DEVELOPMENT OF A TOPICAL R126521 FORMULATION WITH IN VITRO SKIN PERMEATION AND RELEASE STUDIES

摘要

In vitro release tests are efficient tools to investigate the influence of excipients and solvents on the release of active compounds from a formulation. The skin accumulation of R126521 from conventional and investigational topical formulations was very low. The incorporation of PEG 400 or HPβCD in formulations improved the release of the formulation, but not the in vitro skin accumulation. Therefore, it can be concluded that the limiting factor in R126521 skin penetration is the skin barrier function, and not its availability from the formulation. The penetration enhancers limonene, oleic acid and linolenic acid significantly increased the skin accumulation and permeation of R126521. Currently, formulations of R126521 with these penetration enhancers are being developed.