The development of nanomaterials has significantly impacted human history by covering most of the application areas. Nanobiomedicine and point-of-care devices are one of the critical application areas. The developments in these areas greatly impact drug and gene delivery, diagnostic imaging, infectious disease detection, regenerative medicine, and cancer therapeutics. Nanomaterials have many unique properties that are utilized in healthcare technologies, and several studies are being carried out to benefit from them for research and their real-life use in nanobiomedicine. Nanomaterials are selected according to their biological, chemical, and physical properties, which differ from their bulk forms. They do not have adequate features in their bare forms to be used in solutions for diagnostic, treatment, and detection systems. The functionalization strategies for nanomaterials have created many opportunities to modify nanomaterials and make them a good selection for different applications of nanobiomedicine and point-of-care. These strategies enhance diagnostic, targeting, detection, and biocompatibility properties while decreasing nanomaterials’ side effects. With the increasing popularity of nanomaterials, many developed functionalized strategies accelerated by creating more solutions for health technologies. These functionalization methods include several strategies, such as coating with polymers, conjugation with biomolecules, and modification with small ligands. Also, the developed technologies are enabled to functionalize the compounds that are already functionalized to take advantage of all of the properties of materials. This chapter provides a comprehensive literature review to demonstrate different functionalization strategies developed with nanomaterials for several application areas of nanobiomedicine and point-of-care in literature and discusses the future of nanomaterials in healthcare technologies.