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Open AccessArticle

New In Vitro Coculture Model for Evaluating Intestinal Absorption of Different Lipid Nanocapsules

1
MINT, INSERM U1066, CNRS UMR 6021, SFR ICAT, University of Angers, F-49000 Angers, France
2
SCIAM, SFR ICAT, University of Angers, F-49000 Angers, France
3
Laboratoire de Pharmacologie-Toxicologie, CRPV, Angers University Hospital Center, F-49000 Angers, France
*
Author to whom correspondence should be addressed.
Academic Editor: Ana Beloqui García
Pharmaceutics 2021, 13(5), 595; https://doi.org/10.3390/pharmaceutics13050595
Received: 6 April 2021 / Revised: 19 April 2021 / Accepted: 20 April 2021 / Published: 21 April 2021
(This article belongs to the Special Issue Oral Drug Delivery Systems Based on Lipid-Based Carriers)
Standard models used for evaluating the absorption of nanoparticles like Caco-2 ignore the presence of vascular endothelium, which is a part of the intestinal multi-layered barrier structure. Therefore, a coculture between the Caco-2 epithelium and HMEC-1 (Human Microvascular Endothelial Cell type 1) on a Transwell® insert has been developed. The model has been validated for (a) membrane morphology by transmission electron microscope (TEM); (b) ZO-1 and β-catenin expression by immunoassay; (c) membrane integrity by trans-epithelial electrical resistance (TEER) measurement; and (d) apparent permeability of drugs from different biopharmaceutical classification system (BCS) classes. Lipid nanocapsules (LNCs) were formulated with different sizes (55 and 85 nm) and surface modifications (DSPE-mPEG (2000) and stearylamine). Nanocapsule integrity and particle concentration were monitored using the Förster resonance energy transfer (FRET) technique. The result showed that surface modification by DSPE-mPEG (2000) increased the absorption of 55-nm LNCs in the coculture model but not in the Caco-2. Summarily, the coculture model was validated as a tool for evaluating the intestinal absorption of drugs and nanoparticles. The new coculture model has a different LNCs absorption mechanism suggesting the importance of intestinal endothelium and reveals that the surface modification of LNCs can modify the in vitro oral absorption. View Full-Text
Keywords: intestinal absorption; Caco-2; HMEC-1; apparent permeability; lipid nanocapsule; förster resonance energy transfer intestinal absorption; Caco-2; HMEC-1; apparent permeability; lipid nanocapsule; förster resonance energy transfer
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MDPI and ACS Style

Kaeokhamloed, N.; Roger, E.; Béjaud, J.; Lautram, N.; Manero, F.; Perrot, R.; Briet, M.; Abbara, C.; Legeay, S. New In Vitro Coculture Model for Evaluating Intestinal Absorption of Different Lipid Nanocapsules. Pharmaceutics 2021, 13, 595. https://doi.org/10.3390/pharmaceutics13050595

AMA Style

Kaeokhamloed N, Roger E, Béjaud J, Lautram N, Manero F, Perrot R, Briet M, Abbara C, Legeay S. New In Vitro Coculture Model for Evaluating Intestinal Absorption of Different Lipid Nanocapsules. Pharmaceutics. 2021; 13(5):595. https://doi.org/10.3390/pharmaceutics13050595

Chicago/Turabian Style

Kaeokhamloed, Norraseth; Roger, Emillie; Béjaud, Jérôme; Lautram, Nolwenn; Manero, Florence; Perrot, Rodolphe; Briet, Marie; Abbara, Chadi; Legeay, Samuel. 2021. "New In Vitro Coculture Model for Evaluating Intestinal Absorption of Different Lipid Nanocapsules" Pharmaceutics 13, no. 5: 595. https://doi.org/10.3390/pharmaceutics13050595

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