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Facile construction of dual-targeting delivery system by using lipid capped polymer nanoparticles for anti-glioma therapy

机译：使用脂质封端的聚合物纳米粒子进行双靶向递送系统进行抗胶瘤治疗的舒适构造

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摘要

Recent progress has suggested that dual targeting drug delivery systems, which are functionalized with two active ligands targeting the blood brain barrier (BBB) and brain tumor cells respectively, provide a promising strategy to improve the chemotherapeutic efficacy for gliomas. The key to successfully developing such systems is to functionalize nanoparticles (NPs) with active ligands, though they usually suffer from several issues such as NP aggregation, drug leakage and complicated chemical synthesis. Herein we report a facile way of constructing a dual targeting delivery system by simply using lipid capped polymer NPs. The NPs were constructed with a poly lactic-co-glycolic acid (PLGA) core for hydrophobic doxorubicin (DOX) loading, and a lipid (lecithin and DSPE-PEG(2000)-COOH) shell. The DSPE-PEG(2000)-COOH provides an excellent anchor for ligand conjugation. As a proof of concept, two active ligands of angiopep-2 peptide and AS1411 aptamer were covalently linked to NPs through a single step synthesis, with little effect on particle size, stability, drug loading and drug release performance. The accumulative drug release of the NPs in PBS (pH 7.4) over 144 h is similar to 50%, suggesting a sustained drug release profile. The NPs showed significantly enhanced uptake by brain capillary endothelial cells (BCECs) and C6 glioma cells as indicated by fluorescence microscopy and quantitative flow cytometry, demonstrating the dual targeting efficiency. The BBB penetration ability is validated by using an in vitro BBB model, and the in vitro cell inhibition study showed increased cytotoxicity of the NPs to glioma cells.
机译：最近的进展表明，双靶向药物递送系统分别用两个活性配体官能化，其分别用靶向血脑屏障（BBB）和脑肿瘤细胞，提供了提高胶质瘤的化学治疗效果的有希望的策略。成功开发这种系统的关键是用活性配体挥发纳米颗粒（NPS），尽管它们通常遭受若干问题，例如NP聚集，药物泄漏和复杂的化学合成。在此，我们通过简单地使用脂质封端的聚合物NP来报告一种构建双靶向递送系统的容易方式。用用于疏水性多柔比星（DOX）负载的聚乳酸 - 共乙醇酸（PLGA）核和脂质（卵磷脂和DSPE-PEG（2000）-COOH）壳构建NPS。 DSPE-PEG（2000）-COOH提供用于配体缀合的优异锚。作为概念证据，通过单步合成与NPS共价连接血管素-2肽和As1411 Aptamer的两种活性配体，对粒度，稳定性，药物负载和药物释放性能几乎没有影响。在144小时内，PBS（pH7.4）中NP的累积药物释放类似于50％，表明持续的药物释放曲线。 NPS显示脑毛细管内皮细胞（BCEC）和C6胶质瘤细胞的显着增强，如荧光显微镜和定量流式细胞仪所示，展示了双靶向效率。通过使用体外BBB模型验证BBB渗透能力，体外细胞抑制研究显示NPS对胶质瘤细胞的细胞毒性增加。

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  • 来源
    《RSC Advances》 |2018年第1期|共10页
  • 作者

    Wang Shengfeng; Zhao Chuantong; Liu Peng; Wang Zhe; Ding Jinsong; Zhou Wenhu;

  • 作者单位

    Cent S Univ Xiangya Sch Pharmaceut Sci Changsha 410013 Hunan Peoples R China;

    Cent S Univ Xiangya Sch Pharmaceut Sci Changsha 410013 Hunan Peoples R China;

    Cent S Univ Xiangya Sch Pharmaceut Sci Changsha 410013 Hunan Peoples R China;

    Cent S Univ Xiangya Sch Pharmaceut Sci Changsha 410013 Hunan Peoples R China;

    Cent S Univ Xiangya Sch Pharmaceut Sci Changsha 410013 Hunan Peoples R China;

    Cent S Univ Xiangya Sch Pharmaceut Sci Changsha 410013 Hunan Peoples R China;

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  • 正文语种 eng
  • 中图分类 化学;
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