Solubility Enhancement of Itraconazole by Centrifugal Melt Spinning Technique

Abstract

Itraconazole is an antifungal drug with poor water solubility and limited bioavailability, presenting difficulties in achieving effective therapeutic applications. This study aimed to employ centrifugal melt spinning, an innovative method, to improve the solubility of itraconazole. In this process, itraconazole was subjected to centrifugal forces while melting, forming amorphous solid dispersions. Microfibers loaded with 10% w/w itraconazole were prepared through centrifugal melt spinning, employing sucrose as a carrier. ITZ-sucrose microfibers with uniform morphology and an average diameter of 14.27 ± 2.90 μm were successfully fabricated, as evidenced by the scanning electron microscopy results. XRD and DSC measurements confirmed the amorphous nature of the spun microfibers. The solubility of Itraconazole sucrose microfibers was significantly enhanced by 17-fold compared to plain itraconazole. The dissolution experiments demonstrated that sucrose microfibers loaded with ITZ achieved a significant release of 94.96 ± 1.47% within 10 minutes, representing a substantial enhancement compared to plain drugs. The study indicated that utilizing the centrifugal melt spinning technique successfully generated amorphous solid dispersions of itraconazole, leading to a considerable improvement in the drug’s solubility.