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dc.contributor.authorLalatsa, Aikaterini
dc.contributor.authorLee, Vivian
dc.contributor.authorMalkinson, John P.
dc.contributor.authorZloh, Mire
dc.contributor.authorSchätzlein, Andreas G
dc.contributor.authorUchegbu, Ijeoma F.
dc.date.accessioned2013-01-11T13:59:08Z
dc.date.available2013-01-11T13:59:08Z
dc.date.issued2012-06
dc.identifier.citationLalatsa , A , Lee , V , Malkinson , J P , Zloh , M , Schätzlein , A G & Uchegbu , I F 2012 , ' A prodrug nanoparticle approach for the oral delivery of a hydrophilic peptide, leucine(5)-enkephalin, to the brain ' , Molecular Pharmaceutics , vol. 9 , no. 6 , pp. 1665-1680 . https://doi.org/10.1021/mp300009u
dc.identifier.issn1543-8384
dc.identifier.otherPURE: 1268116
dc.identifier.otherPURE UUID: 3f5ef5d8-0b72-48c4-9aa8-f27eb51cbfe3
dc.identifier.otherWOS: 000304728700014
dc.identifier.otherPubMed: 22574705
dc.identifier.otherScopus: 84862015361
dc.identifier.urihttp://hdl.handle.net/2299/9581
dc.description.abstractThe oral use of neuropeptides to treat brain disease is currently not possible because of a combination of poor oral absorption, short plasma half-lives and the blood-brain barrier. Here we demonstrate a strategy for neuropeptide brain delivery via the (a) oral and (b) intravenous routes. The strategy is exemplified by a palmitic ester prodrug of the model drug leucine(5)-enkephalin, encapsulated within chitosan amphiphile nanoparticles. Via the oral route the nanoparticle-prodrug formulation increased the brain drug levels by 67% and significantly increased leucine(5)-enkephalin's antinociceptive activity. The nanoparticles facilitate oral absorption and the prodrug prevents plasma degradation, enabling brain delivery. Via the intravenous route, the nanoparticle-prodrug increases the peptide brain levels by 50% and confers antinociceptive activity on leucine(5)-enkephalin. The nanoparticle-prodrug enables brain delivery by stabilizing the peptide in the plasma although the chitosan amphiphile particles are not transported across the blood-brain barrier per se, and are excreted in the urine.en
dc.format.extent16
dc.language.isoeng
dc.relation.ispartofMolecular Pharmaceutics
dc.subjectblood-brain barrier
dc.subjectpeptide
dc.subjectoral delivery
dc.subjectnanoparticles
dc.subjectLeucine-enkephalin
dc.subjectOpioid
dc.titleA prodrug nanoparticle approach for the oral delivery of a hydrophilic peptide, leucine(5)-enkephalin, to the brainen
dc.contributor.institutionDepartment of Pharmacy
dc.contributor.institutionSchool of Life and Medical Sciences
dc.contributor.institutionHealth & Human Sciences Research Institute
dc.contributor.institutionCentre for Research into Topical Drug Delivery and Toxicology
dc.contributor.institutionNanopharmaceutics
dc.contributor.institutionPharmaceutics
dc.contributor.institutionMedicinal and Analytical Chemistry
dc.description.statusPeer reviewed
dc.relation.schoolSchool of Life and Medical Sciences
dcterms.dateAccepted2012-06
rioxxterms.versionVoR
rioxxterms.versionofrecordhttps://doi.org/10.1021/mp300009u
rioxxterms.typeJournal Article/Review
herts.preservation.rarelyaccessedtrue


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