ROS-triggered cycle amplification effect: A prodrug activation nanoamplifier for tumor-specific therapy

ROS 引发的循环放大效应:用于肿瘤特异性治疗的前体药物活化纳米放大器

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作者:Zeqian Huang, Yaqing Ding, Yong Luo, Meixu Chen, Zishan Zeng, Tao Zhang, Yue Sun, Yanjuan Huang, Chunshun Zhao

Significance

Owing to the striking difference in ROS level between cancer cells and normal cells, ROS-responsive prodrugs are regarded as a promising approach for tumor-specific therapy. However, the stability and responsiveness of prodrugs are hard to balance. Preferable sensitivity may cause premature activation while favorable stability may lead to incomplete prodrug activation and insufficient active drug release. This study provides a tailored ROS-responsive prodrug activation nanoamplifier with favorable stability and effective prodrug activation capacity. The nanoamplifier can undergo a self-amplifying positive feedback loop to achieve numerous bioactive drugs generation in situ under ROS triggers within the tumor microenvironment, showing the enhanced antitumor therapeutic effect. Thus, this study provides a new strategy for prodrug activation and tumor-specific therapy.

Statement of significance

Owing to the striking difference in ROS level between cancer cells and normal cells, ROS-responsive prodrugs are regarded as a promising approach for tumor-specific therapy. However, the stability and responsiveness of prodrugs are hard to balance. Preferable sensitivity may cause premature activation while favorable stability may lead to incomplete prodrug activation and insufficient active drug release. This study provides a tailored ROS-responsive prodrug activation nanoamplifier with favorable stability and effective prodrug activation capacity. The nanoamplifier can undergo a self-amplifying positive feedback loop to achieve numerous bioactive drugs generation in situ under ROS triggers within the tumor microenvironment, showing the enhanced antitumor therapeutic effect. Thus, this study provides a new strategy for prodrug activation and tumor-specific therapy.

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