Developing tumor-homing nanoparticles with integrated diagnostic and therapeutic functions, and meanwhile could be rapidly excreted from the body, would be of great interest to realize imaging-guided precision treatment of cancer. In this study, an ultrasmall coordination polymer nanodot (CPN) based on the coordination between tungsten ions (W^VI) and gallic acid (W-GA) was developed via a simple method. After polyethylene glycol (PEG) modification, PEGylated W-GA (W-GA-PEG) CPNs with an ultrasmall hydrodynamic diameter of 5 nm were rather stable in various physiological solutions. Without the need of chelator molecules, W-GA-PEG CPNs could be efficiently labeled with radioisotope ⁶⁴Cu²⁺, enabling positron emission tomography (PET) imaging, which reveals efficient tumor accumulation and rapid renal clearance of W-GA-PEG CPNs upon intravenous injection. Utilizing the radio-sensitizing function of tungsten with strong X-ray absorption, such W-GA-PEG CPNs were able to greatly enhance the efficacy of cancer radiotherapy in inhibiting the tumor growth. With fast clearance and little long-term body retention, those W-GA-PEG CPNs exhibited no appreciable in vivo toxicity. This study presents a type of CPNs with excellent imaging and therapeutic abilities as well as rapid renal clearance behavior, promising for further clinic translation.

中文翻译：

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可清除肾脏的超小配位聚合物纳米点，用于无螯合剂的⁶⁴ Cu标签和影像引导的增强放射治疗

开发具有整合的诊断和治疗功能的肿瘤归巢纳米颗粒，同时可以迅速从体内排出，对于实现影像引导的癌症精确治疗将具有极大的兴趣。在这项研究中，通过一种简单的方法，开发了一种基于钨离子（W ^VI）和没食子酸（W-GA）之间配位的超小配位聚合物纳米点（CPN）。经过聚乙二醇（PEG）修饰后，具有5 nm超小流体动力学直径的PEG化W-GA（W-GA-PEG）CPN在各种生理溶液中相当稳定。不需要螯合剂分子，可以用放射性同位素⁶⁴ Cu ²⁺有效标记W-GA-PEG CPN，可进行正电子发射断层扫描（PET）成像，揭示了静脉注射后W-GA-PEG CPNs的有效肿瘤蓄积和快速肾脏清除率。利用钨具有强X射线吸收的放射增敏功能，这种W-GA-PEG CPN能够极大地增强癌症放射疗法抑制肿瘤生长的功效。这些W-GA-PEG CPN具有快速清除和很少的长期体内滞留的特性，在体内没有明显的毒性。这项研究提出了一种具有出色的成像和治疗能力以及快速的肾脏清除行为的CPN，有望用于进一步的临床翻译。