Based on the fact that oligosaccharides encode biological information, the biorecognition between lectinised drug delivery systems and glycosylated structures in the intestine can be exploited for improved peroral therapy. Basic research revealed that some lectins can mediate mucoadhesion, cytoadhesion, and cytoinvasion of drugs. Entering the vesicular pathway by receptor mediated endocytosis, part of the conjugated drug is accumulated within the lysosomes. Additionally, part of the drug is supposed to be transported across the epithelium. Moreover, factors probably adversely influencing feasibility of the concept such as toxicity, immunogenicity, and intestinal stability of plant lectins are discussed. As exemplified by lectin-grafted prodrug and carrier systems, this strategy is expected to improve absorption and probably bioavailability of poorly absorbable drugs, peptides and proteins as well as therapeutic DNA.