Carbon nanotubes (CNT) are increasingly being investigated for their use in biomedical applications and nanomedicine. An emergent need for the understanding of their in vivo biodistribution and pharmacokinetics is therefore needed to establish the essential properties and criteria for their further development as targeted CNT delivery systems to specific tissues for diagnostics and therapeutic purposes. Until their biodistribution and toxicoketic profiles are fully understood, their translation into the clinic will be hindered. This review will highlight the important factors affecting the biodistribution and pharmacokinetic profile of CNT and address their toxicokinetics following systemic, pulmonary and dermal exposure. © 2013 Elsevier B.V.