Objective

We 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 methods

We 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.

Results

The 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.

Discussion

Our macromolecular design was considered to work well for high Gd³⁺-chelate stability.

中文翻译：

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大分子MRI造影剂的Gd螯合物的稳定性评估。

客观的

我们尝试建立具有高Gd ³⁺螯合稳定性的大分子试剂的设计，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问题的危险因素。

材料和方法

我们从合成聚合物（聚（谷氨酸）均聚物或聚（乙二醇）-b-聚（赖氨酸）嵌段共聚物）和具有​​两个螯合部分（DO3A或DOTA）制备了三种类型的基于Gd的大分子MRI造影剂高螯合稳定性的战略设计。然后，我们检查了这些大分子MRI造影剂的体外Gd ^3+-螯合物的稳定性。

结果

所制备的大分子试剂与批准的小MW Gd-螯合物MRI造影剂中具有最高Gd ^3+-螯合物稳定性的Gd-DOTA相比，具有相同或更高的Gd ^3+-螯合物稳定性。

讨论

我们的大分子设计被认为对高Gd ³⁺螯合物的稳定性很好。