Topical delivery of fluconazole: in vitro skin penetration and permeation using emulsions as dosage forms.
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.
Ayub
Alessandra C
AC
Department of Pharmaceutics, Faculty of Pharmacy, Federal University of Minas Gerais (UFMG), Av. Antonio Carlos, Belo Horizont (MG), Brazil.
Gomes
Aline D M
AD
Lima
Marcus V C
MV
Vianna-Soares
Cristina D
CD
Ferreira
Lucas A M
LA
D000287:Administration, Topical; D000818:Animals; D000935:Antifungal Agents / Q000008:administration & dosage* / Q000737:chemistry / Q000493:pharmacokinetics; D002626:Chemistry, Pharmaceutical / Q000379:methods*; D002851:Chromatography, High Pressure Liquid; D004655:Emulsions; D015725:Fluconazole / Q000008:administration & dosage* / Q000737:chemistry / Q000493:pharmacokinetics; D008297:Male; D051379:Mice; D009181:Mycoses / Q000188:drug therapy; D012869:Skin Absorption; D012995:Solubility; D013552:Swine
D000935:Antifungal Agents; D004655:Emulsions; D015725:Fluconazole