Compared to bulk materials, because of quantum size effects and large surface area to volume ratio, nanomaterials have been proven to be a versatile substrate for different applications. As the nano-related industry continues to grow, nanotoxicology has become an emerging branch of toxicology that concerns itself with characterising the adverse effects resulting from the interactions between nanomaterials and biological systems explored. From the pharmacological and toxicological standpoints, before nanomaterials gains approval and enters into their practical uses, we must have the thoroughgoing understanding about its pharmaco- or toxico-kinetics information and disposition [absorption, distribution, metabolism, elimination (ADME)]. In terms of pharmacokinetics and toxicokinetics, the development of a useful analytical method is of utmost importance, since the accurate determination of the concentration of the substance of interest is indispensable in understanding the pharmacodynamic and toxicodynamic actions of nanomaterials.