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Preparation of cleavable PEG-modified liposome and its anti-tumor study



  A few days ago, Li Zhiqiang, Sun Hai, and Deng Xiaoming of the Hepatobiliary Surgery of the 324th Hospital of the People's Liberation Army published a paper to prepare a PEG-modified paclitaxel-loaded liposome (CLP-PTX) to investigate its anti-tumor ability in vitro. Studies have shown that CLP-PTX is more efficiently taken up by HepG2 cells after PEG cleavage and has a stronger inhibitory effect on tumor cell proliferation. This article was published in the 2014 issue of International Journal of Biomedicine.

  CLP-PTX was prepared by membrane dispersion method. The uptake rate of liposome in hepatocellular carcinoma HepG2 cells before and after PEG fragmentation was investigated by flow cytometry. The proliferation inhibition rate of liposome on HepG2 cells was studied by MTT assay.

  The particle size of CLP-PTX is (95±9.5) nm, the zeta potential is (-3±1.05) mV, and the encapsulation efficiency of paclitaxel is 85.6%. After adding the reducing agent cysteine (Cys), HepG2 cells are treated with PEG. The liposome uptake rate after rupture was significantly higher than that before rupture. The liposome uptake after PEG cleavage was 2.8 times that before rupture, and the difference was statistically significant (P<0.01). The fluorescence uptake was used to qualitatively observe cell uptake. The fluorescence intensity of PEG was significantly stronger than that before cleavage. The results of MTT assay showed that CLP-PTX inhibited the proliferation of HepG2 cells in a concentration-dependent manner, and the inhibition rate of HepG2 cells after PEG cleavage was 1.6 times that before rupture. Consistent with the results of the cellular uptake experiment, the difference was statistically significant (P < 0.01).