基于共晶工程的基黄酮的溶解度和生物利用度的优化。
Optimized solubility and bioavailability of genistein based on cocrystal engineering.
发表日期:2023 Sep 13
作者:
Zhipeng Wang, Qi Li, Qi An, Lixiang Gong, Shiying Yang, Baoxi Zhang, Bin Su, Dezhi Yang, Li Zhang, Yang Lu, Guanhua Du
来源:
DIABETES & METABOLISM
摘要:
基于配合物工程的概念,在溶剂辅助下通过研磨法制备了基黄酮和哌嗪的共晶体,以改善基黄酮的溶解度和生物利用度。通过单晶X射线衍射、粉末X射线衍射、傅里叶变换红外光谱、差示扫描量热法和热重分析等一系列分析技术对共晶体进行了表征和确认。然后,基于理论计算进行了结构分析,并对稳定性、溶解度和生物利用度进行了评价。结果表明,基黄酮和哌嗪的共晶体改善了基黄酮的溶解度和生物利用度。与之前基黄酮共晶体研究相比,本研究系统而全面地从制备、表征、结构分析、稳定性、溶解度和生物利用度评估等方面进行了调查。作为一种简单、高效、环保的方法,配合物工程为优化天然产物的药物特性提供了新的途径,以实现成功的药物配方和输送。© 2023. 中国科学院昆明植物研究所。
With various potential health-promoting bioactivities, genistein has great prospects in treatment of a series of complex diseases and metabolic syndromes such as cancer, diabetes, cardiovascular diseases, menopausal symptoms and so on. However, poor solubility and unsatisfactory bioavailability seriously limits its clinical application and market development. To optimize the solubility and bioavailability of genistein, the cocrystal of genistein and piperazine was prepared by grinding assisted with solvent based on the concept of cocrystal engineering. Using a series of analytical techniques including single-crystal X-ray diffraction, powder X-ray diffraction, Fourier transform infrared spectroscopy, differential scanning calorimetry and thermogravimetric analysis, the cocrystal was characterized and confirmed. Then, structure analysis on the basis of theoretical calculation and a series of evaluation on the stability, dissolution and bioavailability were carried out. The results indicated that the cocrystal of genistein and piperazine improved the solubility and bioavailability of genistein. Compared with the previous studies on the cocrystal of genistein, this is a systematic and comprehensive investigation from the aspects of preparation, characterization, structural analysis, stability, solubility and bioavailability evaluation. As a simple, efficient and green approach, cocrystal engineering can pave a new path to optimize the pharmaceutical properties of natural products for successful drug formulation and delivery.© 2023. Kunming Institute of Botany, CAS.