Semiconductor quantum dots exhibit excellent optical and electronic properties such as broad absorption, narrow emission, and remarkable photostability, rendering them promising candidates for a variety of applications. This chapter introduces the synthesis, surface functionalization, physicochemical properties, and biomedical applications of different types of quantum dots, with focus on their biomedical applications, such as biological imaging, targeted drug delivery and cancer therapy. A brief discussion on the toxicity of quantum dots, as well as the future directions of quantum dots nanotheranostics, is also presented.