Abstract: Cell-penetrating peptides(CPPs) is a class of small molecules peptides which can penetrate cell membrane. CPPs can efficiently load siRNA, functional proteins, small molecule drugs and some other functional fragments of the polypeptide into cells. Researchers take matrix metalloproteinases(MMPs) at high concentrations, over-expressed receptors and the acidic microenvironment in tumor tissues as the targets for reforming CPPs. A number of new tumor-targeted CPPs derivatives are designed and synthesized. They can load some traditional anticancer molecules and educe efficient targeting effect to tumor cells, and enrich the drugs around the tumor tissues. They not only reduce the toxicity of drugs to normal tissues, but also improve the efficiency of the drugs. In this paper, we review the design strategy of targeted CPPs and its research progress in terms of anti-tumor.