Curtin Health Innovation Research Institute, School of Pharmacy, Curtin University, Perth, Western Australia.
Biopolymers. 2011;96(2):166-71. doi: 10.1002/bip.21520.
Poor skin permeability limits the application of peptides to the skin. Enhanced skin permeation could facilitate the development of new therapies for dermatologic and cosmeceutical applications. The aim of this study was to investigate the application of iontophoresis to the delivery of small peptide model compounds (5-aminolevulinic acid and L-alanine-L-tryptophan) across human skin. Under the conditions tested, iontophoresis increased the in vitro permeability coefficient of ALA.HCl across human epidermis from 7 X 10(-5) cm/h with passive diffusion to 110 x 10(-5) cm/h with iontophoresis. D-Glucose permeation elucidated the iontophoretic electrotransport of ALA.HCl to have contributions of both electrorepulsion and electroosmosis. The L-alanine-L-tryptophan permeability coefficient was increased from 1.5 x 10(-5) cm/h to 35 x 10(-5) cm/h with iontophoretic application. Iontophoretic delivery of the dipeptide increased markedly at lower pH because of an increase in electrorepulsive transport. The study demonstrates that iontophoresis can enhance epidermal permeation of a small peptide and peptide-like drug by up to 15- and 22-fold under the conditions tested.
皮肤通透性差限制了肽在皮肤中的应用。增强皮肤渗透性能有助于开发新的治疗方法，用于皮肤科和化妆品应用。本研究旨在探讨离子导入在小肽模型化合物（5-氨基乙酰丙酸和 L-丙氨酸-L-色氨酸）经皮传递中的应用。在测试的条件下，离子导入将 ALA.HCl 通过人表皮的体外渗透系数从被动扩散的 7×10(-5)cm/h 增加到离子导入的 110×10(-5)cm/h。D-葡萄糖渗透阐明了 ALA.HCl 的离子电迁移既有电排斥又有电渗流的贡献。用离子导入法，L-丙氨酸-L-色氨酸的渗透系数从 1.5×10(-5)cm/h 增加到 35×10(-5)cm/h。由于电排斥运输的增加，较低 pH 值时二肽的离子导入输送显著增加。研究表明，在测试条件下，离子导入可以将小肽和肽类药物的表皮渗透增强 15 至 22 倍。
