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dc.contributor.authorWong, Allan K.
dc.contributor.authorRoss, Benjamin P.
dc.contributor.authorChan, Yiu-Ngok
dc.contributor.authorArtursson, Per
dc.contributor.authorLazorova, Lucia
dc.contributor.authorJones, Alun
dc.contributor.authorToth, Istvan
dc.date.accessioned2006-07-22
dc.date.accessioned2017-03-02T00:29:45Z
dc.date.available2015-05-25T05:41:52Z
dc.date.available2017-03-02T00:29:45Z
dc.date.issued2002
dc.identifier.issn0928-0987
dc.identifier.doi10.1016/S0928-0987(02)00078-7
dc.identifier.urihttp://hdl.handle.net/10072/67386
dc.description.abstractPURPOSE: To synthesize a number of analogues of Leu-enkephalin with different lipophilicities and to develop an LC-MS method for determining the Caco-2 cell permeability values of these compounds. METHODS: A number of sugar and sugar plus lipoamino acid analogues of Leu-enkephalin were synthesized by solid-phase and solution methods. An LC-MS method was developed for analyzing the Caco-2 cell assay samples and validated against the traditional method using radiolabelled compounds. RESULTS: A sensitive and specific LC-MS assay was developed. Standard curves were linear in the range of 0.025-5 microM. Apparent permeability values determined by LC-MS and liquid scintillation counter were identical, for both a hydrophilic drug, cephalexin and a lipophilic Leu-enkaphalin analogue. Caco-2 permeability values for the analogues of Leu-enkephalin were determined and it was found that attachment of sugar or sugar and lipoamino acid to the Leu-enkephalin peptide resulted in an increase in the apparent permeability values compared to the native peptide, which was not transported across the Caco-2 cell monolayers. CONCLUSIONS: A rapid, generic LC-MS method for analyzing a range of compounds was developed. Attachment of a sugar or sugar and lipoamino acid to Leu-enkephalin improves the apparent permeability across Caco-2 cell monolayers.
dc.description.peerreviewedYes
dc.description.publicationstatusYes
dc.languageEnglish
dc.language.isoeng
dc.publisherElsevier Science
dc.publisher.placeAmsterdam
dc.relation.ispartofpagefrom113
dc.relation.ispartofpageto118
dc.relation.ispartofissue3
dc.relation.ispartofjournalEuropean Journal of Pharmaceutical Sciences
dc.relation.ispartofvolume16
dc.subject.fieldofresearchPharmacology and Pharmaceutical Sciences
dc.subject.fieldofresearchcode1115
dc.titleDetermination of transport in the Caco-2 cell assay of compounds varying in lipophilicity using LC-MS: enhanced transport of Leu-enkephalin analogues.
dc.typeJournal article
dc.type.descriptionC1 - Articles
dc.type.codec1x
gro.facultyGriffith Health Faculty
gro.date.issued2015-05-25T05:41:52Z
gro.hasfulltextNo Full Text
gro.griffith.authorChan, Yiu-Ngok


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