AIMS: Itraconazole and coumarin-6 loaded polylactic-co-glycolic acid-nanoparticles (PLGA-ITZ- and PLGA-C6-NPs) were synthesized and tested for fungal cell uptake and antifungal ability based on particle size. MATERIALS & METHODS: PLGA-ITZ- and PLGA-C6-NPs were synthesized using an oil-in-water emulsion evaporation method. Fungal cell uptake and antifungal activity of the polymeric NPs was tested on Aspergillus flavus. RESULTS: PLGA-C6-NPs of 203 nm associated with fungal cell surfaces and internalized efficiently, while 1206 nm NPs associated with cell surfaces were internalized less efficiently. Antifungal studies of PLGA-ITZ-NPs of 232, 630 and 1060 nm showed differences in inhibitory activity with 232 nm NPs showing superior activity at the lowest ITZ concentration of 0.003 mg/ml, followed by 630 and 1060 nm NPs. No differences in antifungal activity were observed at higher ITZ concentrations. CONCLUSION: The PLGA-ITZ-NP system can increase bioavailability of ITZ by improving its aqueous dispersibility and efficiently delivering ITZ to fungal cells via endocytosis.
AIMS: Itraconazole and coumarin-6 loaded polylactic-co-glycolic acid-nanoparticles (PLGA-ITZ- and PLGA-C6-NPs) were synthesized and tested for fungal cell uptake and antifungal ability based on particle size. MATERIALS & METHODS: PLGA-ITZ- and PLGA-C6-NPs were synthesized using an oil-in-water emulsion evaporation method. Fungal cell uptake and antifungal activity of the polymeric NPs was tested on Aspergillus flavus. RESULTS: PLGA-C6-NPs of 203 nm associated with fungal cell surfaces and internalized efficiently, while 1206 nm NPs associated with cell surfaces were internalized less efficiently. Antifungal studies of PLGA-ITZ-NPs of 232, 630 and 1060 nm showed differences in inhibitory activity with 232 nm NPs showing superior activity at the lowest ITZ concentration of 0.003 mg/ml, followed by 630 and 1060 nm NPs. No differences in antifungal activity were observed at higher ITZ concentrations. CONCLUSION: The PLGA-ITZ-NP system can increase bioavailability of ITZ by improving its aqueous dispersibility and efficiently delivering ITZ to fungal cells via endocytosis.
Authors: Aline Raquel Voltan; Guillermo Quindós; Kaila P Medina Alarcón; Ana Marisa Fusco-Almeida; Maria José Soares Mendes-Giannini; Marlus Chorilli Journal: Int J Nanomedicine Date: 2016-08-08