Well‐defined amphiphilic PLA‐b‐PMPC diblock copolymers were synthesized. Bimimetic micelles were prepared and applied for release of anti‐cancer drugs (DOX). TEM and DLS analysis revealed a regular spherical shape with small diameter (less than 50 nm) of the micelle. The biocompatibility of PLA‐b‐PMPC micelles was studied, and it was found that the micelles possessed excellent cytocompatibility due to the zwitterionic phosphorylcholine group. DOX could be efficiently loaded into the micelles with a loading efficiency of 44–67%. The DOX‐loaded micelles showed lower cytotoxicity than free drugs and efficiently delivered and released the drug into cancer cells. With these properties, the PLA‐b‐PMPC polymer micelles are attractive as drug carriers for pharmaceutical application.