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  • Microemulsions as vehicles for topical administration of voriconazole: formulation and in vitro evaluation.

Microemulsions as vehicles for topical administration of voriconazole: formulation and in vitro evaluation.

Drug development and industrial pharmacy (2011-06-24)
Gladious Naguib El-Hadidy, Howida Kamal Ibrahim, Magdi Ibrahim Mohamed, Mohamed Farid El-Milligi
ABSTRACT

This work was undertaken to investigate microemulsion (ME) as a topical delivery system for the poorly water-soluble voriconazole. Different ME components were selected for the preparation of plain ME systems with suitable rheological properties for topical use. Two permeation enhancers were incorporated, namely sodium deoxycholate or oleic acid. Drug-loaded MEs were evaluated for their physical appearance, pH, rheological properties and in vitro permeation studies using guinea pig skin. MEs based on polyoxyethylene(10)oleyl ether (Brij 97) as the surfactant showed pseudoplastic flow with thixotropic behavior and were loaded with voriconazole. Jojoba oil-based MEs successfully prolonged voriconazole release up to 4 h. No significant changes in physical or rheological properties were recorded on storage for 12 months at ambient conditions. The presence of permeation enhancers favored transdermal rather than dermal delivery. Sodium deoxycholate was more effective than oleic acid for enhancing the voriconazole permeation. Voriconazole-loaded MEs, with and without enhancers, showed significantly better antifungal activity against Candida albicans than voriconazole supersaturated solution. In conclusion, the studied ME formulae could be promising vehicles for topical delivery of voriconazole.

MATERIALS
Product Number
Brand
Product Description

Sigma-Aldrich
BRIJ® O20, average Mn ~1,150
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Sigma-Aldrich
Jojoba oil from Simmondsia chinensis, tested according to DAC
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Sigma-Aldrich
Brij® O10
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Sigma-Aldrich
Brij® 93, average Mn ~357
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Sigma-Aldrich
ECO BRIJ® O20, average Mn ~1,150
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ECO BRIJ® O10
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