目的：制备转铁蛋白（TF）修饰紫杉醇（PTX）脂质体（TF-PTX-LP），并研究其抑瘤作用。方法：采用薄膜分散法制备

TF-PTX-LP 并观察其形态；定性和定量考察肝癌HepG2 细胞对TF-LP 和LP的摄取情况；检测PTX、PTX-LP和TF-PTX-LP 分别处

理HepG2 细胞24、48、72 h 后细胞的增殖抑制率；以HepG2 细胞制备肿瘤球，考察生理盐水、PTX、PTX-LP和TF-PTX-LP分别处理

0、1、2、4、5、6、7 d 对肿瘤球体积的影响；复制HepG2 荷瘤裸鼠模型，考察生理盐水、PTX、PTX-LP 和TF-PTX-LP（以PTX 计8.5

mg/kg）对荷瘤裸鼠移植瘤的抑制作用。结果：TF-PTX-LP 均呈均一球形，粒径在100～120 nm。TF-LP 处理后细胞的荧光强度强

于LP（P＜0.01）。与PTX、PTX-LP 比较，TF-PTX-LP 处理后细胞的增殖抑制率更高（P＜0.01）。与生理盐水、PTX、PTX-LP 比较，

TF-PTX-LP处理后肿瘤球体积更小，对荷瘤裸鼠的抑瘤率更高，且6、7 d 后抑瘤率差异有统计学意义（P＜0.01）。增殖抑制率和肿

瘤球体积变化呈时间依赖性。结论：成功制得具有良好抑瘤作用的TF-PTX-LP。

OBJECTIVE：To prepare transferrin modified paclitaxel-loaded liposome（TF-PTX-LP），and to study the tumor inhibition

effect. METHODS：TF-PTX-LP was prepared by thin-film method，and morphology of TF-PTX-LP was observed. Qualitative

and quantitative investigation were used to value the uptake efficiency of TF-LP and LP by HepG2 cells. The proliferation inhibition

rate of HepG2 cells was investigated after treated with PTX，PTX-LP and TF-PTX-LP for 24，48 and 72 h. Tumor spheres

were prepared by using HepG2 cells. Effects of normal saline，PTX，PTX-LP and TF-PTX-LP on the volume of tumor spheres

were investigated after 0，1，2，4，5，6 and 7 d treatment. HepG2 tumor-bearing nude mice model was induced. Inhibitory effects

of normal saline，PTX，PTX-LP and TF-PTX-LP（8.5 mg/kg by PTX）on transplantable tumor of tumor-bearing nude mice were investigated.

RESULTS：TF-PTX-LP showed uniform spherical shape，with particle size of 100-120 nm. The fluorescence intensity of

HepG2 cells treated with TF-LP was stronger than that treated with LP（P＜0.01）. Compared with PTX and PTX-LP，TF-PTX-LP

showed higher proliferation inhibition rate（P＜0.01）. Compared with normal saline，PTX and PTX-LP，tumor spheres were smaller

in volume after treated with TF-PTX-LP，and inhibition rate of tumor was higher in tumor-bearing nude mice；there were statistical

significance after treated for 6，7 d（P＜0.01）. The proliferation inhibition rate and tumor spheres volume changed in time-dependent

manner. CONCLUSIONS：TF-PTX-LP which owns good tumor inhibition effect is prepared successfully.