PREPARATIONS OF LIPOSOMAL FLUCONAZOLE AND THEIR INVITRO ANTIFUNGAL ACTIVITY

Fluconazole was successfully incorporated into multilamellar (M 1,V) a nd 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 th an 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 equal ly active against C. kefyr and C. parapsilosis. In an incubation time- dependent assay against C. tropicalis, MLV-Fluconazole was one-fold mo re active after 16 h incubation and two-fold less active than fluconaz ole after 24 or 36 h post-incubation. Our results demonstrate the usef ulness of liposomal formulation of the water-soluble azole, fluconazol e, in the limited in vitro assay method used.