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

Ozcan, Ipek; Azizoglu, Erkan; Senyigit, Taner; Ozyazici, Mine; Ozer, Ozgen


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        "affiliation": "Ege Univ, Fac Pharm, Dept Pharmaceut Technol, TR-35100 Izmir, Turkey", 
        "name": "Ozcan, Ipek"
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      {
        "affiliation": "Ege Univ, Fac Pharm, Dept Pharmaceut Technol, TR-35100 Izmir, Turkey", 
        "name": "Azizoglu, Erkan"
      }, 
      {
        "affiliation": "Ege Univ, Fac Pharm, Dept Pharmaceut Technol, TR-35100 Izmir, Turkey", 
        "name": "Senyigit, Taner"
      }, 
      {
        "affiliation": "Ege Univ, Fac Pharm, Dept Pharmaceut Technol, TR-35100 Izmir, Turkey", 
        "name": "Ozyazici, Mine"
      }, 
      {
        "affiliation": "Ege Univ, Fac Pharm, Dept Pharmaceut Technol, TR-35100 Izmir, Turkey", 
        "name": "Ozer, Ozgen"
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    "description": "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.", 
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      "pages": "461-475", 
      "title": "INTERNATIONAL JOURNAL OF NANOMEDICINE", 
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