酒石酸长春氟宁脂质体的体内外评价  

Characterization of vinflunine tartrate liposomes in vitro and in vivo

作　　者：邹伟伟 王栋海 孙春艳 韩景宾 尹青 杨清敏 王晶翼 

机构地区：[1]山东省注射用微粒给药新技术重点实验室,山东济南250100 [2]齐鲁制药有限公司药物研究院,山东济南250100

出　　处：《药学学报》2011年第12期1515-1519,共5页Acta Pharmaceutica Sinica

基　　金：国家重大新药创制科技重大专项资助项目(2010ZX09401-302-4-2)

摘　　要：采用pH梯度法制备两种不同药脂比的酒石酸长春氟宁脂质体(vinflunine tartrate-loaded liposomes,VT-L)。运用激光粒度仪考察了脂质体的粒径分布和zeta电位;阳离子交换树脂-离心法测定了包封率;以酒石酸长春氟宁注射液(vinflunine tartrate injection,VT-I)为对照,比较了不同药脂比的VT-L对裸鼠体内肿瘤抑制和毒性的情况。结果显示,药脂比为1∶5和1∶10的VT-L平均粒径分别为124.6和128.3 nm,zeta电位分别为-25.3和-22.8 mV,包封率分别为94.46%和97.31%。两种药脂比的VT-L对人非小细胞肺癌A549裸鼠移植瘤的抗瘤效应明显优于VT-I,毒性低于VT-I。而两种药脂比的VT-L的抗瘤效应和毒性无显著差别。Vinflunine tartrate-loaded liposomes（VT-L） with two drug-to-lipid ratios were prepared by pH gradient method.Vesicle size and zeta potential were determined by the Zetasizer Nano ZS.Entrapment efficiency was evaluated by cation exchange resin centrifugalization method.The toxicity and tumor inhibition to nude mouse administrated by VT-L with different drug-to-lipid ratios were investigated and compared with the vinflunine tartrate injection（VT-I）.The results showed that the mean particle size,zeta potential and entrapment efficiency of the VT-L with drug-to-lipid ratios of 1∶5 and 1∶10 were 124.6 nm and 128.3 nm,-25.3 mV and -22.8 mV,94.46% and 97.31%,respectively.The VT-L with two different drug-to-lipid ratios has significantly higher anti-tumor effect to nude mouse transplanted human non-small cell lung carcinoma A549 and lower toxicity than VT-I.While there were no significant differences in anti-tumor effect and toxicity between VT-L with two different drug-to-lipid ratios.

关 键 词：酒石酸长春氟宁 脂质体 包封率 毒性 

分 类 号：R943[医药卫生—药剂学]