Voriconazole into PLGA nanoparticles: Improving agglomeration and antifungal efficacy

Abstract This study is concerned with preparing PLGA nanoparticles loaded with voriconazole (PNLV), investigating the burst release and agglomeration of PNLV, and also evaluating antifungal efficacy of PNLV compared with voriconazole (VRC). The emulsion–solvent evaporation technique for nanoparticles and tests against fungi were completed. The amount of VRC in PNLV with sodium hexametaphosphate was 2.01 ± 0.27%, and burst release of PNLV was reduced by about 33% using 20% ethanol solution ( n  = 3). The mean D 50 of PNLV with or without this salt was 132.8 nm and 6.3 μm, respectively ( n  = 5). In vitro ; the fungal numbers treated with PNLV (3.5 mg/ml, equal amount calculated by VRC) and VRC (70 μg/ml) in tubes at the day 7 were 5.74 log 10 and 6.72 log 10 , respectively ( P In vivo ; the fungal burden treated with PNLV and VRC in tissue from mice kidneys at day 7 after administration was 0.64 log 10 and 2.61 log 10 , respectively (5 mg/kg, P