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  5. Labrasol® is an efficacious intestinal permeation enhancer across rat intestine: Ex vivo and in vivo rat studies
 
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Labrasol® is an efficacious intestinal permeation enhancer across rat intestine: Ex vivo and in vivo rat studies

Author(s)
McCartney, Fiona  
Jannin, Vincent  
Chevrier, Stephanie  
Hristov, Delyan R.  
Brayden, David James  
et al.  
Uri
http://hdl.handle.net/10197/10965
Date Issued
2019-09-28
Date Available
2019-08-12T07:37:39Z
Abstract
Labrasol® ALF (Labrasol®), is a non-ionic surfactant excipient primarily used as a solubilising agent. It was investigated here as an intestinal permeation enhancer in isolated rat colonic mucosae in Ussing chamber and in rat in situ intestinal instillations. Labrasol® comprises mono-, di- and triglycerides and mono- and di- fatty acid esters of polyethylene glycol (PEG)-8 and free PEG-8, with caprylic (C8)- and capric acid (C10) as the main fatty acids. Source components of Labrasol® as well as Labrasol® modified with either C8 or C10 as the sole fatty acid components were also tested to determine which element of Labrasol® was responsible for its permeability-enhancing properties. Labrasol® (4, 8 mg/ml) enhanced the transport of the paracellular markers, [14C] mannitol, FITC-dextran 4000, and FITC-insulin across colonic mucosae. The enhancement was non-damaging, transient, and molecular weight-dependent. The PEG ester fraction of Labrasol® also had enhancing properties. When insulin was administered with Labrasol® in instillations, it had a relative bioavailability of 7% in jejunum and 12% in colon. C8- and C10 versions of Labrasol® and the PEG ester fraction also induced similar bioavailability values in jejunal instillations: 6, 5 and 7% respectively. Inhibition of lipases in instillations did not reduce the efficacy of Labrasol®, suggesting that its mechanism as a PE is not simply due to liberated medium chain fatty acids. Labrasol® acts as an efficacious intestinal permeation enhancer and has potential for use in oral formulations of macromolecules and BCS Class III molecules.
Other Sponsorship
Gattefosse SAS
Type of Material
Journal Article
Publisher
Elsevier
Journal
Journal of Controlled Release
Volume
310
Start Page
115
End Page
126
Copyright (Published Version)
2019 Elsevier
Subjects

Oral peptide delivery...

Intestinal permeation...

Labrasol® ALF

Excipients

Epithelial tight junc...

DOI
10.1016/j.jconrel.2019.08.008
Language
English
Status of Item
Peer reviewed
ISSN
0168-3659
This item is made available under a Creative Commons License
https://creativecommons.org/licenses/by-nc-nd/3.0/ie/
File(s)
No Thumbnail Available
Name

McCartney accepted MS public version.docx

Size

2.95 MB

Format

Unknown

Checksum (MD5)

d048ffea1b78455243db299da4263001

Owning collection
Veterinary Medicine Research Collection
Mapped collections
Conway Institute Research Collection

Item descriptive metadata is released under a CC-0 (public domain) license: https://creativecommons.org/public-domain/cc0/.
All other content is subject to copyright.

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