Phototherapy has developed as a powerful method for remedial modalities. The conventional photosensitizers are “always on” state and lack tumor targeting, which contributed to poor therapeutic effect and high toxicity. Therefore, we developed an aspartyl aminopeptidase (DNPEP) activated self-assembled organic nanoparticles (NRh-Asp NPs) with sensitive external irradiation-induced photothermal therapy and photodynamic therapy (PTT/PDT). NRh-Asp NPs can be activated to NRhNH₂ NPs by DNPEP, demonstrating strong near-infrared (NIR) fluorescence, and efficiently generating heat and singlet oxygen under the near-infrared laser. NRh-Asp NPs was successfully used for visualizing DNPEP in vitro and in vivo in NIR region, and demonstrated good synergistic anti-cancer efficacy of PDT and PTT. These results suggest that DNPEP-mediated NRh-Asp NPs are promising candidates for image-guided phototherapeutic of tumor.

光疗已发展成为一种强有力的治疗方法。传统光敏剂处于“常亮”状态，缺乏肿瘤靶向性，治疗效果差，毒性大。因此，我们开发了一种天冬氨酰氨基肽酶 (DNPEP) 激活的自组装有机纳米粒子 (NRh-Asp NPs)，具有敏感的外部辐射诱导光热疗法和光动力疗法 (PTT/PDT)。NRh-Asp NPs可以被DNPEP激活为NRhNH ₂ NPs，表现出强烈的近红外（NIR）荧光，并在近红外激光下有效地产生热量和单线态氧。NRh-Asp NPs 成功用于在体外和体内可视化 DNPEP在 NIR 区域，显示了 PDT 和 PTT 良好的协同抗癌功效。这些结果表明，DNPEP 介导的 NRh-Asp NPs 是图像引导肿瘤光疗的有希望的候选者。