Wang Hongliang, Tian Tian, Xu Shuning, Yin Yanfei, Shi Huixian
Department of Nuclear Medicine, First Hospital of Shanxi Medical University, Taiyuan, Shanxi 030001, China; Shanxi Key Laboratory of Molecular Imaging &, Collaborative Innovation Center for Molecular Imaging of Precision Medicine, Shanxi Medical University, Taiyuan, Shanxi 030001, China.
Department of Nuclear Medicine, First Hospital of Shanxi Medical University, Taiyuan, Shanxi 030001, China; Shanxi Key Laboratory of Molecular Imaging &, Collaborative Innovation Center for Molecular Imaging of Precision Medicine, Shanxi Medical University, Taiyuan, Shanxi 030001, China.
J Colloid Interface Sci. 2025 Dec 15;700(Pt 1):138351. doi: 10.1016/j.jcis.2025.138351. Epub 2025 Jul 7.
In this study, a novel multifunction Ce-doped carbon dots (CDs) system conjugated with arginine-glycine-aspartic acid (RGD) peptide (RGD-Ce/CDs) was successfully synthesized to enhance tumor-targeting capabilities. Structural characterization revealed uniform, ultra-small particle sizes (∼4.75 nm) and excellent dispersibility. The RGD-Ce/CDs exhibited strong absorption in both the near-infrared region (NIR-I and NIR-II) regions, achieving high photothermal conversion efficiency (PCE) of 31.8 % at 808 nm and 20.6 % at 1060 nm. Furthermore, Ce doping significantly facilitated reactive oxygen species (ROS) generation under NIR irradiation, leveraging the up-conversion effect of Ce. These properties render RGD-Ce/CDs highly promising for combined photothermal (PTT) and photodynamic therapy (PDT). Notably, RGD-Ce/CDs demonstrated excellent biocompatibility, low cytotoxicity, and remarkable photothermal stability. In vivo experiments on tumor-bearing mice showed that RGD-Ce/CDs significantly inhibited tumor growth under both 808 nm and 1060 nm laser irradiation, achieving near-complete tumors ablation in the treatment group. Importantly, RGD peptide conjugation enabled selective tumor targeting, minimizing off-target effects on healthy tissues while enhancing therapeutic efficacy. This facile synthetic strategy provides a promising platform for developing multifunctional, tumor-targeted phototherapeutic agents that synergistically integrate PTT and PDT for cancer treatment.
在本研究中，成功合成了一种与精氨酸-甘氨酸-天冬氨酸（RGD）肽共轭的新型多功能铈掺杂碳点（CDs）系统（RGD-Ce/CDs），以增强肿瘤靶向能力。结构表征显示其粒径均匀、超小（约4.75纳米）且分散性优异。RGD-Ce/CDs在近红外区域（NIR-I和NIR-II）均表现出强烈吸收，在808纳米处实现了31.8%的高光热转换效率（PCE），在1060纳米处为20.6%。此外，铈掺杂显著促进了近红外辐射下活性氧（ROS）的产生，利用了铈的上转换效应。这些特性使RGD-Ce/CDs在光热疗法（PTT）和光动力疗法（PDT）联合应用方面极具潜力。值得注意的是，RGD-Ce/CDs表现出优异的生物相容性、低细胞毒性和显著的光热稳定性。对荷瘤小鼠的体内实验表明，RGD-Ce/CDs在808纳米和1060纳米激光照射下均能显著抑制肿瘤生长，治疗组实现了近乎完全的肿瘤消融。重要的是，RGD肽共轭实现了肿瘤的选择性靶向，在增强治疗效果的同时，将对健康组织的脱靶效应降至最低。这种简便的合成策略为开发多功能、肿瘤靶向光治疗剂提供了一个有前景的平台，该光治疗剂将PTT和PDT协同整合用于癌症治疗。
