Linked Life Data

15067707

Source:http://linkedlifedata.com/resource/pubmed/id/15067707

Statements in which the resource exists as a subject.
PredicateObject
rdf:type
lifeskim:mentions
pubmed:issue
5
pubmed:dateCreated
2004-4-6
pubmed:abstractText
Delta G (DeltaG) is the biologically active fragment of Zonula Occludens Toxin (Zot), an absorption enhancer, that reversibly opens the tight junctions of epithelial and endothelial cells in the small intestine and brain. This study evaluates the possible use of DeltaG in enhancing the oral bioavailability of macromolecules using large paracellular markers as model agents. The transport of [(14)C]Inulin and [(14)C]PEG4000 was evaluated across Caco-2 cells with DeltaG (0, 100, 180 microg/ml). The apparent permeability coefficients (P(app)) were calculated. The in vitro toxicity of DeltaG (180 microg/ml) was assessed. Sprague Dawley rats were dosed intraduodenally (ID) with the following treatments: [(14)C]Inulin or [(14)C]PEG4000 (30 microci/kg) w/o DeltaG (720 microg/kg)/protease inhibitors (PI). Blood was collected and plasma was analyzed for radioactivity. DeltaG (180 microg/ml) increased [(14)C]Inulin and [(14)C]PEG4000 P(app) by 82.6 and 24.4%, respectively, without any toxicity. After ID administration with DeltaG/PI, C(max) and AUC were significantly (p < 0.05) increased for both Inulin and PEG4000. However, Inulin displayed greater enhancement ratios in vitro and in vivo. This study suggests that DeltaG may be used to enhance the oral bioavailability of macromolecules (e.g., proteins) after coadministration through modulation of paracellular transport.
pubmed:grant
pubmed:language
eng
pubmed:journal
pubmed:citationSubset
IM
pubmed:chemical
pubmed:status
MEDLINE
pubmed:month
May
pubmed:issn
0022-3549
pubmed:author
pubmed:copyrightInfo
Copyright 2004 Wiley-Liss, Inc. and the American Pharmacists Association J Pharm Sci 93:1310-1319, 2004
pubmed:issnType
Print
pubmed:volume
93
pubmed:owner
NLM
pubmed:authorsComplete
Y
pubmed:pagination
1310-9
pubmed:dateRevised
2007-11-14
pubmed:meshHeading
pubmed:year
2004
pubmed:articleTitle
The effect of delta G on the transport and oral absorption of macromolecules.
pubmed:affiliation
Pharmacokinetics-Biopharmaceutics Laboratory, Department of Pharmaceutical Sciences, School of Pharmacy, University of Maryland at Baltimore, 20 Penn Street, Baltimore, Maryland 21201, USA.
pubmed:publicationType
Journal Article, Comparative Study, Research Support, U.S. Gov't, P.H.S., Research Support, U.S. Gov't, Non-P.H.S.