The most used method to synthesize polymer prodrugs relies on direct conjugation of the drug to a preformed polymer via post-functionalization, also termed "grafting to" method. RDRP techniques have been extensively used to elaborate well-defined amphiphilic copolymers for subsequent self-assembly into nano-objects. Interestingly, the compatibility of RDRP with a wide range of functional groups and its ability to achieve complex macromolecular architectures allow predetermined positioning of functionalization sites on the polymer structure for subsequent coupling with drugs. This has direct consequences on the localization of the drugs (e.g., on the side chain or chain end of the copolymer, on the shell or in the core of the nano-object, etc.) and thus on their release kinetics. The "grafting to" strategy also allows drugs to be bound to polymers before or after their self-assembly, thus providing greater flexibility in achieving the desired structure.