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首页> 外文期刊>Biomaterials Science >Ultrafast charge-conversional nanocarrier for tumor-acidity-activated targeted drug elivery
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Ultrafast charge-conversional nanocarrier for tumor-acidity-activated targeted drug elivery

机译：超快电荷对话纳米载体用于肿瘤酸度激活的靶向药物递送

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摘要

Nanocarriers with tumor-acidity-activated charge-conversional ability are of particular interest for targeted drug delivery in the field of precision nanomedicine. Nevertheless, the key challenge of this strategy is the slowness of reversing the surface charge at the tumor tissue. As a proof-of-concept, we synthesized the amphiphilic triblock polymer poly(ethylene glycol)-block-poly(2-carboxyethylacrylate)-blockpoly( 2-azepaneethylmethacrylate) (PEG-b-PCEA-b-PAEMA) to prepare the cisplatin-loaded nanocarrier UCC-NP/Pt. The PAEMA block at the physiological pH values was hydrophobic, which formed the core of UCC-NP/Pt. In contrast, at the tumor acidity, the tertiary amine groups of PAEMA block rapidly protonated, resulting in the ultrafast charge conversion of UCC-NP/Pt within 10 s. Such ultrafast charge-conversional effect more efficiently enhanced tumor cell internalization of nanocarriers, thus achieving targeted drug delivery, which in turn exhibited superior anticancer efficacy even in the cisplatin-resistant cells. This approach provides new avenues for tumor-acidity-activated targeted drug delivery.
机译：纳米载体具有肿瘤酸性活化的电荷 - 交易能力对于精密纳米胺的靶向药物递送特别感兴趣。然而，这种策略的关键挑战是在肿瘤组织处逆转表面电荷的缓慢。作为概念验证，我们合成了两亲三嵌段聚合物聚（乙二醇） - Block-poly（2-羧乙基丙烯酸酯） - Blockpoly（2-亚己庚烷丙烯酸甲酯）（PEG-B-PCEA-B-PAEMA）制备顺铂 - 纳米载波UCC-NP / PT。生理pH值的PAEMA块是疏水的，形成UCC-NP / PT的核心。相反，在肿瘤酸度下，叔胺基团的PAEMA嵌段迅速质子化，导致10秒内UCC-NP / PT的超快电荷转化。这种超快电荷交易效果更有效地增强了纳米载体的肿瘤细胞内化，从而实现了靶向药物递送，即使在顺铂抗细胞中也甚至表现出优异的抗癌效果。这种方法为肿瘤酸度激活的靶向药物递送提供了新的途径。

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  • 来源
    《Biomaterials Science》 |2018年第2期|共6页
  • 作者

    Liu Jing; Iqbal Shoaib; Du Xiao-Jiao; Yuan Youyong; Yang Xianzhu; Li Hong-Jun; Wang Jun;

  • 作者单位

    Univ Sci &

    Technol China Sch Life Sci Hefei 230027 Anhui Peoples R China;

    Univ Sci &

    Technol China Sch Life Sci Hefei 230027 Anhui Peoples R China;

    South China Univ Technol Inst Life Sci Guangzhou 510006 Guangdong Peoples R China;

    South China Univ Technol Inst Life Sci Guangzhou 510006 Guangdong Peoples R China;

    South China Univ Technol Inst Life Sci Guangzhou 510006 Guangdong Peoples R China;

    South China Univ Technol Inst Life Sci Guangzhou 510006 Guangdong Peoples R China;

    Univ Sci &

    Technol China Sch Life Sci Hefei 230027 Anhui Peoples R China;

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  • 原文格式 PDF
  • 正文语种 eng
  • 中图分类 分子生物学;
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