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表面活性剂对氟康唑脂质体特性的影响以增强经皮递送

Effect of surfactants on the characteristics of fluconazole niosomes for enhanced cutaneous delivery.

作者信息

Gupta Madhu, Vaidya Bhuvaneshwar, Mishra Neeraj, Vyas Suresh P

机构信息

Drug Delivery Research Laboratory, Department of Pharmaceutical Sciences , Dr. H. S. Gour Viswavidyalaya, Sagar, India.

出版信息

Artif Cells Blood Substit Immobil Biotechnol. 2011 Dec;39(6):376-84. doi: 10.3109/10731199.2011.611476. Epub 2011 Sep 27.

Abstract

Fluconazole-loaded niosomes were prepared by the film hydration method with different surfactants (Span and Brij series) and characterized for various parameters. Results showed that niosomes composed of Span 40, Span 60, and Brij 72 were most stable with smaller size, i.e. 0.378 ± 0.022 μm, 0.343 ± 0.063 μm, and 0.287 ± 0.012 μm, respectively, along with higher entrapment efficiency (approx. > 41%). In vitro skin permeation and retention studies suggested that cutaneous accumulation was affected by surfactant property and vesicle size. Therefore the niosomes consisting of Span 40, Span 60, and Brij 72 surfactant are seemingly accumulated and form localized drug depots in the skin, thereby releasing the contents in a sustained manner and able to greatly enhance cutaneous retention of the drug.

摘要

采用薄膜水化法,使用不同的表面活性剂(司盘和聚氧乙烯脂肪醇醚系列)制备了载氟康唑的非离子表面活性剂囊泡,并对其各项参数进行了表征。结果表明,由司盘40、司盘60和聚氧乙烯脂肪醇醚72组成的非离子表面活性剂囊泡最稳定,粒径较小,分别为0.378±0.022μm、0.343±0.063μm和0.287±0.012μm,包封率也较高(约>41%)。体外皮肤渗透和滞留研究表明,皮肤蓄积受表面活性剂性质和囊泡大小的影响。因此,由司盘40、司盘60和聚氧乙烯脂肪醇醚72表面活性剂组成的非离子表面活性剂囊泡似乎会在皮肤中蓄积并形成局部药物贮库,从而持续释放其内容物,并能够大大提高药物在皮肤中的滞留率。

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