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DEVELOPMENT AND APPLICATION OF TUMOR DIAGNOSTIC RADIOACTIVE PROBE TARGETING FOLIC ACID RECEPTOR

机译:肿瘤诊断放射探针靶向叶酸受体的开发与应用

摘要

The present invention pertains to a novel liposome-based contrast agent that is for suppressing absorption in the reticuloendothelial system and for tumor-specific delivery of a radiolabeled substance. More specifically, the present invention pertains to: a liposome contrast agent containing a lipid and a compound of chemical formula 1, which is a radiolabeled substance, the liposome contrast agent being characterized in that the lipid is composed of (a) cholesterol, (b) 1,2-dipalmitoyl-sn-glycero-3-phosphocholine (DPPC), and (c) 1,2-distearoyl-sn-glycero-3-phosphoethanolamine-N [methoxy(polyethylene glycol)-2000] (DSPE-PEG2000); and a cancer diagnostic composition containing the liposome contrast agent as an active ingredient. If a liposome system, containing a contrast substance of chemical formula 1 having a unique lipid composition provided by the present invention, is manufactured, the tumor-to-organ uptake ratio of the contrast substance in the reticuloendothelial system increases significantly, thus greatly increasing the tumor diagnostic efficiency of the compound of chemical formula 1.
机译:本发明涉及新颖的基于脂质体的造影剂,其用于抑制网状内皮系统中的吸收并用于放射性标记物质的肿瘤特异性递送。更具体地,本发明涉及:脂质体造影剂,其包含脂质和作为放射性标记物质的化学式1的化合物,该脂质体造影剂的特征在于脂质由(a)胆固醇,(b)构成。 )1,2-二棕榈酰基-sn-甘油-3-磷酸胆碱(DPPC),和(c)1,2-二硬脂基-sn-甘油-3-磷酸乙醇胺-N [甲氧基(聚乙二醇)-2000](DSPE-PEG2000 );含有脂质体造影剂作为有效成分的癌症诊断用组合物。如果制造包含本发明提供的具有独特脂质组成的化学式1的造影剂的脂质体系统,则该造影剂在网状内皮系统中的肿瘤-器官摄取比显着增加,从而大大增加了化学式1的化合物对肿瘤的诊断效率

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