Nanotechnology has promising applications in biomedicine, such as in drug delivery, diagnosis, and tissue engineering. The pharmacokinetics of nanomaterials significantly affects their biological behavior in vivo, affecting their biomedical applications and potential nanotoxicity. In this review, we highlight some recent advances in the pharmacokinetic studies of representative nanomaterials. We focus on the relationships between the physicochemical properties of nanomaterials and physiological consequences.