Glycotargeting relies on carrier molecules possessing carbohydrates that are recognized and internalized by cell surface mammalian lectins. Numerous types of glycotargeting vehicles have been designed based on the covalent attachment of saccharides to proteins, polymers and other aglycones. These carriers have found their major applications in antiviral therapy, immunoactivation, enzyme replacement therapy and gene therapy. This review compared different types of glycotargeting agents and the lectins which have been successfully targeted to treat both model and human diseases. It may be concluded that the discovery of new mammalian lectins which endocytose their ligands will lead to the rapid development of new glycotargeting agents founded on the principles of carbohydrate-protein interactions.