title: Enhanced dermal delivery of diflucortolone valerate using lecithin/chitosan nanoparticles: in-vitro and in-vivo evaluations.
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.
authors: Ege University, Faculty of Pharmacy, Department of Pharmaceutical Technology, Bornova, Izmir, Turkey. ipek.ozcan@ege.edu.tr
authors: Ipek
authors: I
authors: Özcan
authors: Erkan
authors: E
authors: Azizoğlu
authors: Taner
authors: T
authors: Senyiğit
authors: Mine
authors: M
authors: Özyazıcı
authors: Özgen
authors: Ö
authors: Özer
mesh_terms: D000279:Administration, Cutaneous; D000818:Animals; D000893:Anti-Inflammatory Agents / Q000008:administration & dosage / Q000737:chemistry / Q000493:pharmacokinetics; D048271:Chitosan / Q000008:administration & dosage / Q000737:chemistry*; D004060:Diflucortolone / Q000008:administration & dosage / Q000031:analogs & derivatives* / Q000737:chemistry / Q000493:pharmacokinetics; D004337:Drug Carriers / Q000008:administration & dosage / Q000737:chemistry* / Q000494:pharmacology; D004487:Edema / Q000188:drug therapy; D005782:Gels / Q000008:administration & dosage / Q000737:chemistry; D054709:Lecithins / Q000008:administration & dosage / Q000737:chemistry*; D008297:Male; D055595:Mechanical Phenomena; D053758:Nanoparticles / Q000008:administration & dosage / Q000737:chemistry*; D010316:Particle Size; D051381:Rats; D017208:Rats, Wistar; D012867:Skin / Q000737:chemistry / Q000378:metabolism; D012869:Skin Absorption / Q000187:drug effects*; D014661:Vasoconstriction / Q000187:drug effects
chemical_list: D000893:Anti-Inflammatory Agents; D004337:Drug Carriers; D005782:Gels; D054709:Lecithins; C013486:diflucortolone valerate; D048271:Chitosan; D004060:Diflucortolone
keywords: TEWL; anti-inflammatory activity; skin blanching; skin permeation
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