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ACTA Pharmaceutica Sciencia
2025 , Vol 63 , Num 4
Improving the antifungal activity of itraconazole by solid dispersi
1 Mustansiriyah University, College of Pharmacy, Department of Pharmaceutics, Baghdad, Iraq2 Mustansiriyah University, College of Pharmacy, Department of Clinical Laboratory Science, Baghdad, Iraq
DOI : 10.23893/1307-2080.APS6355 Viewed : 73 - Downloaded : 21 Itraconazole (ITZ), a potent antifungal agent, suffers from poor water solubility and limited bioavailability, hindering its therapeutic effectiveness, particularly in the treatment of vaginal candidiasis. This study aimed to enhance the solubility, dissolution rate, and antifungal efficacy of ITZ through the formulation of solid dispersions (SDs) using hydrophilic polymers (Polyvinylpyrrolidone {PVP} K30, hydroxypropyl methylcellulose E5 {HPMC E5}, and Soluplus) via physical mixing and solvent evaporation techniques. Characterization was done by Differential Scanning Calorimetry, Powder X-ray Diffraction, and Fourier Transform Infrared Spectroscopy, which confirmed reduced crystallinity and improved drug-polymer interactions, especially in the ITZ-PVP K30 system prepared by solvent evaporation (RE). Furthermore, saturated solubility, dissolution study, and antifungal activity were performed. Then the optimized formulation was further developed into PEG-based vaginal suppositories with full evaluation test. Among all formulations, ITZ-PVP K30 RE exhibited the highest solubility (527.34 µg/mL), superior dissolution (91.18% at 120 minutes), and the greatest antifungal activity (25 mm inhibition zone) against Candida albicans. Evaluation demonstrated acceptable physicochemical properties, optimal drug release (96.4% with 10% glycerin), and enhanced antifungal efficacy (30 mm inhibition zone). This novel ITZ-PVP K30 mixture suppository formulation presents a promising alternative for the localized treatment of vaginal candidiasis with improved efficacy and patient compliance. Keywords : itraconazole, Candida albicans, solid dispersion, vaginal candidiasis