Pharmaceutical Research 2014-11-01

Acid-responsive polymeric nanocarriers for topical adapalene delivery.

Chenchen Guo, Rajeshree H Khengar, Mingjing Sun, Zheng Wang, Aiping Fan, Yanjun Zhao

Index: Pharm. Res. 31(11) , 3051-9, (2014)

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Abstract

The acne skin is characteristic of a relatively lower pH microenvironment compared to the healthy skin. The aim of this work was to utilize such pH discrepancy as a site-specific trigger for on-demand topical adapalene delivery.The anti-acne agent, adapalene, was encapsulated in acid-responsive polymer (Eudragit® EPO) nanocarriers via nanoprecipitation. The nanocarriers were characterized in terms of particle size, surface morphology, drug-carrier interaction, drug release and permeation.Adapalene experienced a rapid release at pH 4.0 in contrast to that at pH 5.0 and 6.0. The permeation study using silicone membrane revealed a significant higher drug flux from the nanocarrier (6.5 ± 0.6 μg.cm(-2).h(-1)) in comparison to that (3.9 ± 0.4 μg.cm(-2).h(-1)) in the control vehicle (Transcutol®). The in vitro pig skin tape stripping study showed that at 24 h post dose-application the nanocarrier delivered the same amount of drug to the stratum corneum as the positive control vehicle did.The acid-responsive nanocarriers hold promise for efficient adapalene delivery and thus improved acne therapy.