To utilize the multiple 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.
Keywords: Ginsenosides; Glut 1; Liposomes; Long circulation; Rg3 liposomes; Structure activity relationship; Tumor targeting.
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