Effect of formulation components on the in vitro permeation of microemulsion drug delivery system of fluconazole.
The purpose of this study was to evaluate the effect of formulation components on the in vitro skin permeation of microemulsion drug delivery system containing fluconazole (FLZ). Lauryl alcohol (LA) was screened as the oil phase of microemulsions. The pseudo-ternary phase diagrams for microemulsion regions were constructed using LA as the oil, Labrasol (Lab) as the surfactant and ethanol (EtOH) as the cosurfactant. The formulation which showed a highest permeation rate of 47.15 +/- 1.12 microg cm(-2) h(-1) and appropriate physicochemical properties was optimized as containing 2% FLZ, 10% LA, 20% Lab/EtOH (1:1), and 68% double-distilled water (w/w). The efficiency of microemulsion formulation in the topical delivery of FLZ was dependent upon the contents of water and LA as well as Lab/EtOH mixing ratio. It was concluded that the percutaneous absorption of FLZ from microemulsions was enhanced with increasing the LA and water contents, and with decreasing the Lab/EtOH ratio in the formulation. Candida albicans was used as a model fungus to evaluate the antifungal activity of the best formula achieved, which showed the widest zone of inhibition as compared to FLZ reference. The studied microemulsion formulation showed a good stability for a period of 3 months. These results indicate that the studied microemulsion formulation might be a promising vehicle for topical delivery of FLZ.
Patel
Mrunali R
MR
Indukaka Ipcowala College of Pharmacy, Sardar Patel University, New Vallabh Vidyanagar 388 121, India. rashmru@gmail.com
Patel
Rashmin B
RB
Parikh
Jolly R
JR
Solanki
Ajay B
AB
Patel
Bharat G
BG
D000818:Animals; D000935:Antifungal Agents / Q000008:administration & dosage* / Q000494:pharmacology; D002176:Candida albicans / Q000187:drug effects; D002626:Chemistry, Pharmaceutical; D016503:Drug Delivery Systems; D004355:Drug Stability; D004553:Electric Conductivity; D004655:Emulsions; D005079:Excipients; D015725:Fluconazole / Q000008:administration & dosage* / Q000494:pharmacology; D006863:Hydrogen-Ion Concentration; D066298:In Vitro Techniques; D008297:Male; D008859:Microscopy, Polarization; D009821:Oils / Q000737:chemistry; D010316:Particle Size; D051381:Rats; D017208:Rats, Wistar; D012031:Refractometry; D012869:Skin Absorption; D012995:Solubility; D014783:Viscosity
D000935:Antifungal Agents; D004655:Emulsions; D005079:Excipients; D009821:Oils; D015725:Fluconazole