Helodermin-loaded nanoparticles: characterization and transport across an in vitro model of the follicle-associated epithelium
(2007) Journal of Controlled Release — Vol. 118, n° 3, p. 294-302 (2007)
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- Authors
Schneider, Yves-Jacques 
- 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.
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Citations
des Rieux, A., Fievez, V., Momtaz, M., Detrembleur, C., Alonso-Sande, M., Van Gelder, J., Cauvin, A., Schneider, Y.-J., & Préat, V. (2007). Helodermin-loaded nanoparticles: characterization and transport across an in vitro model of the follicle-associated epithelium. Journal of Controlled Release, 118(3), 294-302. https://doi.org/10.1016/j.jconrel.2006.12.023 (Original work published 2007)