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首页> 外文期刊>Journal of Materials Science >Phenylboronic acid-functionalized ultra-pH-sensitive micelles for enhanced tumor penetration and inhibition in vitro
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Phenylboronic acid-functionalized ultra-pH-sensitive micelles for enhanced tumor penetration and inhibition in vitro

机译：苯基硼酸官能化超pH敏感胶束，用于增强肿瘤渗透和体外抑制作用

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摘要

In this work, the tumor-targeted ultra-pH-responsive conjugates (PBA/Dex-g-OE) and nontargeted conjugates (Dex-g-OE) were successfully prepared and could easily self-assemble into stable micelles with lower CMC values in neutral aqueous solution. Transmission electron microscopy and dynamic light scattering measurement indicated that the resulting micelles have desirable size distribution and regular spherical shape. The PBA/Dex-g-OE micelles possessed high stability in physiological condition and were pH sensitive to both extracellular and intracellular acidic conditions. Doxorubicin (DOX) was efficiently loaded to give the DOX-loaded micelles (PBA/Dex-g-OE-DOX and Dex-g-OE-DOX) with the desirable drug loading contents. In vitro cellular uptake and growth inhibition assays suggested that PBA/Dex-g-OE-DOX micelles were more efficiently internalized by monolayer tumor cells and three-dimensional multicellular tumor spheroids (MCTS) than nontargeted micelles (Dex-g-OE-DOX), leading to the fast and complete destruction of MCTS in vitro.
机译：在这项工作中，成功制备了肿瘤靶向的超pH响应偶联（PBA / DEX-G-OE）和不靶向缀合物（DEX-G-OE），并且可以容易地将稳定的胶束自组装成具有较低的CMC值中性水溶液。透射电子显微镜和动态光散射测量表明所得胶束具有所需的尺寸分布和规则的球形。 PBA / DEX-G-OE胶束在生理病症中具有高稳定性，并且对细胞外和细胞内酸性条件的pH值敏感。有效地装载了多柔比星（DOX）以使DOX加载的胶束（PBA / DEX-G-OE-DOX和DEX-G-OE-DOX）与所需的药物负载含量。体外细胞摄取和生长抑制测定表明，通过单层肿瘤细胞和三维多细胞肿瘤球状体（MCT）比不靶向胶束更有效地内化PBA / DEX-G-OE-DOX胶束（DEX-G-OE-DOX） ，导致体外快速完全地破坏MCT。

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  • 来源
    《Journal of Materials Science》 |2019年第7期|共17页
  • 作者

    Qin Jiejie; Huang Yan; Yan Guoqing; Wang Jun; Hu Liefeng; Zhang Panpan; Tang Rupei;

  • 作者单位

    Anhui Univ Anhui Key Lab Modern Biomfg Engn Res Ctr Biomed Mat Sch Life Sci 111 Jiulong Rd Hefei 230601 Anhui Peoples R China;

    Anhui Univ Anhui Key Lab Modern Biomfg Engn Res Ctr Biomed Mat Sch Life Sci 111 Jiulong Rd Hefei 230601 Anhui Peoples R China;

    Anhui Univ Anhui Key Lab Modern Biomfg Engn Res Ctr Biomed Mat Sch Life Sci 111 Jiulong Rd Hefei 230601 Anhui Peoples R China;

    Anhui Univ Anhui Key Lab Modern Biomfg Engn Res Ctr Biomed Mat Sch Life Sci 111 Jiulong Rd Hefei 230601 Anhui Peoples R China;

    Anhui Univ Anhui Key Lab Modern Biomfg Engn Res Ctr Biomed Mat Sch Life Sci 111 Jiulong Rd Hefei 230601 Anhui Peoples R China;

    Anhui Univ Anhui Key Lab Modern Biomfg Engn Res Ctr Biomed Mat Sch Life Sci 111 Jiulong Rd Hefei 230601 Anhui Peoples R China;

    Anhui Univ Anhui Key Lab Modern Biomfg Engn Res Ctr Biomed Mat Sch Life Sci 111 Jiulong Rd Hefei 230601 Anhui Peoples R China;

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  • 正文语种 eng
  • 中图分类 工程材料学;
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