"Enhancing the solubility of ketoconazole: formulation, development of melt-spun dispersions using sucrose and lactose as carriers"

Abstract

Ketoconazole is a poorly water-soluble antifungal agent with limited bioavailability, which poses challenges in attaining effective therapeutic levels. This study focused on enhancing the solubility of ketoconazole using centrifugal melt spinning, a novel formulation technique. During this process, ketoconazole was exposed to centrifugal forces in its molten state, resulting in the formation of amorphous solid dispersions. In this formulation approach, ketoconazole was incorporated into amorphous solid dispersions using centrifugal melt spinning. The process involved subjecting the drug to centrifugal forces during melting, facilitating its dispersion within a hydrophilic matrix. Microfibers containing 10% w/w ketoconazole were successfully prepared using sucrose as the carrier, enabling the formation of stable amorphous fibers potentially enhancing solubility and dissolution rate. n comparison, the drug-loaded microfibers prepared with sucrose and lactose exhibited markedly faster release rates, achieving 94.98 ± 0.61% and 91.47 ± 0.52% respectively, within the same time period. This enhanced release is attributed to the increased surface area of the fibers relative to that of conventional tablet formulations.