Topical delivery of fluconazole: in vitro skin penetration and permeation using emulsions as dosage forms

Drug Dev Ind Pharm. 2007 Mar;33(3):273-80. doi: 10.1080/03639040600829989.

Abstract

We investigated in vitro skin penetration and permeation of fluconazole from emulsions containing different penetration enhancers. Fluconazole permeation was high (15-65% of the applied dose) across hairless mouse skin and low (8-9%) across pig ear skin. Permeation across mice skin from a formulation containing propyleneglycol and isopropyl myristate was significantly higher than that observed with the paraffin oil and propyleneglycol or Transcutol emulsions. With pig skin, the paraffin oil or isopropyl myristate and propyleneglycol emulsions showed similar skin permeation and penetration. However, these emulsions provided epidermal concentrations higher than the minimal inhibitory concentrations for most dermatophytes.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Administration, Topical
  • Animals
  • Antifungal Agents / administration & dosage*
  • Antifungal Agents / chemistry
  • Antifungal Agents / pharmacokinetics
  • Chemistry, Pharmaceutical / methods*
  • Chromatography, High Pressure Liquid
  • Emulsions
  • Fluconazole / administration & dosage*
  • Fluconazole / chemistry
  • Fluconazole / pharmacokinetics
  • Male
  • Mice
  • Mycoses / drug therapy
  • Skin Absorption
  • Solubility
  • Swine

Substances

  • Antifungal Agents
  • Emulsions
  • Fluconazole