The integration of composite functions in one material is a great promise towards personalized nanomedicine, aiming at enhancing the therapeutic efficacy of drugs and avoiding under- or over-treatment of specific diseases. Multi-tasked molecules, as well as self-assembled systems and functionalized nanosized particles are promising candidates for delivering drugs to the biological target. Particular interest is devoted to the study of the physico-chemical properties, structural features and colloidal stability of multi-functionalized vesicles spontaneously formed by amphiphilic macromolecules or of multi-functionalized nanoparticles. Their validation in terms of cell uptake or photodynamic properties (for those species possessing specific chromophores) is also performed by exploiting fluorescence microscopy or the spectroscopic response under light irradiation (oxygen radicals production). The kinetics of the release and the stability of the drug in an environment mimicking the biological target are also investigated.