studies were performed by infecting the rats with candida species. It was observed that MN-loaded SLN-bearing hydrogel was more efficient in the treatment of candidiasis. Results indicate that MN-loaded SLN-bearing hydrogel provides a sustaining MN topical effect as well as quicker relief from fungal infection.

摘要

将药物涂抹在病变部位具有将药物直接输送到作用部位的潜在优势。这项工作的主要目的是制备并评价硝酸咪康唑(MN)负载的固体脂质纳米粒(SLN)用于局部应用。MN 负载的 SLN 通过改良溶剂注入法制备,并对其形状、表面形态、粒径和药物包封进行了表征。这些固体脂质纳米粒呈球形,表面光滑,平均粒径为 206.39 +/- 9.37nm。MN 负载的 SLN 载药凝胶的体外药物释放与 MN 混悬液和 MN 凝胶进行了比较;MN 负载的 SLN 载药凝胶在 24 小时内呈现出持续的药物释放。胶带剥离实验表明,与 MN 混悬液和 MN 凝胶相比,MN 负载的 SLN 载药凝胶的保留率提高了 10 倍。通过用念珠菌感染大鼠进行体内研究。结果表明,MN 负载的 SLN 载药凝胶在治疗念珠菌病方面更有效。结果表明,MN 负载的 SLN 载药凝胶既能提供持续的 MN 局部作用,又能更快地缓解真菌感染。

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