Nanoparticles drug delivery system has sustained and controled release features as wel as targeted drug deliv-ery, which can change the characteristics of drug distributionin vivo. It can increase the stability of the drug and enhance drug bioavailability. The selective targeting of nanoparticles can be achieved through enhanced permeability and retention efect and a conjugated specific ligand or through the efects of physiological conditions, such as pH and temperature. Nanoparticles can be prepared by using a wide range of materials and can be used to encapsulate chemotherapeutic agents to reduce toxic-ity, which can be used for imaging, therapy, and diagnosis. In this research, recent progress on nanoparticles as a targeted drug delivery system wil be reviewed, including positive-targeting, negative-targeting, and physicochemical-targeting used as anticancer drug carriers.