Development and evaluation of microemulsions for transdermal delivery of insulin.

ISRN Pharmaceutics Pub Date : 2011-01-01 Epub Date: 2011-07-07 DOI:10.5402/2011/780150
Jadupati Malakar, Suma Oomen Sen, Amit Kumar Nayak, Kalyan Kumar Sen
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引用次数: 57

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.

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胰岛素透皮微乳的研制与评价。
以肉豆肉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,研制了经皮胰岛素微乳。构建了伪三元相图来确定微乳的组成。以油酸为油相的微乳通过小鼠皮肤和山羊皮肤的胰岛素渗透通量相对大于以肉豆酸异丙酯为油相的微乳。以2%二甲亚砜(DMSO)为渗透增强剂,油酸含量为10%,水相含量为38%,表面活性剂含量为50%,负载胰岛素的微乳液通过山羊皮肤的渗透通量为4.93±0.12 μg/cm(2)/h。这些微乳的体外胰岛素渗透在24小时内遵循Korsmeyer-Peppas模型(R(2) = 0.923至0.973),具有非菲克的“异常”机制。综上所述,这些初步数据表明,微乳剂用于胰岛素透皮给药是有希望的。
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