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


Creative Commons License

OZCAN I., AZİZOĞLU E. , ŞENYİĞİT T., ÖZYAZICI M. , OZER O.

INTERNATIONAL JOURNAL OF NANOMEDICINE, cilt.8, ss.461-475, 2013 (SCI İndekslerine Giren Dergi) identifier identifier identifier

  • Cilt numarası: 8
  • Basım Tarihi: 2013
  • Doi Numarası: 10.2147/ijn.s40519
  • Dergi Adı: INTERNATIONAL JOURNAL OF NANOMEDICINE
  • Sayfa Sayıları: ss.461-475

Özet

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.