Superparamagnetic iron-oxide nanoparticles with tailored surface chemistry may be regarded as one of the most popular multifunctional materials for biomedical applications. Their unique capabilities to enhance the proton relaxation of specific tissues, coupled with outstanding magnetic manipulability make them highly promising probes/ vectors for magnetic resonance imaging (MRI) contrast enhancement, magnetic fluid hyperthermia (MFH) for selective destruction of cancer cells and magnetically modulated drug or gene delivery. The present study contributes some new tool-boxes for the facile, water-based synthesis of biocompatible coating-stabilized multifunctional iron-oxide nanoparticles (MNPs), simultaneously integrated with fluorophores, targeting agents and/ or chemotherapeutic drugs. Herein, we describe some novel strategies to design and synthesize theragnostic MNPs that can simultaneously trace, target and kill cancer cells while allowing a real time monitoring of drug delivery through combined MR and fluorescence imaging.