Functional Hyperbranched Polylysine as Potential Contrast Agent Probes for Magnetic Resonance Imaging

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• 作者：Guangyue Zu ; Min Liu ; Kunchi Zhang ; Shanni Hong ; Jingjin Dong ; Yi Cao ; Bin Jiang ; Liqiang Luo ; Renjun Pei
• 刊名：Biomacromolecules
• 出版年：2016
• 出版时间：June 13, 2016
• 年：2016
• 卷：17
• 期：6
• 页码：2302-2308
• 全文大小：468K
• 年卷期：0
• ISSN：1526-4602

文摘

Researchers have never stopped questing contrast agents with high resolution and safety to overcome the drawbacks of small-molecule contrast agents in clinic. Herein, we reported the synthesis of gadolinium-based hyperbranched polylysine (HBPLL-DTPA-Gd), which was prepared by thermal polymerization of l-lysine via one-step polycondensation. After conjugating with folic acid, its potential application as MRI contrast agent was then evaluated. This contrast agent had no obvious cytotoxicity as verified by WST assay and H&E analysis. Compared to Gd(III)-diethylenetriaminepentaacetic acid (Gd-DTPA) (r₁ = 4.3 mM^–1 s^–1), the FA-HBPLL-DTPA-Gd exhibited much higher longitudinal relaxivity value (r₁ = 13.44 mM^–1 s^–1), up to 3 times higher than Gd-DTPA. The FA-HBPLL-DTPA-Gd showed significant signal intensity enhancement in the tumor region at various time points and provided a long time window for MR examination. The results illustrate that FA-HBPLL-DTPA-Gd will be a potential candidate for tumor-targeted MRI.