Most anticancer drugs cause severe side effect due to the lack of selectivity for cancer cells. In recent years, new strategies of micellar systems, which design for specifically target anticancer drugs to tumors, are developed at the forefront of polymeric science. To improve efficiency of delivery and cancer specificity, considerable emphasis has been placed on the development of micellar systems with passive and active targeting. In this review article, we summarized various strategies of designing multifunctional micellar systems in the purpose of improving delivery efficiency. Micellar systems compose of a multifunctional copolymer or a mixture of two or more copolymers with different properties is a plausible approach to tuning the resulting properties and satisfied various requirements for anticancer drug delivery. It appears that multifunctional micellar systems hold great potential in cancer therapy. © 2013 Wiley Periodicals, Inc. J Biomed Mater Res Part A: 102A: 2024–2038, 2014.