title: Helodermin-loaded nanoparticles: characterization and transport across an in vitro model of the follicle-associated epithelium.
abstract: M cells represent a potential portal for oral delivery of peptides and proteins due to their high endocytosis abilities. An in vitro model of human FAE (co-cultures) was used to evaluate the influence of M cells on the transport of free and encapsulated helodermin--a model peptide--across the intestinal epithelium. M cells enhanced transport of intact helodermin (18-fold, Papp=3 x 10(-6) cm s(-1)). As pegylation increased nanoparticle transport by M cells, helodermin was encapsulated in 200 nm nanoparticles containing PEG-b-PLA:PLGA 1:1. Stability of the selected formulation was demonstrated in simulated gastric and intestinal fluids. M cells increased the transport of helodermin encapsulated in these nanoparticles by a factor of 415, as compared to Caco-2 cells. Transport of free and encapsulated helodermin occurred most probably by endocytosis. In conclusion, M cells improved helodermin transport across the intestinal epithelium, confirming their high potential for oral delivery of peptides.
authors.affiliation: Unité de Pharmacie Galénique, Université catholique de Louvain, Brussels, Belgium.
authors.forename: Anne
authors.initials: A
authors.lastname: des Rieux
authors.forename: Virginie
authors.initials: V
authors.lastname: Fievez
authors.forename: Maryam
authors.initials: M
authors.lastname: Momtaz
authors.forename: Christophe
authors.initials: C
authors.lastname: Detrembleur
authors.forename: Maria
authors.initials: M
authors.lastname: Alonso-Sande
authors.forename: Jan
authors.initials: J
authors.lastname: Van Gelder
authors.forename: Annick
authors.initials: A
authors.lastname: Cauvin
authors.forename: Yves-Jacques
authors.initials: YJ
authors.lastname: Schneider
authors.forename: Véronique
authors.initials: V
authors.lastname: Préat
mesh_terms: D018938:Caco-2 Cells; D004337:Drug Carriers / Q000008:administration & dosage / Q000493:pharmacokinetics; D006801:Humans; D036341:Intercellular Signaling Peptides and Proteins; D007408:Intestinal Absorption / Q000187:drug effects / Q000528:radiation effects; D007413:Intestinal Mucosa / Q000187:drug effects / Q000378:metabolism*; D008954:Models, Biological; D053758:Nanoparticles / Q000008:administration & dosage*; D010455:Peptides / Q000008:administration & dosage* / Q000493:pharmacokinetics*; D021381:Protein Transport / Q000187:drug effects / Q000502:physiology
chemical_list: D004337:Drug Carriers; D036341:Intercellular Signaling Peptides and Proteins; D010455:Peptides; C040442:heliodermin