title: Microemulsions as vehicles for topical administration of voriconazole: formulation and in vitro evaluation.
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.
authors.affiliation: Department of Pharmaceutics and Industrial Pharmacy, College of Pharmacy, Misr University for Science and Technology, 6th of October City, Egypt.
authors.forename: Gladious Naguib
authors.initials: GN
authors.lastname: El-Hadidy
authors.forename: Howida Kamal
authors.initials: HK
authors.lastname: Ibrahim
authors.forename: Magdi Ibrahim
authors.initials: MI
authors.lastname: Mohamed
authors.forename: Mohamed Farid
authors.initials: MF
authors.lastname: El-Milligi
mesh_terms: D000287:Administration, Topical; D000818:Animals; D000935:Antifungal Agents / Q000737:chemistry; D002626:Chemistry, Pharmaceutical; D003840:Deoxycholic Acid / Q000737:chemistry*; D004337:Drug Carriers / Q000737:chemistry; D004355:Drug Stability; D004655:Emulsions / Q000737:chemistry; D006168:Guinea Pigs; D006863:Hydrogen-Ion Concentration; D019301:Oleic Acid / Q000737:chemistry*; D010539:Permeability; D010938:Plant Oils / Q000737:chemistry; D011092:Polyethylene Glycols / Q000737:chemistry; D011136:Polysorbates / Q000737:chemistry; D011743:Pyrimidines / Q000008:administration & dosage* / Q000737:chemistry*; D012212:Rheology / Q000379:methods; D012995:Solubility; D013501:Surface-Active Agents / Q000737:chemistry; D014230:Triazoles / Q000008:administration & dosage* / Q000737:chemistry*; D065819:Voriconazole; D014867:Water / Q000737:chemistry; D014885:Waxes / Q000737:chemistry
chemical_list: D000935:Antifungal Agents; D004337:Drug Carriers; D004655:Emulsions; D010938:Plant Oils; D011136:Polysorbates; D011743:Pyrimidines; D013501:Surface-Active Agents; D014230:Triazoles; D014885:Waxes; D003840:Deoxycholic Acid; D014867:Water; D019301:Oleic Acid; D011092:Polyethylene Glycols; C034743:jojoba wax; C033084:polyethylene glycol oleyl ether; D065819:Voriconazole