title: Preparations of liposomal fluconazole and their in vitro antifungal activity.
abstract: Fluconazole was successfully incorporated into multilamellar (MLV) and large unilamellar liposomes (LUV). Both MLV and LUV were stable up to 72 h in saline but were less stable in the high-resolution medium. The MLV-entrapped fluconazole was found to be four-fold more active than LUV-entrapped fluconazole against Candida pseudotropicalis and over six-fold more active against C. albicans. The MLV-fluconazole was one-fold less active than free fluconazole in terms of its endpoints (MIC value). However, when compared with free fluconazole, MLV-fluconazole was one-fold more active against two strains of C. albicans and equally active against C. kefyr and C. parapsilosis. In an incubation time-dependent assay against C. tropicalis, MLV-Fluconazole was one-fold more active after 16 h incubation and two-fold less active than fluconazole after 24 or 36 h post-incubation. Our results demonstrate the usefulness of liposomal formulation of the water-soluble azole, fluconazole, in the limited in vitro assay method used.
authors.affiliation: SynPhar Laboratories Inc., Taiho Alberta Centre, Edmonton, Canada.
authors.forename: M
authors.initials: M
authors.lastname: Singh
authors.forename: M P
authors.initials: MP
authors.lastname: Singh
authors.forename: S N
authors.initials: SN
authors.lastname: Maiti
authors.forename: A
authors.initials: A
authors.lastname: Gandhi
authors.forename: R G
authors.initials: RG
authors.lastname: Micetich
authors.forename: H
authors.initials: H
authors.lastname: Atwal
mesh_terms: D000935:Antifungal Agents / Q000008:administration & dosage / Q000494:pharmacology*; D002175:Candida / Q000187:drug effects; D002176:Candida albicans / Q000187:drug effects; D003470:Culture Media; D004337:Drug Carriers; D015725:Fluconazole / Q000008:administration & dosage / Q000494:pharmacology*; D007202:Indicators and Reagents; D008081:Liposomes; D008826:Microbial Sensitivity Tests; D010316:Particle Size
chemical_list: D000935:Antifungal Agents; D003470:Culture Media; D004337:Drug Carriers; D007202:Indicators and Reagents; D008081:Liposomes; D015725:Fluconazole