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Optimized synthesis of glycyrrhetinic acid-modified chitosan 5-fluorouracil nanoparticles and their characteristics

  • 作者:
  • 地址:

    [1]Pudong New Area Dist Zhoupu Hosp, Dept Gen Surg, Shanghai, Peoples R China.

    [2]Pudong New Area Dist Zhoupu Hosp, Dept Endoscopy, Shanghai, Peoples R China.

    [3]Zhejiang Huafon Spandex Co Ltd, Zhejiang Huafon Fiber Res Inst, Wenzhou, Peoples R China.

    [4]Wuhan Univ Technol, Sch Mat Sci & Engn, Wuhan 430070, Peoples R China.

    [5]Fudan Univ, Dept Gen Surg, Shanghai Peoples Hosp 5, Shanghai 200433, Peoples R China.

  • 语种:
    英文
  • 期刊:
    INTERNATIONAL JOURNAL OF NANOMEDICINE ISSN:1178-2013 2014 年 9 卷 (695 - 710) ; 2014
  • 文献号:
    296FV
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  • 关键词:
  • 摘要:

    The nanoparticle drug delivery system, which uses natural or synthetic polymeric material as a carrier to deliver drugs to targeted tissues, has a broad prospect for clinical application for its targeting, slow-release, and biodegradable properties. Here, we used chitosan (CTS) and hepatoma cell-specific binding molecule glycyrrhetinic acid to synthesize glycyrrhetinic acid-modified chitosan (GA-CTS). The synthetic product was confirmed by infrared (IR) spectra and hydrogen-1 nuclear magnetic resonance. The GA-CTS/5-fluorouracil (5-FU) nanoparticles were synthesized by combining GA-CTS and 5-FU and conjugating 5-FU onto the GA-CTS nanomaterial. The central composite design was performed to optimize the preparation process as CTS:tripolyphosphate sodium (TPP) weight ratio =5:1, 5-FU:CTS weight ratio =1:1, TPP concentration =0.05% (w/v), and cross-link time =50 minutes. GA-CTS/5-FU nanoparticles had a mean particle size of 193.7 nm, a polydispersity index of 0.003, a zeta potential of +27.4 mV, and a drug loading of 1.56%. The GA-CTS/5-FU nanoparticle had a protective effect on the drug against plasma degrading enzyme, and provided a sustained release system comprising three distinct phases of quick, steady, and slow release. Our study showed that the peak time, half-life time, mean residence time and area under the curve of GA-CTS/5-FU were longer or more than those of the 5-FU group, but the maximum concentration (C-max) was lower. We demonstrated that the nanoparticles accumulated in the liver and have significantly inhibited tumor growth in an orthotropic liver cancer mouse model.

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  • 基金信息:
    Natural Science Foundation of Shanghai [12nm0502202, 114119a4700]; Pudong New Area Science and Technology Development Fund [PKJ2012-Y24]; Pudong New Area Health System discipline lead development program [PWRd2013-10]
  • 推荐引用方式
    GB/T 7714:
    Cheng Mingrong,Chen Houxiang,Wang Yong, et al. Optimized synthesis of glycyrrhetinic acid-modified chitosan 5-fluorouracil nanoparticles and their characteristics [J].INTERNATIONAL JOURNAL OF NANOMEDICINE,2014,9:695-710.
  • APA:
    Cheng Mingrong,Chen Houxiang,Wang Yong,Xu Hongzhi,&Zhang Zhiping.(2014).Optimized synthesis of glycyrrhetinic acid-modified chitosan 5-fluorouracil nanoparticles and their characteristics .INTERNATIONAL JOURNAL OF NANOMEDICINE,9:695-710.
  • MLA:
    Cheng Mingrong, et al. "Optimized synthesis of glycyrrhetinic acid-modified chitosan 5-fluorouracil nanoparticles and their characteristics" .INTERNATIONAL JOURNAL OF NANOMEDICINE 9(2014):695-710.
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