Formulation and Characterization of Novel Itraconazole-Loaded PLGA Nanoparticles for Potential Topical Delivery

Akar Othman Hamakarim; Twana Mohammed  Mohammed Ways

doi:10.54133/ajms.v9i2.2513

Authors

Akar Othman Hamakarim Department of Pharmaceutics, College of Pharmacy, University of Sulaimani, Sulaymaniyah 46001, Kurdistan Region, Iraq https://orcid.org/0009-0008-8888-7166
Twana Mohammed Mohammed Ways Department of Pharmaceutics, College of Pharmacy, University of Sulaimani, Kurdistan Region, Iraq https://orcid.org/0000-0002-7595-2159

DOI:

https://doi.org/10.54133/ajms.v9i2.2513

Keywords:

Itraconazole, Formulation Optimization, Polymeric Nanoparticles, PLGA 75:25

Abstract

Background: Itraconazole (ITZ) is a potent antifungal drug limited by poor water solubility and systemic side effects when taken orally. Topical administration offers a safer approach; however, efficient penetration through the stratum corneum remains a challenge. Objective: To develop and optimize ITZ-loaded PLGA nanoparticles (NPs) by investigating the effects of polymer type (PLGA 50:50 and 75:25) and stabilizers (Tween-80 and PVA) on the NPs size, PDI, and zeta potential, and to evaluate in vitro drug release of free ITZ and NPs. Methods: NPs were prepared by the nanoprecipitation method and were characterized using DLS for particle size, PDI, and zeta potential; FTIR spectroscopy for confirmation of drug encapsulation; FESEM and TEM for morphological assessment; and in vitro drug release studies. Results: All NP formulations were in the nano-size range. The optimal formulation, containing PLGA 75:25 and 1% Tween-80, had the smallest particle size and lowest PDI, with an encapsulation efficiency of 54.74%, a drug loading capacity of 8.46%, and a yield of 58.77%. FTIR spectroscopy confirmed successful incorporation of ITZ into the PLGA matrix, whereas FESEM and TEM revealed smooth, spherical NPs with uniform distribution and no aggregation. In vitro drug release studies of the NPs demonstrated a biphasic profile: an initial burst followed by a controlled release, as opposed to the rapid release of free ITZ. Conclusions: The NPs were successfully prepared. The optimized ITZ-loaded PLGA nanoparticles showed favorable physicochemical characteristics, efficient encapsulation, and controlled drug release, highlighting potential as a topical delivery system for antifungal therapy.

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