Abstract: Chemotherapy is one of the common ways for clinical cancer therapy. In most cases, patients are treated with chemotherapeutic drugs by intravenous injection. The cytotoxic drugs in bloodstream not only can be delivered to the tumor tissues, but also can spread to the whole body, and cause side effects. The latest research shows that gold nanoparticles is a highly effective anti-tumor drug carrier, which can carry drugs through blood vessels and tissue barriers into tumor lesions, and specifically accumulate in tumor tissues, effectively reducing the adverse effects of chemotherapy drugs in the body. In comparison with other nanomaterials, gold nano particles are easier to be modified with multiple compounds, proteins and nucleic acids, and possesses unique advantages for the application in tumor imaging and treatment. This paper summarizes the research progress on tumor-targeted drug delivery induced by gold nanoparticles, and elaborated the merits and demerits of gold nanoparticles in surface modification, targeting strategies and biosecurity.