目的：制备抗肿瘤靶向药物紫杉醇白蛋白磁性纳米颗粒（magnetic paclitaxel albumin nanoparticle，MAG-TAX-NP）和碘化油MAG-TAX-NP，观察碘化油MAG-TAX-NP治疗大鼠肝癌的效果。 方法： 以白蛋白、纳米Fe3O4颗粒为载体，用乳化-超声-加热固化法制备MAG-TAX-NP和碘化油MAG-TAX-NP，紫外分光光度法检测其紫杉醇的含量并计算MAG-TAX-NP的载药率及包封率，电镜下观察MAG-TAX-NP的形态。建立大鼠肝癌模型，除空白对照组外，分别将碘化油、碘化油紫杉醇﹑碘化油磁性纳米颗粒、碘化油MAG-TAX-NP各0.2 ml注入各组荷瘤大鼠肝固有动脉内进行治疗，14 d后处死大鼠，取肝肿瘤组织称重，计算各组抑瘤率；电镜观察碘化油MAG-TAX-NP对肝肿瘤的抑制作用。 结果： 制备的MAG-TAX-NP形态圆滑，粒径约70 nm，平均载药率为（5.62±0.08）%，平均包封率为（80.72±0.96）%。碘化油、碘化油紫杉醇﹑碘化油磁性纳米颗粒、碘化油MAG-TAX-NP各组的抑瘤率分别为(43.2±2.24)%、(51±3.33)%、(57.4±3.66)%和(87.4±4.11)%，碘化油MAG-TAX-NP组的抑瘤率明显提高（P<0.01）；此外，碘化油MAG-TAX-NP作用于肝肿瘤后，肝癌细胞出现大量凋亡与坏死。 结论： 碘化油MAG-TAX-NP可抑制大鼠肝癌的生长，有望成为紫杉醇治疗肝癌的新剂型。

Objective : To prepare anti-cancer targeting drug paclitaxel albumin magnetic nanoparticles (MAG-TAX-NP) and iodinate oil MAG-TAX-NP, and study the efficacy of iodinate oil MAG-TAX-NP on rat liver cancer. Methods: MAG-TAX-NP was prepared by emulsion-ultrasonic-solidification heat method using albumin and nano-Fe3O4 particles as carriers, and then iodinate oil MAG-TAX-NP was constructed. The content of paclitaxel was detected by UV spectrophotometry, and the loading rate and the entrapment efficiency of MAG-TAX-NP were calculated. The morphology of MAG-TAX-NP was observed under electron microscope. Rat liver tumor model was established. In addition to the blank group, 0.2 ml of iodinate oil, iodinate oil paclitaxel, iodinate oil magnetic nanoparticle, or iodinate oil MAG-TAX-NP was separately injected into the hepatic artery of tumor-bearing rats. Tumor-bearing rats were sacrificed 14 d after injection, the liver tumors were weighed and the tumor inhibitory rates in each group were calculated. The inhibitory rate of Iodinate oil MAG-TAX-NP on liver tumors was observed under an electron microscope. Results: The prepared MAG-TAX-NP was smooth; its diameter was about 70 nm; its average loading rate was 5.62%; and its average entrapment efficiency was 8072%. The tumor inhibitory rate of iodinate oil MAG-TAX-NP treatment group was significantly increased (P<0.01), with tumor inhibitory rates of iodinate oil, iodinate oil paclitaxel, iodinate oil magnetic nanoparticle, and iodinate oil MAG-TAX-NP treatment groups being (43.2±2.24)%, (51±3.33)%, (57.4±3.66)%, and (87.4±4.11)%, respectively. Furthermore, liver tumor cells showed lots of apoptosis and necrosis after iodinate oil MAG-TAX-NP treatment. Conclusion: Iodinate oil MAG-TAX-NP can inhibit growth of rat liver tumors, which might become a novel paclitaxel formulation in treatment of liver cancers.

黑龙江省科技攻关计划重点项目基金资助（No. GB05C 402-07）；黑龙江省教育厅科技项目基金资助（No. 11521183）