Wang Wen-Yi, Hui Patrick C L, Wat Elaine, Ng Frency S F, Kan Chi-Wai, Lau Clara B S, Leung Ping-Chung
Institute of Textiles and Clothing, The Hong Kong Polytechnic University, Hung Hom, Kowloon, Hong Kong, China.
Institute of Chinese Medicine, The Chinese University of Hong Kong, Shatin, New Territories, Hong Kong, China.
Polymers (Basel). 2016 Nov 21;8(11):406. doi: 10.3390/polym8110406.
A major concern for transdermal drug delivery systems is the low bioavailability of targeted drugs primarily caused by the skin's barrier function. The resistance to the carrier matrix for the diffusion and transport of drugs, however, is routinely ignored. This study reports a promising and attractive approach to reducing the resistance to drug transport in the carrier matrix, to enhance drug permeability and bioavailability via enhanced concentration-gradient of the driving force for transdermal purposes. This approach simply optimizes and reconstructs the porous channel structure of the carrier matrix, namely, poloxamer 407 (P407)-based hydrogel matrix blended with carboxymethyl cellulose sodium (CMCs). Addition of CMCs was found to distinctly improve the porous structure of the P407 matrix. The pore size approximated to normal distribution as CMCs were added and the fraction of pore number was increased by over tenfold. Transdermal studies showed that P407/CMCs saw a significant increase in drug permeability across the skin. This suggests that P407/CMC with improved porous structure exhibits a feasible and promising way for the development of transdermal therapy with high permeability and bioavailability, thereby avoiding or reducing use of any chemical enhancers.
经皮给药系统的一个主要问题是靶向药物的生物利用度低，这主要是由皮肤的屏障功能造成的。然而，药物在载体基质中扩散和运输时对载体基质的阻力通常被忽略。本研究报告了一种有前景且有吸引力的方法，即通过增强经皮驱动力的浓度梯度来降低药物在载体基质中的运输阻力，以提高药物渗透性和生物利用度。该方法简单地优化和重建了载体基质的多孔通道结构，即与羧甲基纤维素钠（CMCs）混合的泊洛沙姆407（P407）基水凝胶基质。发现添加CMCs可显著改善P407基质的多孔结构。随着CMCs的添加，孔径近似正态分布，孔数分数增加了十倍以上。经皮研究表明，P407/CMCs的药物经皮渗透率显著提高。这表明具有改进多孔结构的P407/CMC为开发具有高渗透性和生物利用度的经皮治疗提供了一种可行且有前景的方法，从而避免或减少使用任何化学促进剂。
