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Itraconazole-Loaded Poly(Lactic- Co -Glycolic) Acid Nanoparticles for Improved Antifungal Activity

2010; Future Medicine; Volume: 5; Issue: 7 Linguagem: Inglês

10.2217/nnm.10.68

1748-6963

Nipur R Patel, K. E. Damann, Claudia Leonardi, Cristina M. Sabliov,

Microencapsulation and Drying Processes

Poly(lactic-co-glycolic) acid (PLGA) nanoparticles containing the hydrophobic antifungal itraconazole (ITZ) were developed to address the need for more effective means of treating fungal infections.PLGA-ITZ nanoparticles were synthesized using an oil-in-water emulsion evaporation method. Nanoparticle morphology (studied by transmission electron microscopy), size zeta potential (dynamic light scattering), encapsulation efficiency (UV-visible spectroscopy), release profile and antifungal activity were characterized.PLGA-ITZ nanoparticles (of 220 nm in diameter) completely inhibited Aspergillus flavus growth over 11 days at 0.03 mg/ml ITZ; a similar effect was achieved at ×100 ITZ concentrations (3 mg/ml) in emulsified form. The ITZ in water formulation had the least antifungal effect, inhibiting growth for only 2 days at 3 mg/ml ITZ.This system is envisioned to increase bioavailability of ITZ by improving aqueous dispersibility and increasing antifungal penetration, thereby increasing antifungal activity of the entrapped drug.