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Enhanced dermal delivery of diflucortolone valerate using lecithin/chitosan nanoparticles: in-vitro and in-vivo evaluations

Authors Özcan İ, Azizoğlu E, Şenyiğit T, Özyazıcı M, Özer Ö

Received 20 November 2012

Accepted for publication 28 December 2012

Published 30 January 2013 Volume 2013:8(1) Pages 461—475

DOI https://doi.org/10.2147/IJN.S40519

Checked for plagiarism Yes

Review by Single-blind

Peer reviewer comments 4

İpek Özcan, Erkan Azizoğlu, Taner Şenyiğit, Mine Özyazıcı, Özgen Özer

Ege University, Faculty of Pharmacy, Department of Pharmaceutical Technology, Bornova, Izmir, Turkey

Abstract: The objective of this study was to prepare a suitable formulation for dermal delivery of diflucortolone valerate (DFV) that would maintain the localization in skin layers without any penetration and to optimize efficiency of DFV. Drug-loaded lecithin/chitosan nanoparticles with high entrapment efficiency (86.8%), were successfully prepared by ionic interaction technique. Sustained release of DFV was achieved without any initial burst release. Nanoparticles were also incorporated into chitosan gel at different ratios for preparing a more suitable formulation for topical drug delivery with adequate viscosity. In ex-vivo permeation studies, nanoparticles increased the accumulation of DFV especially in the stratum corneum + epidermis of rat skin without any significant permeation. Retention of DFV from nanoparticle in chitosan gel formulation (0.01%) was twofold higher than commercial cream, although it contained ten times less DFV. Nanoparticles in gel formulations produced significantly higher edema inhibition in rats compared with commercial cream in in-vivo studies. Skin blanching assay using a chromameter showed vasoconstriction similar to that of the commercial product. There were no barrier function changes upon application of nanoparticles. In-vitro and in-vivo results demonstrated that lecithin/chitosan nanoparticles in chitosan gel may be a promising carrier for dermal delivery of DFV in various skin disorders.

Keywords: skin permeation, anti-inflammatory activity, skin blanching, TEWL

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