Magnetic nanoparticles (MNPs), particularly made of iron oxides, have been extensively studied as diagnostic imaging agents and therapeutic delivery vehicles. In this review, special emphasis is set on the 'recent advancements of drug-conjugated MNPs used for therapeutic applications'. The most prevalent preparation methods and chemical functionalization strategies required for translational biomedical nanoformulations are outlined. Particular attention is, then, devoted to the tailored conjugation of drugs to the MNP carrier according to either noncovalent or covalent attachments, with advantages and drawbacks of both pathways conferred. Notable examples are presented to demonstrate the advantages of MNPs in respective drug-delivery applications. Understanding of the preparation, conjugation and delivery processes will definitely bring, in the next decades, a novel magneto-nanovehicle for effective theranostics.