Emancipating Target‐Functionalized Carbon Dots from Autophagy Vesicles for a Novel Visualized Tumor Therapy

Abstract Killing the tumor cells by a visualized targeting system is a promising strategy with which to achieve high efficiency, low side effects, and a high survival rate for tumor therapy. Here, an autophagy regulation strategy is reported by emancipating target‐functionalized carbon dots from autophagy vesicles for the efficient visualized tumor therapy. The folic acid modified N‐doped carbon dots (FN‐CDs) are selectively endocytosed (specific cellular uptake rate >93.40%) and stably existed in autophagic vacuoles in tumor cells. Next, the autophagic vacuoles are “opened” by the autophagy inhibitors. Released FN‐CDs activate both the intrinsic and extrinsic apoptotic signaling pathway and kill tumor cells efficiently. This method achieves therapeutic effects with high performance in 26 types of tumor cell lines. Animal experiments show that the 30 d survival rate of this therapeutic strategy is much higher than that with traditional drug treatment. Real‐time imaging/monitoring and its effects on the intelligent tumor therapy are also demonstrated based on the stable, strong, green emission from FN‐CDs.