目的:制备活性高、水溶性好的(-)-Antofine脂质体,并进行其体内外抗乳腺癌活性研究。方法:采用薄膜分散法制备(-)-Antofine脂质体,用紫外分光光度仪测定(-)-Antofine脂质体包封率,用MTT法测定(-)-Antofine脂质体细胞活力,通过荷瘤小鼠实验评价体内抑瘤活性和主要脏器指数。结果:用薄膜分散法成功制得了(-)-Antofine脂质体,平均包封率为80.8%±2.2%,平均载药量为26.7%±1.4%,(-)-Antofine脂质体具有较好的水溶性,体内外实验结果均表明(-)-Antofine脂质体的抗乳腺癌活性较(-)-Antofine原药有所提高。结论:(-)-Antofine脂质体具有较高的包封率,提高了(-)-Antofine水溶性和抗肿瘤活性。 OBJECTIVE: To prepare (-) - Antofine liposomes with high activity and good water solubility and to study their anti-breast cancer activity in vitro and in vivo. Methods: (-) - Antofine liposomes were prepared by membrane dispersion method. The entrapment efficiency of (-) - Antofine liposomes was determined by UV spectrophotometry. The viability of (-) - Antofine liposomes was determined by MTT assay. Tumor-bearing mice in vivo evaluation of anti-tumor activity and major organ index. Results: The (-) - Antofine liposomes were successfully prepared by the membrane dispersion method. The average entrapment efficiency was (80.8% ± 2.2%) and the average drug load was 26.7% ± 1.4% Good water solubility, in vitro and in vivo results show that (-) - Antofine liposomal anti-breast cancer activity than (-) - Antofine original drug has increased. Conclusion: (-) - Antofine liposomes have higher entrapment efficiency and improve (-) - Antofine water solubility and antitumor activity.