Optimized solubility and bioavailability of genistein based on cocrystal engineering

Natural Products and Bioprospecting

Original Article

Guanhua Du¹  Baoxi Zhang²  Yang Lu²  Dezhi Yang²  Shiying Yang²  Zhipeng Wang²  Qi An²  Qi Li²  Lixiang Gong²  Li Zhang²  Bin Su³ 

[1] Beijing City Key Laboratory of Drug Target and Screening Research, National Center for Pharmaceutical Screening, Institute of Materia Medica, Chinese Academy of Medical Sciences and Peking Union Medical College, 100050, Beijing, People’s Republic of China;Beijing City Key Laboratory of Polymorphic Drugs, Center of Pharmaceutical Polymorphs, Institute of Materia Medica, Chinese Academy of Medical Sciences and Peking Union Medical College, 100050, Beijing, People’s Republic of China;Shandong Soteria Pharmaceutical Co., Ltd., 271100, Laiwu, China;

关键词: Genistein;    Piperazine;    Cocrystal;    Solubility;    Bioavailability;   

DOI  :  10.1007/s13659-023-00397-w

 received in 2023-08-11, accepted in 2023-09-03,  发布年份 2023

来源: Springer

【 摘 要 】

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.Graphical Abstract

【 授权许可】

CC BY   
© Kunming Institute of Botany, CAS 2023

【 图 表 】

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