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The anti-tumor performance of docetaxel liposomes surface-modified with glycyrrhetinic acid
1Department of Pharmaceutics, State Key Laboratory of Natural Medicines, China Pharmaceutical University, Nanjing, China.
Purpose:
Anti-tumor performance of docetaxel liposomes surface-modified with glycyrrhetinic acid (GA-DX-Lip) as a new hepatocytes-targeted delivery vehicle was investigated, unmodified docetaxel liposome (DX-Lip) was chosen as a comparison.
Methods:
GA-DX-Lip was prepared by film dispersion method. The physicochemical properties were characterized. The cellular uptake mechanism of GA-modified liposomes was studied in hepatocytes and nonparenchymal cells. Pharmacokinetics and the anti-tumor activity in vitro and in vivo of GA-DX-Lip were investigated.
Results:
The size of GA-DX-Lip was about 90 nm with negative charge and the entrapment efficiency was more than 95%. GA-modified liposomes had the specific receptor-mediated cellular endocytosis to hepatocytes, and the uptake ratio of hepatocytes to nonparenchymal cells was 2.28 times. The tumor inhibitory ratio of GA-DX-Lip in vitro was 2.03 times of DX-Lip, the T/C of GA-DX-Lip was 20.14%, better than the 33.27% of DX-Lip. There was no obvious difference in pharmacokinetics parameters.
Discussion And Conclusion:
The preliminary cellular uptake test showed the receptor-mediated endocytosis and enhanced hepatocytes-target for GA-modified liposomes. Compared with the unmodified liposome, GA-DX-Lip possessed better anti-tumor activity and unchanged pharmacokinetic behavior. The present results suggest that the GA-modified liposomes may be a promising delivery system for hepatocytes-target.
