Effect of the structure of ginsenosides on the in vivo fate of their liposomes  

作　　者：Chen Chen Jiaxuan Xia Hongwei Ren Anni Wang Ying Zhu Ru Zhang Zicheng Gan Jianxin Wang 

机构地区：[1]Department of Pharmaceutics,School of Pharmacy,Fudan University&Key Laboratory of Smart Drug Delivery,Ministry of Education,Shanghai 201203,China [2]Institute of Tropical Medicine,Guangzhou University of Chinese Medicine,Guangzhou 510006,China [3]Institute of Integrated Chinese and Western Medicine,Fudan University,Shanghai 200040,China

出　　处：《Asian Journal of Pharmaceutical Sciences》2022年第2期219-229,共11页亚洲药物制剂科学（英文）

基　　金：supported by the National Natural Science Foundation of China (No. 82074277 and 81773911);the Development Project of Shanghai Peak Disciplines-Integrated Medicine (No. 20180101)

摘　　要：To utilize themultiple functions and give full play of ginsenosides,a variety of ginsenosides with different structures were prepared into liposomes and evaluated for their effect on the stability,pharmacokinetics and tumor targeting capability of liposomes.The results showed that the position and number of glycosyl groups of ginsenosides have significant effect on the in vitro and in vivo properties of their liposomes.The pharmacokinetics of ginsenosides liposomes indicated that the C-3 sugar group of ginsenosides is beneficial to their liposomes for longer circulation in vivo.The C-3 and C-6 glycosyls can enhance the uptake of their liposomes by 4T1 cells,and the glycosyls at C-3 position can enhance the tumor active targeting ability significantly,based on the specific binding capacity to Glut 1 expressed on the surface of 4T1 cells.According to the results in the study,ginsenoside Rg3 and ginsenoside Rh2 are potential for exploiting novel liposomes because of their cholesterol substitution,long blood circulation and tumor targeting capabilities.The results provide a theoretical basis for further development of ginsenoside based liposome delivery systems.

关 键 词：GINSENOSIDES Liposomes Structure activity relationship Rg3 liposomes Long circulation Tumor targeting Glut 1 

分 类 号：R285[医药卫生—中药学]