ELECTROPORATION OF MAMMALIAN SKIN - A MECHANISM TO ENHANCE TRANSDERMAL DRUG-DELIVERY
ELECTROPORATION OF MAMMALIAN SKIN - A MECHANISM TO ENHANCE TRANSDERMAL DRUG-DELIVERY
复制标题
DOI：
10.1073/pnas.90.22.10504
复制
发表时间：
1993-11-15
影响因子：
11.1
通讯作者：
WEAVER, JC
中科院分区：
文献类型：
--
作者：
PRAUSNITZ, MR;BOSE, VG;WEAVER, JC
哺乳动物的皮肤由于其最外层和死亡层角质层而具有显著的屏障功能。通过该区域的经皮转运主要通过细胞间脂质发生，主要以双层组织。电穿孔是通过施加短（微秒至毫秒）电脉冲在脂质双层中产生水性孔。我们的测量结果表明，电穿孔发生在角质层的细胞间脂质双层的机制，涉及短暂的结构变化。通量增加高达4个数量级的观察与人类皮肤在体外的三个极性分子具有电荷之间的-1和-4和分子量略大于1000。在动物皮肤的体内观察到类似的通量增加。这些结果可能对药物输送和其他医学应用具有重要意义。
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.