Itraconazole-loaded poly(lactic-co-glycolic) acid nanoparticles for improved antifungal activity

Aims: 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. Materials & methods: 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. Results: 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 x 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. Conclusion: 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.