Jia-You Fang, Y. Leu, Ying-Yue Wang
Jun 1, 2002
Citations
2
Influential Citations
58
Citations
Quality indicators
Journal
European journal of pharmaceutical sciences : official journal of the European Federation for Pharmaceutical Sciences
Abstract
Nonivamide, a so-called synthetic capsaicin, is a substitute for capsaicin which has a similar chemical structure and pharmacological activities as those of capsaicin. The purposes of this study were to explore the in vivo pharmacodynamic responses of nonivamide in hydrogels using Wistar rat as an animal model and to correlate the in vivo results with in vitro topical application. The incorporation of Pluronic F-127 polymer into hydrogels resulted in retarded release of nonivamide. Chitosan and carboxymethylcellulose hydrogels produced higher levels of in vitro nonivamide permeation and skin distribution. The in vivo effects of nonivamide on skin perturbation and vasodilation were found to differ depending on dose and duration after topical application. Quantification of transepidermal water loss was demonstrated to correlate with the measured in vitro skin distribution of nonivamide. The various doses of nonivamide in the hydrogels did not markedly influence erythematous reactions of skin as determined by colorimetric measurements. Hydrogel formulations of nonivamide delivered more drug to the skin and produced greater pharmacodynamic activities than did cream bases of capsaicin.