Due to their special physicochemical, optical, and biological properties, noble metal nanoparticles have huge potential for application in many different biological and medical areas, such as highly sensitive diagnostic assay, thermal ablation, radiotherapy, or carriers for drugs and gene delivery. This chapter selectively reviews the bio-functionalization of metallic nanoparticles and their recent applications in medicine. The chapter is divided into four sections: Introduction, Bioconjugation of Metallic Nanoparticles, Cancer Therapy, and Gene Delivery. After a short introduction, we present few general strategies for bioconjugation of metallic nanoparticles: physisorption, physisorption using mediator molecules, covalent binding of biomolecules to cross-linkers, covalent binding of biomolecules to nanoparticles, and linking of biotinylated biomolecules to streptavidin-functionalized nanoparticles. The third section presents the recent advances in cancer therapy based on two strategies: passive targeting and antibody targeting, using functionalized gold nanoparticles. The fourth section describes the gene delivery process, by which foreign DNA is introduced into the host cells. The process typically involves the formation of transient pores or "holes" into the cell membrane, which allows the uptake of foreign material. The main aspects that are discussed about the gene delivery process are the stealth character and the targeted recognition of tissues.