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dc.contributor.authorCheng, W P
dc.contributor.authorGray, A I
dc.contributor.authorTetley, L
dc.contributor.authorHang, T L B
dc.contributor.authorSchatzlein, A G
dc.contributor.authorUchegbu, I F
dc.date.accessioned2012-01-03T12:01:06Z
dc.date.available2012-01-03T12:01:06Z
dc.date.issued2006-05
dc.identifier.citationCheng , W P , Gray , A I , Tetley , L , Hang , T L B , Schatzlein , A G & Uchegbu , I F 2006 , ' Polyelectrolyte nanoparticles with high drug loading enhance the oral uptake of hydrophobic compounds ' , Biomacromolecules , vol. 7 , no. 5 , pp. 1509-1520 . https://doi.org/10.1021/bm060130l
dc.identifier.issn1525-7797
dc.identifier.otherPURE: 383155
dc.identifier.otherPURE UUID: 239c7587-19d0-4c3c-9141-003e6c337a76
dc.identifier.otherWOS: 000237593600018
dc.identifier.otherScopus: 33744552970
dc.identifier.urihttp://hdl.handle.net/2299/7532
dc.description.abstractIn the pharmaceutical industry, orally active compounds are required to have sufficient water solubility to enable dissolution within the gastrointestinal tract prior to absorption. Limited dissolution within the gastrointestinal tract often reduces the bioavailability of hydrophobic drugs. To improve gastrointestinal tract dissolution, nonaqueous solvents are often used in the form of emulsions and microemulsions. Here, we show that oil-free polyelectrolyte nanosystems (micellar dispersions and 100 - 300 nm particles) prepared from poly(ethylenimines) derivatized with cetyl chains and quaternary ammonium groups are able to encapsulate high levels of hydrophobic drug (0.20 g of drug per g of polymer) for over 9 months, as demonstrated using cyclosporine A (log P = 4.3). The polyelectrolytes facilitate the absorption of hydrophobic drugs within the gastrointestinal tract by promoting drug dissolution and by a hypothesized mechanism involving paracellular drug transport. Polyelectrolyte nanoparticle drug blood levels are similar to those obtained with commercial microemulsion formulations. The polyelectrolytes do not promote absorption by inhibition of the P-glycoprotein efflux pump.en
dc.format.extent12
dc.language.isoeng
dc.relation.ispartofBiomacromolecules
dc.subjectCYCLOSPORINE-A
dc.subjectCACO-2 CELLS
dc.subjectTRANSEPITHELIAL PERMEABILITY
dc.subjectNONIONIC SURFACTANTS
dc.subjectP-GLYCOPROTEIN
dc.subjectMICELLES
dc.subjectABSORPTION
dc.subjectCOPOLYMERS
dc.subjectCYTOCHROME-P450
dc.subjectSOLUBILIZATION
dc.titlePolyelectrolyte nanoparticles with high drug loading enhance the oral uptake of hydrophobic compoundsen
dc.contributor.institutionDepartment of Pharmacy
dc.contributor.institutionHealth & Human Sciences Research Institute
dc.description.statusPeer reviewed
dcterms.dateAccepted2006-05
rioxxterms.versionofrecordhttps://doi.org/10.1021/bm060130l
rioxxterms.typeJournal Article/Review
herts.preservation.rarelyaccessedtrue


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