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首页> 外文期刊>Advanced Functional Materials >Tumor-Responsive Small Molecule Self-Assembled Nanosystem for Simultaneous Fluorescence Imaging and Chemotherapy of Lung Cancer
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Tumor-Responsive Small Molecule Self-Assembled Nanosystem for Simultaneous Fluorescence Imaging and Chemotherapy of Lung Cancer

机译：肿瘤反应性小分子自组装纳米系统，用于肺癌的同时荧光成像和化学疗法

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摘要

Cancer therapeutic drugs face various transportation barriers in transit to the tumor site, making the delivery of effective drug concentrations problematic. Moreover, these drugs are very difficult to use due to their adverse off-target effects. Thus, it is very essential to develop a drug delivery system that can deliver drugs to achieve effective local concentrations without side effects on healthy tissues. Herein, the authors report a self-assembled nanodrug system in which hydrophobic antitumor drugs are packaged into nanoparticles to improve water solubility, tumor targeting ability, blood retention time, and chemotherapeutic effect. The nanodrugs are degraded into smaller ones when exposed to the tumor microenvironment, extravasated from leaky regions of the tumor vasculature, and displayed matrix metalloproteinase-2 (MMP-2)-induced degradation and antitumor property. To construct this unique system, an amphiphilic multifunctional molecule (Pep-Cy5) is synthesized by attaching a MMP-2-cleavable peptide to a hydrophobic near-infrared dye, Cy5. Two hydrophobic anticancer drugs are conjugated to Pep-Cy5 through hydrophobic interactions to form the self-assembled nanodrug system. The MMP-2-induced degradation and hydrophobic antitumor drug interchangeability features of this nanosystem enable the hydrophobic antitumor drugs to exhibit longer blood-retention times, improved intratumoral accumulation, fewer side effects, and higher anticancer efficacies compared with free drugs.
机译：癌症治疗药物在转运至肿瘤部位时面临各种运输障碍，从而使有效药物浓度的输送成为问题。此外，由于它们的不良脱靶作用，这些药物非常难以使用。因此，开发一种能够递送药物以达到有效的局部浓度而又不对健康组织产生副作用的药物递送系统非常重要。在此，作者报告了一种自组装的纳米药物系统，其中将疏水性抗肿瘤药物包装到纳米颗粒中，以改善水溶性，肿瘤靶向能力，血液保留时间和化学治疗效果。当暴露于肿瘤微环境时，纳米药物被降解成较小的纳米药物，从肿瘤脉管系统的渗漏区域渗出，并表现出基质金属蛋白酶2（MMP-2）诱导的降解和抗肿瘤特性。为了构建这个独特的系统，通过将MMP-2可裂解的肽连接到疏水性近红外染料Cy5上来合成两亲性多功能分子（Pep-Cy5）。两种疏水性抗癌药物通过疏水性相互作用与Pep-Cy5结合，形成自组装的纳米药物系统。与游离药物相比，该纳米系统的MMP-2诱导的降解和疏水性抗肿瘤药物可互换性特性使疏水性抗肿瘤药物显示出更长的血液保留时间，改善的肿瘤内累积，更少的副作用以及更高的抗癌效力。

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  • 来源
    《Advanced Functional Materials》 |2016年第47期|8735-8745|共11页
  • 作者

    Yang Yuming; Yue Caixia; Han Yu; Zhang Wei; He Aina; Zhang Chunlei; Yin Ting; Zhang Qian; Zhang Jingjing; Yang Yao; Ni Jian; Sun Jielin; Cui Daxiang;

  • 作者单位

    Shanghai Jiao Tong Univ, Inst Nano Biomed & Engn, Shanghai Engn Res Ctr Intelligent Diag & Treatmen, Dept Instrument Sci & Engn,Sch Elect Informat & E, 800 Dongchuan Rd, Shanghai 200240, Peoples R China;

    Shanghai Jiao Tong Univ, Inst Nano Biomed & Engn, Shanghai Engn Res Ctr Intelligent Diag & Treatmen, Dept Instrument Sci & Engn,Sch Elect Informat & E, 800 Dongchuan Rd, Shanghai 200240, Peoples R China;

    Shanghai Jiao Tong Univ, Inst Nano Biomed & Engn, Shanghai Engn Res Ctr Intelligent Diag & Treatmen, Dept Instrument Sci & Engn,Sch Elect Informat & E, 800 Dongchuan Rd, Shanghai 200240, Peoples R China;

    Shanghai Jiao Tong Univ, Affiliated Peoples Hosp 6, Dept Orthoped, 600 Yishan Rd, Shanghai 200233, Peoples R China;

    Shanghai Jiao Tong Univ, Affiliated Peoples Hosp 6, Dept Oncol, 600 Yishan Rd, Shanghai 200233, Peoples R China;

    Shanghai Jiao Tong Univ, Inst Nano Biomed & Engn, Shanghai Engn Res Ctr Intelligent Diag & Treatmen, Dept Instrument Sci & Engn,Sch Elect Informat & E, 800 Dongchuan Rd, Shanghai 200240, Peoples R China;

    Shanghai Jiao Tong Univ, Inst Nano Biomed & Engn, Shanghai Engn Res Ctr Intelligent Diag & Treatmen, Dept Instrument Sci & Engn,Sch Elect Informat & E, 800 Dongchuan Rd, Shanghai 200240, Peoples R China|Shanghai Jiao Tong Univ, Affiliated Peoples Hosp 6, Dept Oncol, 600 Yishan Rd, Shanghai 200233, Peoples R China;

    Shanghai Jiao Tong Univ, Inst Nano Biomed & Engn, Shanghai Engn Res Ctr Intelligent Diag & Treatmen, Dept Instrument Sci & Engn,Sch Elect Informat & E, 800 Dongchuan Rd, Shanghai 200240, Peoples R China|Shanghai Jiao Tong Univ, Collaborat Innovat Ctr Syst Biol, Natl Ctr Translat Med, 800 Dongchuan Rd, Shanghai 200240, Peoples R China;

    Shanghai Jiao Tong Univ, Inst Nano Biomed & Engn, Shanghai Engn Res Ctr Intelligent Diag & Treatmen, Dept Instrument Sci & Engn,Sch Elect Informat & E, 800 Dongchuan Rd, Shanghai 200240, Peoples R China;

    Shanghai Jiao Tong Univ, Inst Nano Biomed & Engn, Shanghai Engn Res Ctr Intelligent Diag & Treatmen, Dept Instrument Sci & Engn,Sch Elect Informat & E, 800 Dongchuan Rd, Shanghai 200240, Peoples R China;

    Shanghai Jiao Tong Univ, Inst Nano Biomed & Engn, Shanghai Engn Res Ctr Intelligent Diag & Treatmen, Dept Instrument Sci & Engn,Sch Elect Informat & E, 800 Dongchuan Rd, Shanghai 200240, Peoples R China|Shanghai Jiao Tong Univ, Collaborat Innovat Ctr Syst Biol, Natl Ctr Translat Med, 800 Dongchuan Rd, Shanghai 200240, Peoples R China;

    Shanghai Jiao Tong Univ, Collaborat Innovat Ctr Syst Biol, Natl Ctr Translat Med, 800 Dongchuan Rd, Shanghai 200240, Peoples R China;

    Shanghai Jiao Tong Univ, Inst Nano Biomed & Engn, Shanghai Engn Res Ctr Intelligent Diag & Treatmen, Dept Instrument Sci & Engn,Sch Elect Informat & E, 800 Dongchuan Rd, Shanghai 200240, Peoples R China|Shanghai Jiao Tong Univ, Collaborat Innovat Ctr Syst Biol, Natl Ctr Translat Med, 800 Dongchuan Rd, Shanghai 200240, Peoples R China;

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