文献类型：期刊文献

英文题名：A Drug-in-Adhesive Matrix Based on Thermoplastic Elastomer: Evaluation of Percutaneous Absorption, Adhesion, and Skin Irritation

作者：Wang, ChengXiao[1,2];Liu, Ran[1,2];Tang, XiuZhen[2];Han, Wei[1]

机构：[1]E China Univ Sci & Technol, Sch Pharm, Shanghai 200237, Peoples R China;[2]Natl Engn Res Ctr Tradit Chinese Med, Shanghai 201203, Peoples R China

年份：2012

卷号：13

期号：4

起止页码：1179

外文期刊名：AAPS PHARMSCITECH

收录：;WOS:【SCI-EXPANDED(收录号:WOS:000313500500017)】；

基金：This research was supported by the National Science and Technology Key Program for the 11th Five-Year Plan of China (2008BAI53B075).

语种：英文

外文关键词：adhesion; in vivo absorption; skin irritation; thermoplastic elastomer; transdermal drug delivery

摘要：A novel drug-in-adhesive matrix was designed and prepared. A thermoplastic elastomer, styrene-isoprene-styrene (SIS) block copolymer, in combination with tackifying resin and plasticizer, was employed to compose the matrix. Capsaicin was selected as the model drug. The drug percutaneous absorption, adhesion properties, and skin irritation were investigated. The results suggested that the diffusion through SIS matrix was the rate-limiting step of capsaicin percutaneous absorption. [SI] content in SIS and SIS proportions put important effects on drug penetration and adhesion properties. The chemical enhancers had strong interactions with the matrix and gave small effect on enhancement of drug skin permeation. The in vivo absorption of samples showed low drug plasma peaks and a steady and constant plasma level for a long period. These results suggested that the possible side effects of drug were attenuated, and the pharmacological effects were enhanced with an extended therapeutic period after application of SIS matrix. The significant differences in pharmacokinetic parameters produced by different formulations demonstrated the influences of SIS copolymer on drug penetrability. Furthermore, the result of skin toxicity test showed that no skin irritation occurred in guinea pig skin after transdermal administration of formulations.