Drug delivery system to deliver active reagents in a controlled manner is an important therapeutic challenge. In order to improve the efficiency, safety, and patient compliance of drugs, drug delivery researches have focused on how to reduce toxicity, increase absorption and distribution, and improve release profile. In our lab, we are focusing on multifunctional stimuli-responsive carbon dot-based systems for specific controllable targeting delivery of anticancer drugs (paclitaxel, doxorubicin, etc.) or therapeutic agents (photothermal agents, nitride oxide, etc.). By employing multiple responsive modified carbon dots such as pH, temperature, redox, etc., the release of drugs after injection can be controlled at desired tumor site with sustained release.