Improvement in Percutaneous Absorption of Prednisolone by β- and ϒ-Cyclodextrin Complexations

Abstract

In vitro release characteristics of prednisolone (PD) and its β- and ϒ-cyclodextrin (β - and ϒ-CyD) complexes were investigated by using an ointment release simulator with artificial double-layer membranes. The release of PD from hydrophilic ointment was significantly improved by pand ϓ-CyD complexations. Permeation and uptake studies indicated that the enhanced release of PD from the ointment may be mainly due to the faster dissolution of PD in the base and the lower binding affinity of PD to the ointment base as a result of the CyD complexations. The percutaneous absorption of PD from hydrophilic ointment after application to the rabbit skin was also increased by CyD complexations. The in vitro and in vivo data suggest that CyDs can improve the topical bioavailability of PD. © 1987, The Pharmaceutical Society of Japan. All rights reserved.