Resveratrol (Res) is a promising molecule for.ghting cancer. However, the potential of the drug is immensely hindered by several limiting factors, including poor water solubility, limited chemical stability, and low bioavailability. In or-der to solve the above problems, we report a facile synthesis of a Res-loaded folate-terminated PEG-liposome (FA-PEG-Lip) coated mesoporous carbon nanotube (MCN) nanosystem (FA-PEG-Lip@MCN/Res) by simply sonicating Res and MCN in FA-PEG-Lip suspensions. The as-obtained FA-PEG-Lip@MCN/Res exhibits a nanoscale size [width: (80±10) nm, length: (600±100) nm], a negative surface potential (-10.2 mV), an excellent drug loading (131.59 mg/g MCN), good monodisper-sity and near infrared (NIR) laser stimulation-response release. Owing to folate receptor-mediated targeted delivery, the FA-PEG-Lip@MCN/Res nanosystem can deliver loaded Res to human breast cancer MCF-7 cells with high speci.city. The cell toxicity viability shows that unloaded FA-PEG-Lip@MCN has no cytotoxicity, confirming its suitability as a drug vehicle. In addition, a systematic in vitro and in vivo experiments demonstrated that, under NIR laser irradiation, the FA-PEG-Lip@ MCN/Res nanosystem exhibits highly e.cient chemotherapy/photothermal synergistic therapy. All in all, the FA-PEG-Lip@ MCN/Res nanosystem can simultaneously improve Res water solubility, enhance Res stability, extend plasma half-life of Res in mice, folate receptor targeting, NIR laser stimulation-response release, and synergistic tumor therapy, which may greatly promote the application of Res in clinical practice.