文献名： Clobetasol-loaded nanostructured lipid carriers for epidermal targeting

作者： Luis Antônio Dantas Silva1, Lígia Marquez Andrade1, Fernando Augusto Pires de Sá2, Ricardo Neves Marreto1, Eliana Martins Lima1, Tais Gratieri2 andStephânia Fleury Taveira1
1Laboratory of Pharmaceutical Technology, School of Pharmacy, Universidade Federal de Goiás (UFG), Goiânia, GO, Brasil
2Laboratory of Food, Drugs and Cosmetics (LTMAC), Universidade de Brasília (UnB), Campus Universitário Darcy Ribeiro, Asa Norte, 70.910-900, Brasília, Brasília, DF, Brasil

摘要：
Objectives
The aim of this study was to investigate in vitro the epidermal targeting potential of clobetasol propionate-loaded nanostructured lipid carriers (CP-NLC) when compared to that of chitosan-coated (CP-NLC-C).

Methods
CP-NLC were prepared by microemulsion method and characterized by dynamic light scattering, transmission electron microscopy, in vitro release and permeation studies. To verify epidermal targeting, permeation studies were performed in two sets of experiments. For the first set, the skin was removed from the diffusion cell and stratum corneum (SC) was separated from the remaining skin (RS). For the second set, the whole epidermis (EP) was separated from the dermis (DER). CP quantification was performed in each skin layer.

Key findings
A novel clobetasol propionate-loaded NLC was produced with 1/5th of the drug dose used in commercial formulations and, even so, presented greater skin permeation. Both chitosan-coated and uncoated NLC enhanced the amount of CP in the epidermis more than 80-fold when compared to the commercial formulation (20.26 ± 2.77; 17.85 ± 0.49 and 0.22 ± 0.02 μg/cm2, respectively). Differently from chitosan-coated NLC, the uncoated NLC did not show dermal retention.

Conclusions
NLC proved to be a system with potential for targeting drug delivery to the epidermal layer.

关键词：chitosan;Clobetasol;epidermal targeting;lipid nanoparticle;skin permeation