Cleavable PEG modified paclitaxel loaded liposome for tumor targeting and therapy
10.3760/cma.j.issn.1673-4181.2014.03.004
- VernacularTitle:可断裂PEG修饰脂质体的制备及其抗肿瘤研究
- Author:
Zhiqiang LI
;
Hai SUN
;
Xiaoming DENG
;
Fengshen ZHANG
- Publication Type:Journal Article
- Keywords:
Cleavable polyethylene glycol;
Liposome;
Tumor
- From:
International Journal of Biomedical Engineering
2014;37(3):143-147,后插5
- CountryChina
- Language:Chinese
-
Abstract:
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.