Chiral Strategy for Developing High-Performance Polymeric Gadolinium-Based MRI Contrast Agents for Vascular and Tumor Imaging
X. K. Zhou, Xinzhong Ruan, Xingjiang Li, Weiyuan Xu, Xinhui Xiao, A. Chen, Yinghui Ding, Jilai Zhang, Gengshen Mo, Yong Jian, Xiaoying Wu, Fangfu Ye, Zhiqiang Wang, Yi Li, Lixiong Dai
Abstract
High Resolution Image Download MS PowerPoint Slide Magnetic resonance imaging (MRI) is a critical tool in medical diagnostics, yet conventional MRI contrast agents (CAs) are often limited by their small-molecule nature, resulting in rapid clearance and low relaxivity. This study presents a chiral strategy for developing high-performance polymeric gadolinium-based CAs, PAA-EOB-GdA and PAA-EOB-GdB, tailored for enhanced vascular and tumor imaging. Notably, PAA-EOB-GdA, a chiral Gd-DOTA derivative integrated with sodium poly(acrylic acid) (PAA), benefits from the optimized water exchange rate of chiral Gd(III) complex and the polymer effect of PAA, exhibiting exceptionally high relaxivity ( r 1 = 37.87 mM –1 s –1, 11.9-fold of clinical Gd-DOTA) and showed remarkable imaging efficacy in magnetic resonance angiography (MRA) with low-dose administration (0.05 mmol kg –1 ) and an extended imaging duration. Its performance in tumor imaging was also impressive, maintaining superior enhancement values compared to Gd-DOTA. These characteristics feature PAA-EOB-GdA as a promising candidate for clinical diagnosis in both vascular and tumor imaging applications.