Selenium nanoparticles present an enhanced genetic actions and possess superior adsorptive capacity due to the interaction between the nanoparticles and NH, C=O, COO- and C-N groups of proteins. This review is focused on the biomedical applications of surafce funtionalized selenium nanoparticles. The engineering of exterior surface of the selenium nanoparticles has further emphasizing on the recent progresses in regulating monolayer structures for competent delivery of drugs and biomolecules. Crucial queries of transport, uptake, and clearance are discussed and illustrated through the prospects of selenium nanoparticles. The work presents an insight of how biomedical research can evolve with selenium nanoparticles and where we see the field is heading in the near future.