Stability evaluation of Gd chelates for macromolecular MRI contrast agents.
Stability evaluation of Gd chelates for macromolecular MRI contrast agents.
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高分子MRI造影剂Gd螯合物的稳定性评价。
DOI：
10.1007/s10334-019-00805-8
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发表时间：
2020
期刊：
影响因子：
--
通讯作者：
Kouichi Shiraishi
中科院分区：
文献类型：
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作者：
Masayuki Yokoyama;Kouichi Shiraishi
我们试图设计具有高Gd ~（3+）螯合稳定性的大分子试剂，因为从Gd螯合物释放的游离Gd 3+离子被认为是引起毒副作用和安全性问题的危险因素。材料和方法我们从合成聚合物制备了三种类型的基于Gd的大分子MRI造影剂（聚（谷氨酸）均聚物或聚（乙二醇）-b-聚（赖氨酸）嵌段共聚物）和螯合部分（D 03 A或D 0 TA），其具有用于高螯合物稳定性的两种策略设计。然后，我们研究了这些大分子MRI造影剂的体外Gd 3 +-螯合物的稳定性。结果制备的大分子试剂表现出相同或更高的Gd 3 +-螯合物的稳定性/比Gd-DOTA，具有最高的Gd 3 +-螯合物的稳定性之间批准的小分子量Gd-螯合物MRI造影剂。Discussion我们的大分子设计被认为是工作良好的高Gd 3 +-螯合物的稳定性。
ObjectiveWe try to establish designs for the macromolecular agents possessing high Gd3+-chelating stability, because free Gd3+ion released from Gd chelates is known as a risk factor to cause toxic side effects and a safety concern.Materials and methodsWe prepared three types of Gd-based macromolecular MRI contrast agents from a synthetic polymer (poly(glutamic acid) homopolymer or poly(ethylene glycol)-b-poly(lysine) block copolymer) and a chelating moiety (DO3A or DOTA) having two strategic designs for high chelate stability. Then, we examine the in vitro Gd3+-chelate stability of these macromolecular MRI contrast agents.ResultsThe prepared macromolecular agents exhibited the same or higher Gd3+-chelate stability as/than did Gd-DOTA that possesses the highest Gd3+-chelate stability among the approved small-MW Gd-chelate MRI contrast agent.DiscussionOur macromolecular design was considered to work well for high Gd3+-chelate stability.