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用于胰岛素经皮递送的微乳剂的开发与评价。

Development and evaluation of microemulsions for transdermal delivery of insulin.

作者信息

Malakar Jadupati, Sen Suma Oomen, Nayak Amit Kumar, Sen Kalyan Kumar

机构信息

Department of Pharmaceutics, Bengal College of Pharmaceutical Sciences and Research, West Bengal, Durgapur 713212, India.

出版信息

ISRN Pharm. 2011;2011:780150. doi: 10.5402/2011/780150. Epub 2011 Jul 7.

Abstract

Insulin-loaded microemulsions for transdermal delivery were developed using isopropyl myristate or oleic acid as the oil phase, Tween 80 as the surfactant, and isopropyl alcohol as the cosurfactant. The pseudoternary phase diagrams were constructed to determine the composition of microemulsions. The insulin permeation flux of microemulsions containing oleic acid as oil phase through excised mouse skin and goat skin was comparatively greater than that of microemulsions containing isopropyl myristate as oil phase. The insulin-loaded microemulsion containing 10% oleic acid, 38% aqueous phase, and 50% surfactant phase with 2% dimethyl sulfoxide (DMSO) as permeation enhancer showed maximum permeation flux (4.93 ± 0.12 μg/cm(2)/hour) through goat skin. The in vitro insulin permeation from these microemulsions was found to follow the Korsmeyer-Peppas model (R(2) = 0.923 to 0.973) over a period of 24 hours with non-Fickian, "anomalous" mechanism. Together these preliminary data indicate the promise of microemulsions for transdermal delivery of insulin.

摘要

以肉豆蔻酸异丙酯或油酸为油相、吐温80为表面活性剂、异丙醇为助表面活性剂,制备了用于经皮给药的载胰岛素微乳。构建了拟三元相图以确定微乳的组成。含油酸作为油相的微乳通过切除的小鼠皮肤和山羊皮肤的胰岛素渗透通量相对大于含肉豆蔻酸异丙酯作为油相的微乳。含10%油酸、38%水相和50%表面活性剂相并添加2%二甲基亚砜(DMSO)作为渗透促进剂的载胰岛素微乳通过山羊皮肤显示出最大渗透通量(4.93±0.12μg/cm²/小时)。在24小时内,这些微乳的体外胰岛素渗透遵循Korsmeyer-Peppas模型(R² = 0.923至0.973),其机制为非菲克、“异常”机制。这些初步数据共同表明微乳用于胰岛素经皮给药具有前景。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/2635/3263709/62e2d802b0cc/PHARMACEUTICS2011-780150.001.jpg

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