Abstract
Particle design in recent years has attempted to overcome solubility limitations in drug development. In this work, the particle microstructures of itraconazole (ITZ) were designed by a supercritical anti-solvent (SAS) process, with or without hydroxypropyl methylcellulose (HPMC) as the dispersing material, where the processing-microstructure-solubility relationship was investigated. The results showed that ITZ particles with different shapes and crystal forms were obtained, which enhanced the ITZ solubility from 4.4 μg/mL to 108.5 μg/mL. For the optimal sample, ITZ crystal transformed into amorphous state, resulting in high solubility and fast dissolution rate. Moreover, hydrogen bond interaction was formed between HPMC and ITZ, which could hinder the recrystallization of dissolved ITZ, resulting in its complete dissolution. Also, the production efficiency was increased to 38.5 mg ITZ/min, which laid a foundation for the scale-up. These results show the great potential of SAS process on the particle design of poorly soluble drugs for solubility enhancement.
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