甲氨蝶呤磁靶向脂质体的制备及初步评价

 目的通过对甲氨蝶呤磁靶向脂质体的处方及制备工艺研究,研制高包封率和稳定的脂质体。方法采用逆向蒸发法制备甲氨蝶呤磁靶向脂质体,以正交实验优化处方;测定了脂质体中药物的包封率和脂质体的粒径;分离并测定了磁性脂质体中包裹的铁磁性物质的含量;初步考察了脂质体的稳定性。结果甲氨蝶呤磁靶向脂质体的包封率大于60%,平均粒径为627.8nm,多分散系数为0.131,每毫升脂质体乳浊液包裹铁磁性物质为116.1μg,具有良好的稳定性。结论所有的实验结果提示,该制备工艺和处方可以制备具有高包封率及稳定性的甲氨蝶呤磁靶向脂质体。

Preparation of Stable Magnetoliposomes with High Encapsulation Efficiency of Methotrexate

OBJECTIVE To get an optimized formulation of the stable magnetoliposomes with high encapsulation efficiency of methotrexate. METHODS The methotrexate magnetoliposomes were prepared by reverse evaporating method. The formulation was optimized by orthogonal design. The encapsulation efficiency, the particle size and the content of encapsulated Fe₂O₃ were determined. RESULTS The encapsulation efficiency of the methotrexate reached 60%, and the particle size of the liposome was 627.8 nm with the polydispersity index of 0.131. The concentration of the encapsulated Fe₂O₃ was 116.1 μg. CONCLUSION The results suggest that this method can be used to prepare a stable magnetoliposomes with high encapsulation efficiency of methotrexate.