Upconverting nanoparticles have attracted a large amount of interest, primarily due to their attractive potential applications in bioimaging and therapy. This chapter reviews different methods of synthesis for the preparation of upconverting nanoparticles, covering the theory of nucleation and growth, as well as a wide range of methods, for example, arrested precipitation, hot injection, microemulsion and microwave-assisted techniques. Finally, some examples for bio/ medical applications of upconverting nanoparticles are discussed.