脂质微球作为抗肿瘤药物载体的应用。

Use of lipid microspheres as a drug carrier for antitumour drugs.

作者信息

Mizushima Y, Shoji Y, Kato T, Fukushima M, Kurozumi S

出版信息

J Pharm Pharmacol. 1986 Feb;38(2):132-4. doi: 10.1111/j.2042-7158.1986.tb04527.x.

DOI:10.1111/j.2042-7158.1986.tb04527.x

Abstract

9-Oxo-15-hydroxy-delta 7,10,13-prostatrienoic acid methyl ester (delta 7-PGA1), an antitumour drug was incorporated into lipid microspheres of 0.2 micron diameter (lipo-delta 7-PGA1). In in-vivo experiments, lipo-delta 7-PGA1 had a significantly greater antitumour activity than free delta 7-PGA1 against P388 leukaemia. Lipo-delta 7-PGA1 slightly, but significantly, prolonged the survival time of mice inoculated with L1210 leukaemia, whereas free delta 7-PGA1 did not. Against MM46 ascites tumour, the survival time after treatment with 10 mg kg-1 of lipo-delta 7-PGA1 was significantly greater than that after the same dose of free delta 7-PGA1. The results suggest that lipid microspheres can be used as drug delivery carriers for lipid soluble antitumour agents.

摘要

9-氧代-15-羟基-δ7,10,13-前列腺三烯酸甲酯（δ7-PGA1），一种抗肿瘤药物，被载入直径为0.2微米的脂质微球（脂质体-δ7-PGA1）中。在体内实验中，脂质体-δ7-PGA1对P388白血病的抗肿瘤活性显著高于游离的δ7-PGA1。脂质体-δ7-PGA1略微但显著地延长了接种L1210白血病小鼠的存活时间，而游离的δ7-PGA1则没有。对于MM46腹水瘤，用10 mg kg-1脂质体-δ7-PGA1治疗后的存活时间显著长于相同剂量游离δ7-PGA1治疗后的存活时间。结果表明，脂质微球可作为脂溶性抗肿瘤药物的给药载体。