In recent years, polymeric scaffolds have been used in several biomedical applications for the delivery of drugs or other biologically relevant molecules. Polymeric nanostructures possess different (and in some cases more powerful) properties respect to bulk materials. This, leaded academic researchers and industry to cooperate in developing pioneering nanostructured materials for industrial and biomedical applications. Moreover, the preparation and use of systems with multiple (multifunctional) properties (i.e., bioconjugation with superparamagnetic, fluorescent or targeting molecules) will represent in the future a viable and innovative tool for application in several clinical fields. This brief critical review collects and discusses some recent patents about the preparation and use of these multifunctional nanoparticles in biomedicine and in non-invasive bioimaging applications.