FORMULATION AND CHARACTERIZATION OF ITRACONAZOLE TABLETS FROM NANOSUSPENSION

Abstract

Itraconazole, a broad-spectrum antifungal agent, exhibits poor aqueous solubility, limiting its oral bioavailability. This study aimed to enhance the solubility and therapeutic efficacy of itraconazole by developing a nanosuspension-based tablet formulation for sustained release. The nanosuspension was prepared using the antisolvent precipitation method, followed by high-shear homogenization and ultrasonication. The optimized nanosuspension (F4) was spray-dried into nanogranules and compressed into tablets containing various polymers including HPMC K100, Carbopol 934, and Eudragit RL. The optimized formulation (F6) containing HPMC K100 demonstrated superior sustained release properties, achieving 99.27% drug release over 12 hours following zero-order kinetics. Characterization studies confirmed nanoscale particle size (307 nm), uniformity, and stability with a zeta potential of −30.5 ± 2.84 mV. The FTIR and DSC analyses indicated no significant drug–excipient interactions and confirmed thermal stability. The developed nanosuspension-based itraconazole tablet presents a promising approach for improving solubility, bioavailability, and sustained antifungal efficacy of poorly soluble drugs.