Cleavable PEG modified paclitaxel loaded liposome for tumor targeting and therapy

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Objective To prepared cleavable PEG modified paclitaxel loaded liposome （CLP-PTX） and to study its capability for tumor targeting.Methods Liposome was prepared by film-ultrasonic method.Cellular uptake by HepG2 cells was explored.The anti-proliferation efficiency of CLP-PTX was evaluated by MTF assay.HepG2 cells were xenografted in athymic nude mice to establish the animal models,which were used to evaluate the anti-cancer effect.Results The mean size of CLP-PTX was （95±9.5） nm with the Zeta potential of （-3±1.05） mV,and the entrapment efficiency of PTX was 85.6%.The cellular uptake of liposomes with addition of cysteine （Cys）was 2.8 times as high as that in the absence of Cys,and the difference was statistically significant （P〈0.01）.Fluorescent microscopy qualitative observation demonstrated that the cells showed higher fluorescence intensity in the presence of Cys.The MTT assay showed the anti-proliferative activity against HepG2 cells of CLP-PTX depended on the paclitaxel concentration,and the inhibition ratio of CLP-PTX with addition of Cys was 1.6 times as high as that in the absence of Cys （P〈0.01）,which was consistent with the cellular uptake results.Conclusions Comparing with paclitaxel,CLP-PTX inhibited the proliferation of HepG2 cells more persistently.Thus,CLP-PTX,as a new nanometer drug,has a special application value for tumor therapy. Key words: Cleavable polyethylene glycol; Liposome; Tumor