Oral drug delivery is the preferred route of administration of drugs. Because of their versatility, nanoparticles often have been investigated for the delivery of a wide number of drugs by this route. This article first examines the physicochemical, pharmaceutical and technological aspects that make nanoparticles a potential oral delivery system for drugs and active biomolecules. Next, upon consideration of in vivo studies, the pharmacokinetic, pharmacological and therapeutic aspects of orally administered nanoparticles are described. Special emphasis is placed on improvement of oral bioavailability of drugs incorporated into nanoparticles. Two main mechanisms involved in enhancing drug absorption are discussed: the protection of drug by nanoparticles against harsh conditions in the gut and the prolongation of gastrointestinal transit of nanoparticles by using bioadhesive polymers. Furthermore, nanoparticle uptake by intestinal cells and oral vaccination by these colloidal carriers are also covered. In this context, the immune responses elicited as well as the protection against pathogens induced by antigen-loaded nanoparticles administered by the oral route are presented. Finally, the main limitations and perspectives of these colloidal carriers as oral drug delivery systems are discussed.