Transdermal drug delivery by in-skin electroporation using a microneedle array
Transdermal drug delivery by in-skin electroporation using a microneedle array
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DOI：
10.1016/j.ijpharm.2010.06.052
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发表时间：
2010-09-15
影响因子：
5.8
通讯作者：
Sugibayashi, Kenji
中科院分区：
文献类型：
--
作者：
Yan, Keshu;Todo, Hiroaki;Sugibayashi, Kenji
本工作的目的是开发一种微创系统，用于将大分子药物输送到深层皮肤组织，即所谓的皮肤内电穿孔（in-skin EP），使用微针（MN）电极阵列。以异硫氰酸荧光素-葡聚糖（FD-4：平均分子量4.3 kDa）为模型大分子药物。MNs被放置以刺穿皮肤屏障角质层，电极被用于EP，以便在皮肤组织上施加高电场以促进可行的皮肤递送。体外皮肤渗透实验表明，In - skin EP对FD-4的皮肤渗透增强作用远高于MN单独或ON-SKIN EP（常规EP处理），并且施加更高的电压和更长的脉冲宽度的EP可以实现更高的渗透。此外，通过LDH浸出试验，In - skin EP未观察到明显的皮肤刺激。这些结果表明，与MN单独和传统的ON-SKIN EP相比，IN-SKIN EP可以更有效地作为大分子药物的潜在皮肤递送系统。(C) 2010 Elsevier B.V.版权所有
The aim of the present work was to develop a minimally invasive system for the delivery of macromolecular drugs to the deep skin tissues, so-called in-skin electroporation (IN-SKIN EP), using a microneedle (MN) electrode array. Fluorescein isothiocyanate (FITC)-dextran (FD-4: average molecular weight, 4.3 kDa) was used as the model macromolecular drug. MNs were arranged to puncture the skin barrier, the stratum corneum, and electrodes were used for EP so that a high electric field could be applied to skin tissues to promote viable skin delivery. In vitro skin permeation experiments showed that IN-SKIN EP had a much higher skin penetration-enhancing effect for FD-4 than MN alone or ON-SKIN EP (conventional EP treatment), and that higher permeation was achieved by applying a higher voltage and longer pulse width of EP. In addition, no marked skin irritation was observed by IN-SKIN EP, which was determined by the LDH leaching test.These results suggest that IN-SKIN EP can be more effectively utilized as a potential skin delivery system of macromolecular drugs than MN alone and conventional ON-SKIN EP. (C) 2010 Elsevier B.V. All rights reserved.