Targeted drug delivery systems (TDDSs) can selectively react with the targeted tissue at cell and subcell level,and can also selectively reach the diseased site and release the drugs slowly,which maintain the drug concentration above an efficaciously critical value for a longer duration of time. For TDDSs of anticancer drugs, such kind of preparations can efficiently minimize the side effects to the undesired tissues or organs, consequently augmenting curative effects of chemotherapy. We summarize the present situation and recent progresses in the prospective field of TDDSs for anticancer drugs. The models of drug targeting, the categories of drug targeting, the targeted drug carriers, and the factors that influence the effect of targeting are introuduced through domestic literatures.Although it is not very near future for clinical application of TDDSs,TDDSs play an important role in overcoming the side effects of cancer therapy and improve curative effect.