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Enhanced Performance of Polymeric 19F MRI Contrast Agents through Incorporation of Highly Water-Soluble Monomer MSEA
Macromolecules ( IF 5.1 ) Pub Date : 2018-07-26 00:00:00 , DOI: 10.1021/acs.macromol.8b01190
Changkui Fu , Cheng Zhang , Hui Peng , Felicity Han , Carly Baker , Yuao Wu , Hang Ta , Andrew K. Whittaker

19F magnetic resonance imaging (MRI) is a powerful noninvasive imaging technique that shows tremendous potential for the diagnosis and monitoring of human diseases. Fluorinated compounds are commonly used as 19F MRI contrast agents to develop “hot spot” imaging. To achieve high-resolution MR images, a high density of 19F nuclei is required in the contrast agents. However, because of the inherent hydrophobicity of fluorinated moieties, aggregation of 19F contrast agents with high fluorine content is often observed in aqueous solution, resulting in attenuated MR signal and low sensitivity, thus significantly limiting their further biological applications. Here we report the synthesis and characterization of a series of polymeric 19F MRI contrast agents with high fluorine content by copolymerizing the well-known fluorinated monomer 2,2,2-trifluoroethyl acrylate (TFEA) with a highly water-soluble monomer 2-(methylsulfinyl)ethyl acrylate (MSEA) using RAFT polymerization. We show that these polymeric contrast agents, although with high fluorine content, display remarkable imaging performance as evidenced by preferable relaxation properties and intense in vitro/in vivo MRI signals, demonstrating the huge potential for eventual clinical applications such as MRI-guided disease diagnosis and therapy.

中文翻译:

通过掺入高度水溶性单体MSEA增强聚合物19 F MRI造影剂的性能

19 F磁共振成像(MRI)是一种强大的无创成像技术,在诊断和监测人类疾病方面显示出巨大的潜力。氟化化合物通常用作19 F MRI造影剂,以开发“热点”成像。为了获得高分辨率的MR图像,在造影剂中需要高密度的19 F核。然而,由于氟化部分的固有疏水性,经常在水溶液中观察到具有高氟含量的19 F造影剂的聚集,导致减弱的MR信号和低灵敏度,从而显着限制了它们的进一步生物学应用。在这里,我们报告了一系列聚合物19的合成和表征通过使用RAFT聚合将众所周知的氟化单体2,2,2-三氟乙基丙烯酸酯(TFEA)与高水溶性单体丙烯酸2-(甲基亚磺酰基)乙酯(MSEA)共聚,从而获得高氟含量的F MRI造影剂。我们显示,这些聚合物造影剂尽管具有较高的氟含量,但显示出显着的成像性能,这表现为较佳的弛豫性能和强烈的体内/体外MRI信号所证明,证明了最终临床应用(如MRI指导的疾病诊断和诊断)的巨大潜力治疗。
更新日期:2018-07-26
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