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- Title
New In Vitro Coculture Model for Evaluating Intestinal Absorption of Different Lipid Nanocapsules.
- Authors
Kaeokhamloed, Norraseth; Roger, Emillie; Béjaud, Jérôme; Lautram, Nolwenn; Manero, Florence; Perrot, Rodolphe; Briet, Marie; Abbara, Chadi; Legeay, Samuel; García, Ana Beloqui
- Abstract
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.
- Subjects
INTESTINAL absorption; FLUORESCENCE resonance energy transfer; NANOCAPSULES; TRANSMISSION electron microscopes; VASCULAR endothelium; DRUG absorption; INTESTINES; SKIN permeability
- Publication
Pharmaceutics, 2021, Vol 13, Issue 5, p595
- ISSN
1999-4923
- Publication type
Article
- DOI
10.3390/pharmaceutics13050595