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Abstract

The possibility of developing bioadhesive drug delivery systems on the basis of molecules which selectively bind to the small intestinal epithelium by specific, receptor-mediated mechanisms was investigated using a lectin isolated from tomato fruits (Lycopersicum esculentum). The tomato lectin (TL) was found to bind specifically onto both isolated, fixed pig enterocytes and monolayers of human Caco-2 cell cultures with a similar affinity. TL-coated polystyrene microspheres (0.98 micron) also showed specific binding to enterocytes in vitro. Lectin binding was found to be favored at neutral pH and to be reduced in an acidic environment. Crude pig gastric mucin, however showed a marked cross-reactivity in vitro, indicating that lectin binding to the cell surface in vivo might be inhibited by mucus.

Nanoparticles for oral delivery: Targeted nanoparticles with peptidic ligands for oral protein delivery

“…They are involved in many cell recognition and adhesion processes. Their conjugation to polymeric nanoparticles significantly increases their transport across the intestinal mucosa by efficiently increasing interactions with the mucus [27, 123, 124] and/or the surface of the epithelial cells [125] and by promoting particle translocation [123, 126]. The association of lectins with nanoparticles can be achieved by adsorption or covalent coupling, with a definite preference for a covalent linkage, if conjugation does not affect lectin activity and specificity.…”

Mucoadhesive Microspheres for Controlled Drug Delivery

“…14) Microspheres, in general, have the potential to be used for targeted and controlled release drug delivery; but coupling of mucoadhesive properties to microspheres has additional advantages, e.g. efficient absorption and enhanced bioavailability of the drugs due to a high surface to volume ratio, a much more intimate contact with the mucus layer, specific targeting of drug to the absorption site achieved by anchoring plant lectins, 15) bacterial adhesions 16) and antibodies, 17) etc. on the surface of the microspheres.…”

Plant Lectins as Medical Tools against Digestive System Cancers

“…Several plant lectins have been used for this purpose and have been aimed toward specific cells and tissues (direct lectin targeting) [ 192 ]. An increase in the cellular uptake of lectin-conjugated particles has been reported [ 193 ]. Another modality of targeted drug delivery consists of glycans coupled to nanoparticles to target endogenous lectins within specific tissues (reverse lectin targeting) [ 194 , 195 ].…”