Glycyrrhetinic acid-modified TPGS polymeric micelles for hepatocellular carcinoma-targeted therapy

作者: Xiumei Zhu , Altansukh Tsend-Ayush , Zhongyue Yuan , Jing Wen , Jiaxin Cai

DOI: 10.1016/J.IJPHARM.2017.07.011

关键词:

摘要: In this study, glycyrrhetinic acid (GA)-modified D-α-tocopheryl polyethylene glycol 1000 succinate (TPGS) polymeric micelles (TGA PMs) were developed for the delivery of etoposide (ETO) to hepatoma cells. GA was incorporated as a ligand because its high affinity hepatocytes, while TPGS functioned P-gp inhibitor reverse multidrug resistance. ETO-loaded TGA PMs (ETO-TGA displayed mean particle size 133.6±1.2nm with low poly-dispersity index (0.224±0.013) and negative zeta potential (-16.30mV). The drug loading entrapment efficiency ETO-TGA 10.4% 79.8%, respectively. also exhibited faster release behavior at pH 5.8 relatively stable 7.4. Confocal laser scanning microscope (CLSM) observations in vivo imaging studies revealed that higher cellular uptake selective accumulation tumor site, indicating good targetability. Furthermore, significant cytotoxicity towards HepG2 cells anti-tumor efficacy (75.96%), compared control group. This could be due TGA-mediated targeted hepatocytes well inhibition. These findings suggest have used system hepatic cancer therapy.

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