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.