甲氨蝶呤热敏磁靶向脂质体的制备和靶向性研究

Study of the preparation and targeting effect of methotrexate thermosensitive magnetoliposomes

采用正交设计以37℃和43℃释出的游离药物之比为评价指标优化甲氨蝶呤热敏磁靶向脂质体处方。并测定了小鼠尾静脉注射甲氨蝶呤溶液和甲氨蝶呤脂质体后,全血和肌肉中的药物浓度。结果表明,给予甲氨蝶呤脂质体后再外加磁场并置于43℃环境,脂质体靶向效率Te提高6.8倍,相对摄取量Re提高6.5倍。说明本实验制备的脂质体具有很高的靶向性。

The formulation of the methotrexate thermosensitive magnetoliposomes was optimized by orthogonal design according to the ratio of drug release property of liposomes at 37℃ and 43℃ in vitro. And the targeting effect of methotrexate liposomes prepared under the optimum condition was studied by the determination of methotrexate in whole blood and muscles. The results indicated that the targeting effect （Te）of methotrexate lipo- somes increased 6.8 folds while the relative uptake effect （Re）increased 6.5 folds. It was shown that the methotrexate liposomes prepareded in this paper had high targeting effect.