Formulation And Evaluation of Spray-Dried Ternary Solid Dispersions of Amorphous Itraconazole

Abstract

Although it is extensively utilized to treat both systemic and superficial fungal infections, the therapeutic efficacy of itraconazole is severely constrained due to its extremely low oral bioavailability and extremely poor water solubility. The purpose of this research was to create and assess amorphous itraconazole spray-dried ternary solid dispersions with improved solubility properties by means of hydrophilic carriers such as polyvinylpyrrolidone K30 (PVP K30) and Sylysia® 350. The melt-quench process was used to create the amorphous itraconazole, which was then spray-dried into binary and ternary solid dispersions. The drug content was adequate in all formulations, indicating that the spray drying process was effective in incorporating the medicine. Pure crystalline itraconazole, amorphous itraconazole, and binary solid dispersions all performed poorly in comparison to the ternary solid dispersion containing PVP K30 and Sylysia® 350 (F3), which achieved the best dissolution performance. Amorphization, greater wettability, increased surface area, drug molecular dispersion, and the synergistic action of the hydrophilic polymer and porous silica carrier were all factors in the enhanced solubility.