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 ×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.
Publication Source (Journal or Book title)
Nanomedicine (London, England)
Patel, N. R., Damann, K., Leonardi, C., & Sabliov, C. M. (2010). Itraconazole-loaded poly(lactic-co-glycolic) acid nanoparticles for improved antifungal activity. Nanomedicine (London, England), 5 (7), 1037-50. https://doi.org/10.2217/nnm.10.68