Functionalized platinum nanoparticles have been of considerable interest in recent research due to their properties and applications, among which they stand out as therapeutic agents. The functionalization of the surfaces of nanoparticles can overcome the limits of medicine by increasing selectivity and thereby reducing the side effects of conventional drugs. With the constant development of nanotechnology in the biomedical field, functionalized platinum nanoparticles have been used to diagnose and treat diseases such as cancer and infections caused by pathogens. This review reports on physical, chemical, and biological methods of obtaining platinum nanoparticles and the advantages and disadvantages of their synthesis. Additionally, applications in the biomedical field that can be utilized once the surfaces of nanoparticles have been functionalized with different bioactive molecules are discussed, among which antibodies, biodegradable polymers, and biomolecules stand out.