The application of Nanocarriers (NCs) provides a promising strategy to solve the problems faced by traditional chemotherapy drugs, like the imprecise delivery, poor bioavailability, high dose requirement, and the tendency to develop multidrug resistance. With the protection of NCs, chemotherapy drugs can reach the lesion site and then release accurately and completely. Although some reviews have summarized the biological applications of NCs, little attention has been given to the advantages and disadvantages of analyzing organic, inorganic, and hybrid NCs separately for targeted therapy and identifying means to further improve the targeting ability. First, in this review, we emphasize three factors that have a marked impact on targeted therapy: the tumor microenvironment (TME), the different administration modalities (intravenous, oral, and intracavitary administration), and the targeting pathways (passive and active). Second, a systematic examination of the advantages and disadvantages of polymeric NCs, dendrimers, micelles, liposomes, mesoporous silica NCs, gold NCs, quantum dots, nano clay, core-shell NCs, and MOFs for targeted therapy are reviewed. Further, we propose three ways to improve the efficiency of targeted therapy, including regulating the size, shape, and surface properties of NCs.