甲氨蝶呤脂质体的载体潜能。甲氨蝶呤在小鼠器官组织水平的变化[作者译]。

J Freise, G Schäfer, F W Schmidt, P Magerstedt
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引用次数: 3

摘要

包裹在脂质体(人工脂囊)中的药物在静脉注射后表现出不同于以自由形式注射的药物的药代动力学。叶酸拮抗剂甲氨蝶呤可以以治疗用浓度(0.5 mg MTX/ml)包裹在脂质体中,并且可以以高包裹稳定性储存。经小鼠尾静脉静脉注射后,发现包裹氨甲蝶呤的脂质体在细胞系统中更富集,内吞率高,且不像游离氨甲蝶呤那样在3小时内被肾脏排出。可以证明,对于肝脏、脾脏、肾脏、肠道、肺和血液等器官,在6小时的时间内,包被甲氨蝶呤的脂质体在组织中富集,例如,6小时后,肝脏中的甲氨蝶呤水平比自由注射的甲氨蝶呤高20倍。
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[The carrier potential of liposomes for methotrexate. Changing of the tissue levels of methotrexate in the organs of mice (author's transl)].

Drugs entrapped in liposomes (artificial lipid vesicles) exhibit different pharmacokinetics after intravenous application than drugs injected in a free form. The folidacidantagonist methotrexate can be entrapped in liposomes in a therapeutically useful concentration (0.5 mg MTX/ml) and can be stored with high stability of entrappment. After intravenous injection into the tail vein of mice liposomes entrapped methotrexate is found more enriched in cell systems with high rate of endocytosis and not eliminated by the kidneys within 3 h like free methotrexate. It can be shown, that for the organs liver, spleen, kidney, gut, lung, and blood over a 6 h period liposomes entrapped methotrexate is enriched in the tissues and that for example after 6 h the methotrexate level in the liver is 20 fold higher in comparison to free injected methotrexate.

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