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    Prodrug Strategy for PSMA-targeted Delivery of TGX-221 to Prostate Cancer Cells

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    Zhao_2012.pdf (911.2Kb)
    Issue Date
    2012-06-04
    Author
    Zhao, Yunqi
    Duan, Shaofeng
    Zeng, Xing
    Liu, Chunjing
    Davies, Neal M.
    Li, Benyi
    Forrest, M. Laird
    Publisher
    American Chemical Society
    Type
    Article
    Article Version
    Scholarly/refereed, author accepted manuscript
    Rights
    This 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.
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    Abstract
    TGX-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.
    URI
    http://hdl.handle.net/1808/24067
    DOI
    https://doi.org/10.1021/mp3000309
    Collections
    • Pharmaceutical Chemistry Scholarly Works [252]
    Citation
    Zhao, 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/mp3000309

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    Contact KU ScholarWorks
    785-864-8983
    KU Libraries
    1425 Jayhawk Blvd
    Lawrence, KS 66045
    785-864-8983

    KU Libraries
    1425 Jayhawk Blvd
    Lawrence, KS 66045
    Image Credits
     

     

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