Abstract

A general scientific principle taught in the areas of biology and biochemistry is that structure determines function. This principle and its consequences have permeated other areas and disciplines, especially in the research and applications of nanomaterials. Particularly in nanoparticle applications to biomedical research, this leitmotiv drives the investigation and advances in nanomedicine, where to achieve effective findings, along bold biomedical applications, it is necessary to design the functionalization of nanoparticles as one of the main objectives. Nanoparticles’ functionalization determines properties such as wettability, stability, biochemical affinity, loading capacity, cell adhesion, intracellular delivery, toxicity, and therapeutic performance. In this chapter review, we present the main functionalization routes such as ligand exchange, phase transfer, bioconjugation, and orthogonal chemistry methods. First, a current overview regarding the global spread of nanotechnology, particularly applied to health sciences, is summarized. Then, to illustrate the effect of the nanomaterials’ surface functionalization and bioconjugation, we discuss punctual cases comprising inorganic nanoparticles, their initial development stages, and potential applications. Finally, the remaining challenge includes the safe-by-design of these nanoparticles that should increase clinic translation. And this goal may be achieved by developing more in situ, eco-friendly, low cost, scalable, efficient, and straightforward production routes.

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