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

Abstract

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.

Keywords::

• activity
• antifungal
• Aspergillus flavus
• GFP
• inhibition
• itraconazole
• nanoparticle
• petri plate
• poly(lactic-co-glycolic) acid

Financial & competing interests disclosure

The authors have no relevant affiliations or financial involvement with any organization or entity with a financial interest in or financial conflict with the subject matter or materials discussed in the manuscript. This includes employment, consultancies, honoraria, stock ownership or options, expert testimony, grants or patents received or pending, or royalties.

No writing assistance was utilized in the production of this manuscript.

Acknowledgements

The authors would like to thank Carlos Astete for sharing his valuable knowledge on nanoparticle synthesis, Cathy DeRobertis for her help with the fungal studies, and Mandy Lopez and the LECOR Laboratory of the LSU Veterinary School of Medicine for equipment use.

Additional information

Funding

The authors have no relevant affiliations or financial involvement with any organization or entity with a financial interest in or financial conflict with the subject matter or materials discussed in the manuscript. This includes employment, consultancies, honoraria, stock ownership or options, expert testimony, grants or patents received or pending, or royalties.