Effect of O-acylterpineol on in vitro penetration of isosorbide dinitrate through rabbit skin
To develop more effective compounds as penetration enhancers, O-acylterpineol derivatives were synthesized by α-terpineol and fatty acid, 1-methyl-2-pyrrolidinone (NMP) and Azone were also employed as reference enhancers.Their promoting activities on the percutaneous absorption of isosorbide dinitrate (ISDN) were tested in vitro across full thickness rabbit skin with ISDN saturated donor solution.Attenuated total reflection-Fourier transform infrared spectroscopy and transepidermal water loss (TEWL) were introduced to investigate the enhancer induced alteration in different skin lipid domains.All the O-acylterpineol derivatives had promoting effects on the percutaneous permeation of ISDN;2-(4-methylcyclohex-3-en-l-yl) propan-2-yl butanoate (C4 alkyl chain) and NMP provided the best enhancement activities for ISDN, they increased the ISDN in accumulation by 7.67-fold and8.50-fold, respectively.After skin treatment, 2-(4-methylcyclohex-3-en-l-yl)propan-2-yl tetradecanoate (C14 alkyl chain)produced the highest shift in the stretching vibration of the methylene in hydrophobic lipid chains, NMP produced the highest shift in the stretching vibration peak position of amide Ⅰ and the lowest shift the stretching vibration peak position of amide Ⅱ.
Yan Li Ligang Zhao Chunyan Wang Gang Han
School of Pharmacy, North China University of Science and Technology, 57 Jianshe south Rod,Tangshan, School of Pharmacy, North China University of Science and Technology, 57 Jianshe south Rod,Tangshan, Dept.of Pharmacy, Tangshan Maternal and Child Health Hospital, 14 Jianshe south Road, Tangshan,Hebei
国际会议
沈阳
英文
380-383
2016-04-28（万方平台首次上网日期，不代表论文的发表时间）