亲淋巴磁共振造影剂的合成、表征和性能研究

Study of Gd-poly-DTPA-EOEA Contrast Agent Targeted for Lymphatic System in Magnetic Resonance Imaging:Preparation,Characterization and Properties

目的:探讨合成亲淋巴造影剂的方法并对其体内外性能进行研究。方法:采用二氨基乙基乙二醇醚(EOEA)-二乙三胺五乙酸(DTPA)线性共聚合物(poly-DTPA-EOEA)为配体,与钆(Gd)的三价盐配位构建T1类线性大分子造影剂,检测二氨基乙基乙二醇-DTPA酰胺共聚物钆配合物(Gd-poly-DTPA-EOEA)的表征和性能。结果:Gd-poly-DTPA-EOEA分子量为20kDa,其中钆的含量为14%(w/w)。T1值为6.45LmM-1s-1。Gd-poly-DTPA-EOEA在血液中的存留时间明显长于小分子造影剂Gd-DTPA,并可进入淋巴结巨噬细胞内。结论:Gd-poly-DTPA-EOEA是一种具有高驰豫率、循环时间长和亲淋巴特性的T1类大分子造影剂。

Objective：To investigate the synthetic way of lymphotropic contrast agents and their characterization, properties both in vitro and in vivo. Methods：Gd-poly-DTPA-EOEA was synthesized to a T1 type liner macromolecular MRI contrast agent by connecting bis （2-aminoethoxy） ethane, triethylamine and DTPA dianhydride with GdC13. Results：The molecular weight of Gd-poly-DTPA-EOEA was 20 kDa, which contains 14 % Gd （w/w）. The T1 relaxation was 6.45 L mM^-1s^-1. The excised lymph node showed evidently that the Gd-poly-DTPA-EOEA could get into the bodies of macrophages in the lymph nodes. The lifetime of the contrast agents in blood is longer than that of the Gd-DTPA, indicated by pharmacokinetics study. Conclusion：Gd-poly-DTPA-EOEA as a T1 type linear macromolecular MRI contrast agents showed that it has relatively higher relaxation, longer period of lifetime in blood vessel and lymphotropic characterization.