Abstract

FORMULATION AND EVALUATION OF POSACONAZOLE-LOADED NANOPARTICLES FOR TOPICAL DRUG DELIVERY SYSTEM

S. Selvaraj*, V. Amarnath, P. Perumal

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Abstract

Nanostructured drug delivery systems offer significant advantages in improving the efficacy of therapeutics by enhancing drug solubility, controlling release, and reducing required doses. The nanoparticles were formulated under 9 different concentrations by emulsification method. From that best formulated nanoparticles F4 will be selected for the nanogel formulation based on the invitro dissolution studies. This study explores the development of posaconazole-loaded nanoparticles (PNPs) incorporated into a nanogel formulation, utilizing TPGS as a permeation enhancer for enhanced antifungal activity. Posaconazole nanoparticles were prepared using an electrostatic stabilization method and characterized for size (70.89–144.5 nm), zeta potential (-26.9 to 1.86), and polydispersity index (PDI 0.284–0.700). The nanoparticles exhibited improved solubility and dissolution rate compared to the pure drug, which showed limited release (41.5% in 0.1 N HCl). The nanoparticle formulations demonstrated a controlled, biphasic drug release profile, with an initial burst phase followed by sustained release, indicating diffusion and degradation-based mechanisms. DSC and FTIR analysis revealed that posaconazole was molecularly dispersed in an amorphous form within the nanoparticles, ensuring no significant interactions with excipients. The nanoparticles were further incorporated into a nanogel formulation with Carbopol 940 as a polymer matrix, showing uniform spreadability, controlled diffusion, and no irritation upon testing. The formulation showed excellent biocompatibility and enhanced antifungal activity. These results suggest that the nanoparticle-based delivery system significantly improves the solubility, stability, and controlled release of posaconazole, offering a promising solution for the treatment of chronic fungal infections. This study highlights the potential of nanotechnology in overcoming the limitations of poorly soluble drugs, particularly BCS class-II drugs.

Keywords: Posaconazole, Nanoparticle, in-vitro evaluation, hydrogel, poor soluble drug.