Oxidation modulators regarding antioxidants and reactive oxygen species (ROS) inducers have been used for the treatment of many diseases. However, a systematic review that refers to delivery system for divergent modulation of oxidative level within the biomedical scope is lacking. To provide a comprehensive summarization and analysis, we review pilot designs for delivering the oxidative modulators and the main applications for inflammatory treatment and tumor therapy. On the one hand, the antioxidants based delivery system can be employed to downregulate ROS levels at inflammatory sites to treat inflammatory diseases (e.g., skin repair, bone-related diseases, organ dysfunction, and neurodegenerative diseases). On the other hand, the ROS inducers based delivery system can be employed to upregulate ROS levels at the tumor site to kill tumor cells (e.g., disrupt the endogenous oxidative balance and induce lethal levels of ROS). Besides the current designs of delivery systems for oxidative modulators and the main application cases, prospects for future research are also provided to identify intelligent strategies and inspire new concepts for delivering oxidative modulators.