The anti-tumor performance of docetaxel liposomes surface-modified with glycyrrhetinic acid

Journal of Drug Targeting
Jie LiJilai Tian

Abstract

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. 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. 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. 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 a...Continue Reading

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Citations

Apr 9, 2014·International Journal of Pharmaceutics·Yinghuan LiGuohui Cui
May 11, 2015·Journal of Controlled Release : Official Journal of the Controlled Release Society·Elisabete FernandesLúcio Lara Santos
Oct 19, 2016·Journal of Controlled Release : Official Journal of the Controlled Release Society·Mona AlibolandiMohammad Ramezani
Feb 19, 2019·Expert Opinion on Drug Delivery·Enhui ZhangPengcheng Li
Sep 7, 2018·Experimental and Therapeutic Medicine·Jing ZhuWei Wu

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