A major field in cancer research is to develop carriers that can deliver drugs into targeted region effectively without side effects. Polymeric micelles (PMs) are core-shell structure with diameters of 10~100nm (suitable size with a narrow distribution could avoid rapid renal excretion and entrapment by the reticuloendothelial system)

which are self-assembled with good biodegradable and biocompatible polymer to form hydrophobic core and hydrophilic shell in an aqueous media. The preparation of PMs with stimuli-responsive block copolymers and modification of target molecules on PMs’ surface could significantly improve the performance of the drug-loaded

enhance drug utilization and anti-tumor activity

reduce the normal tissue toxicity and solve the problem of multi-drug resistance

and thus contribute significantly to the development and progress of chemotherapy. Here we review some of the promising analog of targeting strategies that are under development for drug delivery. This review describes the preparation of polymeric micelles and the targeted modification which greatly enhance the effect of chemotherapy.