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首页> 外文期刊>RSC Advances >Facile construction of dual-targeting delivery system by using lipid capped polymer nanoparticles for anti-glioma therapy
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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颗粒抗胶质瘤疗法轻松构建双靶点递送系统

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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–PEG2000–COOH) shell. The DSPE–PEG2000–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 ～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，双重靶向药物递送系统被分别靶向血脑屏障（BBB）和脑肿瘤细胞的两个活性配体功能化，提供了改善神经胶质瘤化疗疗效的有前途的策略。成功开发此类系统的关键是使具有活性配体的纳米颗粒（NP）功能化，尽管它们通常会遇到诸如NP聚集，药物泄漏和复杂的化学合成等问题。在本文中，我们报告了通过简单地使用脂质封端的聚合物NPs构建双重靶向递送系统的简便方法。 NPs是用聚乳酸-乙醇-乙醇酸（PLGA）核构建的，用于疏水性阿霉素（DOX）的负载，以及脂质（卵磷脂和DSPE–PEG 2000 –COOH）外壳。 DSPE–PEG 2000 -COOH为配体结合提供了极好的锚。作为概念的证明，通过一步合成，两个血管生成肽2肽和AS1411适体的活性配体与NP共价连接，对粒径，稳定性，载药量和药物释放性能影响很小。在144 h内PBS（pH 7.4）中NP的累积释药率为〜50％，这表明药物具有持续释放的特性。如荧光显微镜和定量流式细胞术所表明的，NP显示脑毛细血管内皮细胞（BCEC）和C6神经胶质瘤细胞的摄取显着增强，证明了双重靶向效率。通过使用体外 BBB模型验证了BBB的渗透能力，并且体外细胞抑制研究表明NPs对神经胶质瘤细胞的细胞毒性增加。

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