: Dendrimers showed promise as carriers for oral delivery due to their nanoscale size and transepithelial permeability across the gut epithelium. However, for the successful approval of dendrimer-based oral therapeutics for human use, it is essential to understand their pharmacokinetics. The knowledge of pharmacokinetics of drugs delivered with dendrimers within the context of oral delivery of therapeutics will help in the design of clinical trials, and development of dosage regimens. : This review summarizes the pharmacokinetic aspects of dendrimer and dendrimer-drug complexes after oral administration. We discussed the influence of size, core chemistry, surface charge, surface chemistry, and modification on the pharmacokinetics of dendrimers and dendrimer-drug complexes. Furthermore, we also discussed studies involving alternative dosage forms such as matrix tablets containing dendrimers, dendrimers encapsulated in lipid nanostructures, and chitosan anchored-dendrimers. : From the studies, it is evident that dendrimers significantly improve the oral bioavailability of drugs with poor biopharmaceutical properties. However, further in vivo studies are needed to establish the relationship between the properties of dendrimers and oral pharmacokinetics of dendrimer-drug complexes and conjugates.