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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.
Insights
Liposomal fluconazole, particularly multilamellar vesicles (MLV), shows enhanced antifungal activity against Candida species compared to large unilamellar vesicles (LUV). This formulation demonstrates potential for improved drug delivery in antifungal treatments.
Area of Science:
- Pharmaceutical Sciences
- Drug Delivery Systems
- Antimicrobial Research
Background:
- Fluconazole is a widely used antifungal azole, but its delivery can be optimized.
- Liposomes offer a promising platform for encapsulating and delivering water-soluble drugs like fluconazole.
- Understanding the comparative efficacy of different liposomal formulations is crucial for therapeutic development.
Purpose of the Study:
- To evaluate the incorporation and stability of fluconazole within multilamellar vesicles (MLV) and large unilamellar vesicles (LUV).
- To assess the in vitro antifungal activity of liposomal fluconazole formulations against various Candida species.
- To compare the efficacy of MLV-encapsulated fluconazole with LUV-encapsulated and free fluconazole.
Main Methods:
- Successful incorporation of fluconazole into MLV and LUV liposomes.
- Stability assessment of liposomes in saline and a high-resolution medium over 72 hours.
- In vitro antifungal activity testing using minimum inhibitory concentration (MIC) assays against Candida pseudotropicalis, C. albicans, C. kefyr, and C. parapsilosis.
- Incubation time-dependent assays were performed against C. tropicalis.
Main Results:
- Both MLV and LUV liposomes exhibited stability in saline for up to 72 hours, but showed reduced stability in a high-resolution medium.
- MLV-entrapped fluconazole demonstrated significantly higher activity (4-fold against C. pseudotropicalis, >6-fold against C. albicans) compared to LUV-entrapped fluconazole.
- MLV-fluconazole showed comparable or enhanced activity against specific Candida strains compared to free fluconazole, with variations observed in incubation time-dependent assays.
- The liposomal formulation proved useful in the in vitro assay method.
Conclusions:
- Liposomal encapsulation, particularly in MLV, enhances the in vitro antifungal efficacy of fluconazole against key Candida species.
- The stability of liposomal fluconazole is dependent on the medium, with better performance in saline.
- These findings highlight the potential of liposomal fluconazole as an improved therapeutic strategy for fungal infections.