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Teniposide-loaded multilayer modified albumin nanoparticles with increased passive delivery to the lung

机译：替替碘化物加载的多层改性白蛋白纳米颗粒，随着肺部的被动递送增加

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摘要

The nature of a particle surface has a tremendous influence on the in vitro and in vivo behavior of the particle, in addition to the particle size. In this study, multilayer modified albumin nanoparticles were developed to encapsulate teniposide, an anti-cancer agent used in the treatment of lung cancer, in order to optimize its distribution and pharmacokinetics. Multilayer nanoparticles were prepared by coating albumin particles with chitosan and subsequently with PLG-PEG. The multilayer structure was confirmed by the increase in particle size, reverse potential, surface components and morphology, suggesting a layer by layer coating mechanism, involving electrostatic interaction. According to the results of the in vitro release and cytotoxicity studies, the multilayer particles were slightly pH-sensitive to an acidic environment. More importantly, compared with the commercial injection, the modified particles showed a preference for distribution in the lung and exhibited far lower concentrations in the heart and kidney and a prolonged circulation in plasma after intravenous injection, whereas the naked albumin nanoparticles mainly accumulated in the liver and spleen. In addition, P-CS-NP with a reduced amount of PLG-PEG transiently and extensively accumulated in the lung but then rapidly migrated to the liver or spleen, suggesting that the amount of coated layer on the particles affected the targeting behavior and retention in the lung. Therefore, the structure of the albumin core and multi-coated layers are a very promising way for achieving controlled release and passively targeted delivery to the lung.
机译：除了粒径之外，颗粒表面的性质对颗粒的体外和体内行为具有巨大的影响。在该研究中，开发了多层改性白蛋白纳米颗粒以包封邻碘氮，一种用于治疗肺癌的抗癌剂，以优化其分布和药代动力学。通过用壳聚糖涂覆白蛋白颗粒并随后用PLG-PEG来制备多层纳米颗粒。通过粒度，反向电位，表面分量和形态的增加来证实多层结构，涉及静电相互作用的层涂覆机构的层。根据体外释放和细胞毒性研究的结果，多层颗粒对酸性环境略微pH敏感。更重要的是，与商业注射相比，改性颗粒始置良好的肺部分布，并在静脉注射后血浆中的血浆延长浓度以及血浆中的延长循环，而裸蛋白纳米颗粒主要积聚在肝脏中和脾脏。另外，P-CS-NP瞬时且广泛积聚在肺中的PLG-PEG量，但随后迅速迁移到肝脏或脾脏，表明颗粒上的涂层量影响了靶向行为和保留肺。因此，白蛋白核心和多涂层层的结构是实现控制释放和被动靶向递送至肺的非常有希望的方式。

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  • 来源
    《RSC Advances》 |2016年第84期|共10页
  • 作者

    Guo Haiyan; Fei Siyang; Zhang Yan; Zhang Yu; Gou Jingxin; Zhang Ling; He Haibing; Yin Tian; Wang Yanjiao; Tang Xing;

  • 作者单位

    Shenyang Pharmaceut Univ Coll Pharm Dept Pharmaceut Shenyang 110016 Liaoning Peoples R China;

    Shenyang Pharmaceut Univ Coll Pharm Dept Pharmaceut Shenyang 110016 Liaoning Peoples R China;

    Shenyang Univ Normal Coll Shenyang 110044 Peoples R China;

    Shenyang Pharmaceut Univ Coll Pharm Dept Pharmaceut Shenyang 110016 Liaoning Peoples R China;

    Shenyang Pharmaceut Univ Coll Pharm Dept Pharmaceut Shenyang 110016 Liaoning Peoples R China;

    Shenyang Pharmaceut Univ Coll Pharm Dept Pharmaceut Shenyang 110016 Liaoning Peoples R China;

    Shenyang Pharmaceut Univ Coll Pharm Dept Pharmaceut Shenyang 110016 Liaoning Peoples R China;

    Shenyang Pharmaceut Univ Sch Funct Food &

    Wine Shenyang 110016 Liaoning Peoples R China;

    Shenyang Pharmaceut Univ Coll Pharm Dept Pharmaceut Shenyang 110016 Liaoning Peoples R China;

    Shenyang Pharmaceut Univ Coll Pharm Dept Pharmaceut Shenyang 110016 Liaoning Peoples R China;

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  • 正文语种 eng
  • 中图分类 化学;
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