Nanoparticles (NPs) have been widely used in different areas, including consumer products and medicine. In terms of biomedical applications, NPs or NP-based drug formulations have been extensively investigated for cancer diagnostics and therapy in preclinical studies, but the clinical translation rate is low. Therefore, a thorough and comprehensive understanding of the pharmacokinetics of NPs, especially in drug delivery efficiency to the target therapeutic tissue tumor, is important to design more effective nanomedicines and for proper assessment of the safety and risk of NPs. This review article focuses on the pharmacokinetics of both organic and inorganic NPs and their tumor delivery efficiencies, as well as the associated mechanisms involved. We discuss the absorption, distribution, metabolism, and excretion (ADME) processes following different routes of exposure and the mechanisms involved. Many physicochemical properties and experimental factors, including particle type, size, surface charge, zeta potential, surface coating, protein binding, dose, exposure route, species, cancer type, and tumor size can affect NP pharmacokinetics and tumor delivery efficiency. NPs can be absorbed with varying degrees following different exposure routes and mainly accumulate in liver and spleen, but also distribute to other tissues such as heart, lung, kidney and tumor tissues; and subsequently get metabolized and/or excreted mainly through hepatobiliary and renal elimination. Passive and active targeting strategies are the two major mechanisms of tumor delivery, while active targeting tends to have less toxicity and higher delivery efficiency through direct interaction between ligands and receptors. We also discuss challenges and perspectives remaining in the field of pharmacokinetics and tumor delivery efficiency of NPs.
Keywords: Pharmacokinetics; drug delivery; nanomedicine; nanoparticle; tumor delivery.