Effect of chemical penetration enhancer and iontophoresis on the in vitro percutaneous absorption enhancement of insulin through porcine epidermis.
Effect of chemical penetration enhancer and iontophoresis on the in vitro percutaneous absorption enhancement of insulin through porcine epidermis.
复制标题
化学渗透促进剂和离子电渗疗法对猪表皮胰岛素体外经皮吸收增强的影响。
DOI：
10.1081/pdt-49679
复制
发表时间：
2005
期刊：
影响因子：
--
通讯作者：
Singh,Jagdish
中科院分区：
文献类型：
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作者：
Rastogi,SumeetK;Singh,Jagdish
本研究旨在探讨化学促进剂（脂肪酸、柠檬烯）和离子导入对胰岛素体外通过猪表皮通透性的影响。所使用的脂肪酸如下：棕榈酸（C16:0）、棕榈油酸（C16:1）、硬脂酸（C18:0）、油酸（C18:1）、亚油酸（C18:2）和亚麻酸（C18:3）。经皮吸收研究采用Franz扩散池和Scepter™离子电泳电源。阴极离子电泳在0.2 mA/cm2电流密度下进行。离子透入联合化学促进剂可协同提高胰岛素的体外通透性（p< 0.05）。亚麻酸（C18:3）在被动转运（44.45 × 10−4cm/h）和离子吸附转运（78.03 × 10−4cm/h）过程中对胰岛素的通透性高于其他脂肪酸。与未处理的对照组相比，经亚麻酸和柠檬烯预处理的表皮的Lispro胰岛素通量在被动和离子渗透运输中均显著（p< 0.05）增加。使用柠檬烯作为渗透促进剂，观察到lispro胰岛素的被动和离子渗透通量随供体浓度从100 IU/mL增加到300 IU/mL呈线性增加。在0.5 mA/cm2电流密度和300 IU/mL胰岛素供体溶液条件下，柠檬烯处理表皮的离子迁移通量为45.63 IU/cm2/day。使用10cm2大小的离子电泳贴片，我们将能够在3小时内输送50iu的胰岛素。
The purpose of this study was to investigate the effect of chemical enhancers (fatty acids and limonene) and iontophoresis on the in vitro permeability enhancement of insulin through porcine epidermis. The following fatty acids were used: palmitic (C16:0), palmitoleic (C16:1), stearic (C18:0), oleic (C18:1), linoleic (C18:2), and linolenic (C18:3). Franz diffusion cells and the Scepter™ iontophoretic power source were used for the percutaneous absorption studies. Cathodal iontophoresis was performed at 0.2 mA/cm2current density. Iontophoresis in combination with chemical enhancers synergistically increased (p< 0.05) the in vitro permeability of insulin. Linolenic acid (C18:3) produced greater permeability of insulin through epidermis than did other fatty acids during passive (44.45 × 10− 4cm/h) and iontophoretic (78.03 × 10− 4cm/h) transport. Lispro insulin flux was significantly (p< 0.05) greater through linolenic acid and limonene pretreated epidermis compared to untreated controls during both passive and iontophoretic transports. Using limonene as a penetration enhancer, a linear increase in the passive and iontophoretic flux of lispro insulin was observed with donor concentrations increasing from 100 IU/mL to 300 IU/mL. Iontophoretic flux through limonene-treated epidermis using 0.5 mA/cm2current density and 300 IU/mL insulin donor solution was 45.63 IU/cm2/day. Using an iontophoretic patch size of 10 cm2, we would be able to deliver 50 IU of insulin within 3 h.