1: J Control Release. 2007 Apr 23;118(3):294-302. Epub 2006 Dec 29.

Helodermin-loaded nanoparticles: Characterization and transport across an in
vitro model of the follicle-associated epithelium.

des Rieux A, Fievez V, Momtaz M, Detrembleur C, Alonso-Sande M, Van Gelder J,
Cauvin A, Schneider YJ, Preat V.

Unite de Pharmacie Galenique, Universite catholique de Louvain, Avenue E.
Mounier, 73-20, 1200 Brussels, Belgium; Laboratoire de Biochimie cellulaire,
Institut des Sciences de la Vie, Universite catholique de Louvain, Croix du Sud,
5, 1348 Louvain-La-Neuve, Belgium.

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=3x10(-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.

PMID: 17292503 [PubMed - as supplied by publisher]

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