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    Cathepsin B-sensitive and biocompatible dendritic polyHPMA-gemcitabine prodrug-based nanoscale system markedly enhances the antitumor activity

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    Authors
    Dai, Yan
    Ma, Xuelei
    Zhang, Yanhong
    Chen, Kai
    Tang, James Zhenggui
    Gong, Qiyong
    Luo, Kui
    Issue Date
    2018-09
    
    Metadata
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    Abstract
    To improve therapeutic indexes of gemcitabine (GEM), a stimuli-responsive dendritic polyHPMA copolymer conjugated with gemcitabine (Dendritic polyHPMA-GEM) prodrug was designed and synthesized via one-pot synthesis of RAFT polymerization. The prodrug with dendritic architectures is able to aggregate and form stable nanoscale system with a size of 46 nm. The dendritic prodrug with high molecular weight (HMW) of 168 kDa can biodegrade to low molecular weight (LMW, 29 kDa) segments for excretion. The prodrug demonstrates enzyme-responsive drug release features, and over 95% GEM was released from the carrier with the Cathepsin B within 3 h. The cellular mechanism of the dendritic prodrug was studied, suggesting the cytotoxicity is associated with the cell uptake and cell apoptosis. The prodrug shows good hemocompatibility and in vivo biosafety. Of interest, the dendritic polymer prodrug displays high accumulation within tumors, and markedly improves the in vivo antitumor activity against 4T1 murine breast cancer model compared to the free GEM. These in vivo antitumor activities are characterized as with markedly suppressed tumor volumes, indicating as the much higher tumor growth inhibition (TGI 83%) than that in GEM treatment (TGI, 36%), moreover some tumors are eliminated. The tumor xenograft immunohistochemistry study clearly indicates that the tumor apoptosis is through antiangiogenic effects. These results suggest that the stimuli-responsive dendritic polymer-gemcitabine has great potential as an efficient anticancer agent
    Citation
    Dai, Y., Ma, X., Zhang, Y., Chen, K., Tang, JZ., Luo, K. (2018) 'Cathepsin B-Sensitive and Biocompatible Dendritic polyHPMA-Gemcitabine Prodrug-Based Nanoscale System Markedly Enhances the Antitumor Activity', Biomaterials Science, 6 (11) doi: 10.1039/C8BM00946E
    Publisher
    The Royal Society of Chemistry
    Journal
    Biomaterials Science
    URI
    http://hdl.handle.net/2436/621819
    DOI
    10.1039/C8BM00946E
    Additional Links
    https://pubs.rsc.org/en/content/articlelanding/2018/bm/c8bm00946e#!divAbstract
    Type
    Journal article
    Language
    en
    ISSN
    2047-4830
    ae974a485f413a2113503eed53cd6c53
    10.1039/C8BM00946E
    Scopus Count
    Collections
    Faculty of Science and Engineering

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