酒石酸长春瑞滨长循环热敏脂质体的荷瘤小鼠药效学研究

Pharmacodynamics of vinorelbine tartrate long-circulating thermosensitive liposomes in mice bearing Lewis lung carcinoma cells

目的评价酒石酸长春瑞滨长循环热敏脂质体(V-LCTL)对荷瘤小鼠的药效和不良反应。方法建立荷Lewis肺癌小鼠皮下肿瘤模型,静脉注射药品,比较V-LCTL与酒石酸长春瑞滨注射液(V-I)、酒石酸长春瑞滨长循环脂质体(V-LCL)的抗肿瘤作用,包括肿瘤生长曲线,抑瘤率,考察给药频率及量效关系。结果各治疗组均有抑瘤作用。相同剂量下V-LCTL的抑瘤效果明显强于V-LCL和V-I。单次给药和多次给药对V-LCTL和V-I的抑瘤率无显著影响。单次给药时不良反应明显。V-LCTL的抑瘤效果呈剂量依赖性(低、中、高剂量组抑瘤率分别为54.6%,72.1%,81.5%)。结论 V-LCTL具有比V-I和V-LCL更好的抑瘤效果,多次给药不良反应小,且V-LCTL的抑瘤效果具有剂量依赖关系。

Objective To investigate the tumor inhibition effect and toxicity of vinorelbine tartrate long-circulating ther- mosensitive liposome （V-LCTL） in mice bearing Lewis lung carcinoma cells. Methods A model of tumor-bearing mice was established by subcutaneous injection of Lewis lung cancer cells. The drag solution was intravenously administered to compare the anti-tumor effect of V-LCTL ,vinorelbine tartrate long-circulating liposome （V-LCL） and vinorelbine tartrate injection （V-I）. The tumor growth curve was obtained and the tumor inhibitory rate was calculated. The frequency of ad- ministration and dose-effect relat：~onship of V-LCTL were systematically investigated. Results Each administered group showed inhibition effect on the growth of tumor. The inhibition effect of V-LCTL was better than that of V-LCL group and V- I group, respectively. Two methods of administration showed no significant difference in the inhibition rate of V-LCTL and V-I, but the toxicity and side effect of mice treated by single administration of 30 mg/kg were increased. There was a dose- effect relationship in the treatment of V-LCTL（54.6%, 72. 1%, and 81.5% in its low, medium and higher dose sub- groups）. Conclusion The inhibitory efficiency of V-LCTL is better than that of V-I and V-LCL. Three-time administration of V-LCTL decreases the toxicity and side effect. Th~ tumor inhibitory effect of V-LCTL is positively correlated with the dose.