Combining different therapeutic functions within single tumor-targeted nanoscale delivery systems is promising to overcome the limitations of conventional cancer therapies. Herein, transferrin that recognizes transferrin receptors up-regulated on tumor cells is pre-labeled with iodine-131 (¹³¹I) and then utilized as the stabilizer in the fabrication of polypyrrole (PPy) nanoparticles. The obtained transferrin-capped PPy@Tf-¹³¹I nanoparticles could be used for tumor-targeted radioisotope therapy (RIT) and photothermal therapy (PTT), by employing beta-emission from ¹³¹I and the intrinsic high near-infrared (NIR) absorbance of PPy, respectively. Owing to the transferrin-mediated tumor targeting, PPy@Tf-¹³¹I nanoparticles exhibit obviously enhanced in vitro cancer cell binding and in vivo tumor uptake compared to its non-targeting counterpart. The combined RIT and PTT based on PPy@Tf-¹³¹I nanoparticles is then conducted, achieving a remarkable synergistic therapeutic effect. This work thus demonstrates a rather simple one-step approach to fabricate tumor-targeting nanoparticles based on protein-capped conjugated polymers, promising for combination cancer therapy with great efficacy and high safety.

中文翻译：

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碘131标记的转铁蛋白封端的聚吡咯纳米颗粒，用于靶向肿瘤的协同光热放射性同位素治疗†

在单个靶向肿瘤的纳米级递送系统中结合不同的治疗功能有望克服常规癌症治疗的局限性。在此，识别出在肿瘤细胞上调的转铁蛋白受体的转铁蛋白预先用碘131（¹³¹ I）标记，然后在聚吡咯（PPy）纳米颗粒的制备中用作稳定剂。通过利用¹³¹ I的β发射和固有的高近红外（NIR）吸收率，获得的转铁蛋白封端的PPy @ Tf- ¹³¹ I纳米颗粒可用于肿瘤靶向的放射性同位素疗法（RIT）和光热疗法（PTT）。分别为PPy。由于转铁蛋白介导的肿瘤靶向作用，PPy @ Tf- ¹³¹与它的非靶向对应物相比，I纳米颗粒表现出明显增强的体外癌细胞结合和体内肿瘤吸收。然后进行了基于PPy @ Tf- ¹³¹ I纳米粒子的RIT和PTT的组合，实现了显着的协同治疗效果。因此，这项工作证明了一种相当简单的一步法来制备基于蛋白质封端的共轭聚合物的靶向肿瘤的纳米颗粒，有望以高功效和高安全性用于联合癌症治疗。