Freise J, Schäfer G, Schmidt F W, Magerstedt P
Z Krebsforsch Klin Onkol Cancer Res Clin Oncol. 1977 Nov 18;90(2):187-95. doi: 10.1007/BF00285325.
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.
包裹在脂质体(人工脂质囊泡)中的药物在静脉注射后表现出与以游离形式注射的药物不同的药代动力学。叶酸拮抗剂甲氨蝶呤可以以治疗有效浓度(0.5毫克甲氨蝶呤/毫升)包裹在脂质体中,并且可以在高包封稳定性下储存。将包裹有甲氨蝶呤的脂质体静脉注射到小鼠尾静脉后,发现其在具有高内吞率的细胞系统中富集,并且不像游离甲氨蝶呤那样在3小时内被肾脏清除。可以证明,在6小时内,对于肝脏、脾脏、肾脏、肠道、肺和血液等器官,包裹有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游离注射的甲氨蝶呤高20倍。