Institute of Functional Nano & Soft Materials (FUNSOM), Jiangsu Key Laboratory for Carbon-Based Functional Materials & Devices, Soochow University, Suzhou 215123, China.
Biomater Sci. 2017 Aug 22;5(9):1828-1835. doi: 10.1039/c7bm00409e.
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 (I) and then utilized as the stabilizer in the fabrication of polypyrrole (PPy) nanoparticles. The obtained transferrin-capped PPy@Tf-I nanoparticles could be used for tumor-targeted radioisotope therapy (RIT) and photothermal therapy (PTT), by employing beta-emission from I and the intrinsic high near-infrared (NIR) absorbance of PPy, respectively. Owing to the transferrin-mediated tumor targeting, PPy@Tf-I 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-I 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.
将不同的治疗功能结合在单个肿瘤靶向纳米递药系统中有望克服传统癌症治疗的局限性。在此，识别肿瘤细胞上上调的转铁蛋白受体的转铁蛋白预先用碘-131（I）标记，然后用作聚吡咯（PPy）纳米粒子制备中的稳定剂。所得的转铁蛋白封端的 PPy@Tf-I 纳米粒子可分别通过 I 的β发射和 PPy 的固有高近红外（NIR）吸收用于肿瘤靶向放射性同位素治疗（RIT）和光热治疗（PTT）。由于转铁蛋白介导的肿瘤靶向，与非靶向对照相比，PPy@Tf-I 纳米粒子在体外癌细胞结合和体内肿瘤摄取方面表现出明显增强。然后进行基于 PPy@Tf-I 纳米粒子的联合 RIT 和 PTT，实现了显著的协同治疗效果。因此，本工作展示了一种相当简单的一步法，基于蛋白封端的共轭聚合物制备肿瘤靶向纳米粒子，有望实现高效、高安全性的联合癌症治疗。
