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Biodegradable Macromolecular MRI Contrast Agents

机译:可生物降解的大分子MRI造影剂

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Magnetic resonance imaging (MRI) is a non-invasive clinical diagnostic modality. Paramagnetic metal chelates, e.g. gadolinium complexes, Gd-DTPA (DTPA: diethylenetriaminepentaacetate), Gd-DOTA (DOTA: 1,4,7,10-tetraazadodecanetetraacetic acid) and their derivatives, have been developed as contrast agents to enhance diagnostic MR images. These contrast agents are low molecular weight chelates, have a short blood circulation time and nonspecifically extravasate into normal and disease tissues. Incorporation of the paramagnetic contrast agents into macromolecules can increase both the circulation time of the agents in the blood pool and accumulation in solid tumor due to the hyperpermeability of tumor vasculature. These macromolecular paramagnetic complexes have demonstrated superior contrast enhancement in MR cardiovascular imaging and cancer imaging in the preclinical studies. Unfortunately, the clinical development of these agents is impeded by the safety concerns related to their slow elimination from the body.
机译:磁共振成像(MRI)是一种非侵入性的临床诊断手段。顺磁性金属螯合物,例如developed络合物,Gd-DTPA(DTPA:二亚乙基三胺五乙酸酯),Gd-DOTA(DOTA:1,4,7,10-四氮杂十二烷四乙酸)及其衍生物已开发为造影剂,可增强诊断性MR图像。这些造影剂是低分子量螯合物,血液循环时间短,并且非特异性地渗入正常组织和疾病组织。由于肿瘤脉管系统的高通透性,将顺磁性造影剂掺入大分子中既可以增加其在血池​​中的循环时间,又可以增加实体瘤中的蓄积。在临床前研究中,这些大分子顺磁性复合物在MR心血管成像和癌症成像中已显示出优异的对比度增强。不幸的是,与它们从体内缓慢清除有关的安全问题阻碍了这些药物的临床开发。

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