title: Targeted nanoparticles with novel non-peptidic ligands for oral delivery.
abstract: Orally administered targeted nanoparticles have a large number of potential biomedical applications and display several putative advantages for oral drug delivery, such as the protection of fragile drugs or modification of drug pharmacokinetics. These advantages notwithstanding, oral drug delivery by nanoparticles remains challenging. The optimization of particle size and surface properties and targeting by ligand grafting have been shown to enhance nanoparticle transport across the intestinal epithelium. Here, different grafting strategies for non-peptidic ligands, e.g., peptidomimetics, lectin mimetics, sugars and vitamins, that are stable in the gastrointestinal tract are discussed. We demonstrate that the grafting of these non-peptidic ligands allows nanoparticles to be targeted to M cells, enterocytes, immune cells or L cells. We show that these grafted nanoparticles could be promising vehicles for oral vaccination by targeting M cells or for the delivery of therapeutic proteins. We suggest that targeting L cells could be useful for the treatment of type 2 diabetes or obesity.
authors: Université catholique de Louvain, Louvain Drug Research Institute, Pharmaceutics and Drug Delivery Research Group, Avenue E. Mounier, 73 B1.73.12, 1200 Brussels, Belgium.
authors: Anne
authors: A
authors: des Rieux
authors: Vincent
authors: V
authors: Pourcelle
authors: Patrice D
authors: PD
authors: Cani
authors: Jacqueline
authors: J
authors: Marchand-Brynaert
authors: Véronique
authors: V
authors: Préat
mesh_terms: D000284:Administration, Oral; D001682:Biological Availability; D002241:Carbohydrates / Q000008:administration & dosage / Q000493:pharmacokinetics; D004337:Drug Carriers / Q000008:administration & dosage* / Q000493:pharmacokinetics*; D041981:Gastrointestinal Tract / Q000378:metabolism*; D006801:Humans; D007413:Intestinal Mucosa / Q000378:metabolism; D053758:Nanoparticles / Q000008:administration & dosage* / Q000737:chemistry; D010316:Particle Size; D011506:Proteins / Q000008:administration & dosage* / Q000493:pharmacokinetics; D011956:Receptors, Cell Surface / Q000378:metabolism; D014815:Vitamins / Q000008:administration & dosage / Q000493:pharmacokinetics
chemical_list: D002241:Carbohydrates; D004337:Drug Carriers; D011506:Proteins; D011956:Receptors, Cell Surface; D014815:Vitamins