哺乳动物皮肤的电穿孔：一种增强透皮给药的机制。
Electroporation of mammalian skin: a mechanism to enhance transdermal drug delivery.
作者信息
Prausnitz M R, Bose V G, Langer R, Weaver J C
机构信息
Department of Chemical Engineering, Massachusetts Institute of Technology, Cambridge 02139.
出版信息
Proc Natl Acad Sci U S A. 1993 Nov 15;90(22):10504-8. doi: 10.1073/pnas.90.22.10504.
Abstract
Mammalian skin owes its remarkable barrier function to its outermost and dead layer, the stratum corneum. Transdermal transport through this region occurs predominantly through intercellular lipids, organized largely in bilayers. Electroporation is the creation of aqueous pores in lipid bilayers by the application of a short (microseconds to milliseconds) electric pulse. Our measurements suggest that electroporation occurs in the intercellular lipid bilayers of the stratum corneum by a mechanism involving transient structural changes. Flux increases up to 4 orders of magnitude were observed with human skin in vitro for three polar molecules having charges between -1 and -4 and molecular weights up to slightly more than 1000. Similar flux increases were observed in vivo with animal skin. These results may have significance for drug delivery and other medical applications.
摘要
哺乳动物的皮肤之所以具有卓越的屏障功能，归功于其最外层的死细胞层——角质层。经皮转运主要通过角质层中的细胞间脂质进行，这些脂质大多以双层形式排列。电穿孔是通过施加短暂（微秒至毫秒）的电脉冲在脂质双层中形成水孔。我们的测量表明，角质层细胞间脂质双层中的电穿孔是由一种涉及瞬时结构变化的机制引起的。在体外对三种电荷在 -1 至 -4 之间、分子量略高于 1000 的极性分子进行实验时，观察到通量增加高达 4 个数量级。在动物皮肤的体内实验中也观察到了类似的通量增加。这些结果可能对药物递送及其他医学应用具有重要意义。
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