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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。
Two different lipid-lipid ratio vinflunine tartrate-loaded liposomes (VT-L) were prepared by pH gradient method. The particle size distribution and zeta potential of liposomes were investigated by laser particle size analyzer. The entrapment efficiency was determined by cation exchange resin-centrifugation method. Compared with vinflunine tartrate injection (VT-I) Different drug-lipid ratio of VT-L on tumor inhibition and toxicity in nude mice. The results showed that the average particle size of VT-L with lipid-lipid ratios of 1: 5 and 1:10 were 124.6 and 128.3 nm, respectively. The zeta potentials were -25.3 and -22.8 mV, respectively, and the entrapment efficiencies were 94.46% and 97.31%, respectively. The antitumor effect of VT-L with two drug-lipid ratios on human non-small cell lung cancer A549 xenografted nude mice was significantly better than that of VT-I and lower than that of VT-I. The antitumor effect and toxicity of VT-L with two drug-lipids were not significantly different.