In vitro and in vivo evaluation of didymin cyclodextrin inclusion complexes: characterization and chemosensitization activity

Drug Delivery

Longfa Kou¹  Meng-Ting Lin²  Yin-Di Zhu²  Zhi-Wei Huang²  Qing Yao²  Xue Jiang²  Ying-Zheng Zhao²  Ya-Wen Zheng²  Qing-Hua Lan²  He-Lin Xu² 

[1] Department of Pharmacy, The Second Affiliated Hospital and Yuying Children’s Hospital of Wenzhou Medical University, Wenzhou, Chin;School of Pharmaceutical Sciences, Wenzhou Medical University, Wenzhou, China;

关键词: Didymin;    inclusion complex;    multidrug resistance;    chemosensitization;    2-hydroxypropyl-β-cyclodextrin;   

DOI  :  10.1080/10717544.2019.1704941

来源: publisher

【 摘 要 】

Didymin is a dietary flavonoid that first found in citrus fruits, and possesses antioxidant properties. Our preliminary experiments first discovered that didymin was able to sensitize the resistant cancer cells against chemotherapeutics and combat multidrug resistance. However, its poor aqueous solubility and resultant low bioavailability limit its potentials as an adjuvant phytochemical drug for chemotherapy. Thus, this study prepared the inclusion complex of didymin with β-cyclodextrin and 2-hydroxypropyl-β-cyclodextrin to improve its bioavailability and then evaluate their chemosensitization effects. The didymin inclusion complexes formulation was prepared and their host-guest structure was characterized by FT-IR, PXRD, DSC, and SEM techniques. In vitro/in vivo results demonstrated that didymin inclusion complex enhanced its water solubility and orally bioavailability. Furthermore, didymin inclusion complex exerted considerable chemosensitivity potency, and improve the anti-tumor effects of chemotherapeutics in vivo. Therefore, didymin inclusion complex could provide a safe, effective, economical, and adjuvant drug for future treatment of chemoresistant cancers.

【 授权许可】

CC BY