Receptor-targeted delivery systems have been proposed as means of concentrating therapeutic agents to improve therapeutic effects on disease sites and reduce side effects on normal issues. Herein, we synthesized biocompatible folic acid (FA)-functionalized DHE-modified TiP (TiP-PAH-DHE-FA) nanoparticles as a drug delivery system that possessed high drug loading capability and enhanced folate-receptor-mediated cellular uptake. Moreover, it also allowed drug effect evaluation based on the real-time monitoring of the fluorescence intensity of HE molecules that are triggered by intercellular ROS. This acquired drug delivery system provided a novel platform to integrate efficient cell-specific drug delivery with real-time monitoring of therapeutic efficacy.