Show simple item record

dc.contributor.authorZhao, Yunqi
dc.contributor.authorDuan, Shaofeng
dc.contributor.authorZeng, Xing
dc.contributor.authorLiu, Chunjing
dc.contributor.authorDavies, Neal M.
dc.contributor.authorLi, Benyi
dc.contributor.authorForrest, M. Laird
dc.date.accessioned2017-05-10T16:58:07Z
dc.date.available2017-05-10T16:58:07Z
dc.date.issued2012-06-04
dc.identifier.citationZhao, Y., Duan, S., Zeng, X., Liu, C., Davies, N. M., Li, B., & Forrest, M. L. (2012). Prodrug Strategy for PSMA-targeted Delivery of TGX-221 to Prostate Cancer Cells. Molecular Pharmaceutics, 9(6), 1705–1716. http://doi.org/10.1021/mp3000309en_US
dc.identifier.urihttp://hdl.handle.net/1808/24067
dc.description.abstractTGX-221 is a potent, selective, and cell membrane permeable inhibitor of the PI3K p110β catalytic subunit. Recent studies showed that TGX-221 has anti-proliferative activity against PTEN-deficient tumor cell lines including prostate cancers. The objective of this study was to develop an encapsulation system for parenterally delivering TGX-221 to the target tissue through a prostate-specific membrane aptamer (PSMAa10) with little or no side effects. In this study, PEG-PCL micelles were formulated to encapsulate the drug, and a prodrug strategy was pursued to improve the stability of the carrier system. Fluorescence imaging studies demonstrated that the cellular uptake of both drug and nanoparticles were significantly improved by targeted micelles in a PSMA positive cell line. The area under the plasma concentration time curve of the micelle formulation in nude mice was 2.27-fold greater than the naked drug, and the drug clearance rate was 17.5-fold slower. These findings suggest a novel formulation approach for improving site-specific drug delivery of a molecular-targeted prostate cancer treatment.en_US
dc.publisherAmerican Chemical Societyen_US
dc.rightsThis document is the Accepted Manuscript version of a Published Work that appeared in final form in Molecular Pharmaceutics, copyright © American Chemical Society after peer review and technical editing by the publisher. To access the final edited and published work see http://doi.org/10.1021/mp3000309.en_US
dc.subjectPEG-PCL micelleen_US
dc.subjectTGX-221en_US
dc.subjectPSMAen_US
dc.subjectTarget deliveryen_US
dc.titleProdrug Strategy for PSMA-targeted Delivery of TGX-221 to Prostate Cancer Cellsen_US
dc.typeArticleen_US
kusw.kuauthorZhao, Yunqi
kusw.kuauthorDuan, Shaofeng
kusw.kuauthorLiu, Chunjing
kusw.kuauthorForrest, M. Laird
kusw.kudepartmentPharmaceutical Chemistryen_US
kusw.kudepartmentHiguchi Biosciences Centeren_US
dc.identifier.doi10.1021/mp3000309en_US
kusw.oaversionScholarly/refereed, author accepted manuscripten_US
kusw.oapolicyThis item does not meet KU Open Access policy criteria.en_US
dc.identifier.pmidPMC3601665en_US
dc.rights.accessrightsopenAccess


Files in this item

Thumbnail

This item appears in the following Collection(s)

Show simple item record