Low water solubility, rapid phagocytic and renal clearance, and systemic toxicity represent three major barriers that limit the therapeutic use of many hydrophobic antitumor agents such as doxorubicin (DOXO) and paclitaxel.[1] Various drugdelivery systems, among which polymeric micelles have emerged as a very important system, have been developed to overcome these limitations and deliver various drugs with remarkable in vitro and in vivo success.[2, 3] Polymeric micelles are nanoscopic (10 to 100 nm) colloidal particles self-assembled from amphiphilic block or graft copolymers in aqueous media. The hydrophobic core of the micelles is a carrier compartment that accommodates antitumor drugs, and the shell consists of a brushlike protective corona that stabilizes the nanoparticles in aqueous solution.[4] The basic requirements for polymeric micelles in drug-delivery applications include high drug-loading capacity, biodegradability, long blood circulation times, and controllable drug-release profiles. Research on micelles has been greatly advanced in the Scheme 1. Synthesis of MAL-PEG-PCL copolymer and preparation of cRGD-functionalized, DOXO-loaded micelles.