文章基本信息

标题：Targeting of Soybean-Derived Sterylglucoside Liposomes to Liver Tumors in Rat and Mouse Models
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作者：Kazuyuki SHIMIZU ; Xian-Rong QI ; Yoshie MAITANI 等
期刊名称：Biological and Pharmaceutical Bulletin
印刷版ISSN：0918-6158
电子版ISSN：1347-5215
出版年度：1998
卷号：21
期号：7
页码：741-746
DOI：10.1248/bpb.21.741
出版社：The Pharmaceutical Society of Japan
摘要：The blood clearance, tissue uptake and antitumor efficacy against liver metastasis of M5076 reticulosarcoma in mice and against primary liver cancer in rats of doxorubicin (DOX) encapsulated in two types of liposomes, with and without a soybean-derived sterylglucoside mixture (SG), were examined. Liposomes entrapping DOX were composed of dipalmitoylphosphatidylcholine (DPPC), SG and cholesterol (Ch) at a molar ratio of 6 : 1 : 3, (SG-liposomes) and 6 : 0 : 4 (non-SG-liposomes). Pharmacokinetic analysis of drug disposition was based on the area under the curve (AUC) for liposomes up to 24h following i.v. injection. SG-liposomes showed lower DOX concentrations in blood and higher concentrations in liver compared with non-SG-liposomes. The highest AUC of SG-liposomes in tissue was in liver, 2.4 times higher than that of the free drug. The antitumor efficacy of SG-liposomes was compared with that of free DOX and non-SG-liposomes at a dose of 5 mg DOX/kg. SG-liposomes displayed stronger antitumor activity than the free drug and non-SG-liposomes in murine reticulosarcoma M5076 tumor models and primary liver cancer models reflecting accumulation in hepatocytes. The antitumor activity of SG-liposomes in rats with primary liver cancer was significantly higher compared with free DOX and non-SG-liposomes (ILS : 92.7%).
关键词：liposome;sterylglucoside;M5076;primary liver cancer;doxorubicin