Preparation of hesperetin nanocrystals: effect of solid state and particle morphology on the particle size reduction efficiency / 中国药学杂志

ABSTRACT

OBJECTIVE: Drug properties have important effect on the drug nanosuspenions/nanocrystal production and can determine the final particle size and production efficiency. A number of papers have referred to the optimizations of processes expecting the smaller achievable particle sizes as well as increased production efficiency. Aspects such as stabilizer selection are those most commonly described in the literature. The aims of this study are to systematically investigate the mechanism of nanocrystal formation and identify the physical properties that can affect the particle size reduction process. METHODS: The influence of drug properties such as degree of crystallinity and particle morphology on particle size reduction was systematically investigated by producing hesperetin as a model drug. Processes ie spray-drying, rotavapor, and quench-cooling were applied to modify the physical properties of hesperetin. Both unmodified drugs and modified drugs were used for production of nanosuspension. RESULTS: The nanosuspension with the smallest particle size was obtained from spray-dried hesperetin. CONCLUSION: An improved crystal morphology of modified starting material obtained through spray-drying may lead to a more efficient homogenization process. The drug exists in the nanosuspensions as crystalline, which means recrystallization has occurred as a result of the high pressure homogenization process.