Recent developments in nanotechnology have paved the way for using quantum dots (QDs) in nanodiagnostics and nanotherapeutics. Careful design and preparation of QDs are guided by these application-specific requirements. QDs will probably be one of the first nanomaterial to reach clinical applications, however many challenges in this field have yet to be overcome. In this article, we present an extensive review of the pharmacokinetic properties of QDs. The representative studies responsible for observing quantitative determination of QDs biodistribution in vivo are presented. The effects of size, surface chemistry, and target moiety on their pharmacokinetics are discussed. Finally, future directions for improving the pharmacokinetics of QDs and perspectives in the field are discussed. The understanding of its absorption, distribution, metabolism, and excretion from the body will provide important guidelines for the successful clinical use of QDs.