The present invention is directed to particle comprising a drug and a ligand, and to method of making them and use thereof. Particularly, the present invention results in the covalent entrapment of drug(s) in high amounts in polymer carriers, such as (nano)particle, microspheres and other types of polymer devices for controlled release. The polymer carriers or devices can be decorated with ligands, allowing for targeting specific tissues and/or (non-) invasive monitoring.