^(99m)TC-紫杉醇脂质体的抑瘤作用及体内分布研究

Studies of 99m Tc paclitaxel liposome:antitumor effect and biodistribution

目的：观察９９ｍＴＣ紫杉醇脂质体抑瘤作用及其体内分布，为临床应用提供依据。方法：采用逆相蒸发法制备紫杉醇脂质体，小鼠艾氏癌实体型为实验肿瘤模型。经腹腔分别注入生理盐水、紫杉醇注射液和紫杉醇脂质体，观察抑瘤率和体重变化率；经尾静脉分别注入９９ｍＴｃ紫杉醇脂质体和９９ｍＴｃＯ－４洗脱液观察体内分布情况。结果：紫杉醇脂质体与紫杉醇注射液两组抑瘤率差异无显著性；同生理盐水组相比，紫杉醇脂质体组的体重变化率无统计学意义，紫杉醇注射液组体重变化率有统计学意义，两组体重变化差异有显著性；９９ｍＴＣ紫杉醇脂质体主要分布于肝脾，同对照组相比，差异有显著性。结论：紫杉醇脂质体与紫杉醇注射液有相同的抗瘤活性，且降低了药物毒副作用９９ｍＴＣ紫杉醇脂质体主要分布于肝脾，对肿瘤无靶向性。

Purpose:To observe the antitumor activity and biodistribution of 99m Tc paclitaxel liposome.Methods:Paclitaxel liposome was prepared by reverse phase evaporation method. Ehrlich tumor xenografts in mice were established for studies.The weight changes of the mice and tumors weight,after injection of saline,paclitaxel, paclitaxel liposome via i.p.,were analyzed. 99m Tc labeled paclitaxel liposome and 99m TcO - 4 solution was injected through tail vein into the mice.Biodistribution was investigated under SPECT after 2hr,and the uptake rates of tumor,liver,spleen and lung were calculated.Results:The difference in antitumoractivity between the free and liposomal paclitaxel was not statistically significant,but weight changes were statistically significant.A high uptake was found in the liver and spleen.Conclusion:Free and liposomal paclitaxel showed similar antitumor effect,but the toxicity of paclitaxel liposome was lower.The accumulation of radioactive paclitexel was mainly in liver and spleen without targeting on tamor mass.