Lipid nanocapsules maintain full integrity after crossing a human intestinal epithelium model

Lipid nanocapsules (LNCs) have demonstrated great potential for the oral delivery of drugs having very limited oral bioavailability (BCS class II, III and IV molecules). It has been shown previously that orally-administered LNCs can permeate through mucus, increase drug absorption by the epithelial...

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Bibliographic Details
Published inJournal of controlled release Vol. 253; pp. 11 - 18
Main Authors Roger, Emilie, Gimel, Jean-Christophe, Bensley, Conor, Klymchenko, Andrey S., Benoit, Jean-Pierre
Format Journal Article
LanguageEnglish
Published Netherlands Elsevier B.V 10.05.2017
Elsevier
Subjects
Caco-2
Caco-2 Cells
Fluorescence Resonance Energy Transfer
Fluorescent Dyes - administration & dosage
Fluorescent Dyes - pharmacology
FRET
Humans
Integrity
Intestinal Mucosa - metabolism
Intestinal transport
Life Sciences
Lipids - administration & dosage
Lipids - pharmacology
Models, Biological
Nanocapsules
Nanocapsules - administration & dosage
Pharmaceutical sciences
Polyethylene Glycols - administration & dosage
Polyethylene Glycols - pharmacology
Transcytosis
FRET
Caco-2
Intestinal transport
Nanocapsules
Integrity
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Summary:Lipid nanocapsules (LNCs) have demonstrated great potential for the oral delivery of drugs having very limited oral bioavailability (BCS class II, III and IV molecules). It has been shown previously that orally-administered LNCs can permeate through mucus, increase drug absorption by the epithelial tissue, and finally, increase drug bioavailability. However, even if transport mechanisms through mucus and the intestinal barrier have already been clarified, the preservation of particle integrity is still not known. The aim of the present work is to study in vitro the fate of LNCs after their transportation across an intestinal epithelium model (Caco-2 cell model). For this, two complementary techniques were employed: Förster Resonance Energy Transfer (FRET) and Nanoparticle Tracking Analysis (NTA). Results showed, after 2h, the presence of nanoparticles in the basolateral side of the cell layer and a measurable FRET signal. This provides very good evidence for the transcellular intact crossing of the nanocarriers. Graphical abstract [Display omitted]
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ISSN:0168-3659
1873-4995
DOI:10.1016/j.jconrel.2017.03.005