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人工载脂蛋白包膜使纳米颗粒能够靶向脑部。

Artificial apolipoprotein corona enables nanoparticle brain targeting.

机构信息

School of Medicine and Surgery, Nanomedicine Center, Neuroscience Center, University of Milano-Bicocca, Monza, Italy.

Department of Pharmaceutical Sciences, University of Perugia, Perugia, Italy.

出版信息

Nanomedicine. 2018 Feb;14(2):429-438. doi: 10.1016/j.nano.2017.11.008. Epub 2017 Nov 21.

Abstract

Many potential therapeutic compounds for brain diseases fail to reach their molecular targets due to the impermeability of the blood-brain barrier, limiting their clinical development. Nanotechnology-based approaches might improve compounds pharmacokinetics by enhancing binding to the cerebrovascular endothelium and translocation into the brain. Adsorption of apolipoprotein E4 onto polysorbate 80-stabilized nanoparticles to produce a protein corona allows the specific targeting of cerebrovascular endothelium. This strategy increased nanoparticle translocation into brain parenchyma, and improved brain nanoparticle accumulation 3-fold compared to undecorated particles (119.8 vs 40.5 picomoles). Apolipoprotein decorated nanoparticles have high clinical translational potential and may improve the development of nanotechnology-based medicine for a variety of neurological diseases.

摘要

由于血脑屏障的不渗透性,许多用于脑部疾病的潜在治疗化合物无法到达其分子靶点,从而限制了它们的临床开发。基于纳米技术的方法可以通过增强与脑血管内皮细胞的结合和向脑内转移来改善化合物的药代动力学。载脂蛋白 E4 吸附到聚山梨醇酯 80 稳定的纳米颗粒上,形成蛋白冠,从而可以特异性靶向脑血管内皮细胞。与未修饰的颗粒相比,该策略使纳米颗粒向脑实质的转移增加了 3 倍,脑内纳米颗粒的积累增加了 3 倍(119.8 与 40.5 皮摩尔)。载脂蛋白修饰的纳米颗粒具有很高的临床转化潜力,可能会改善各种神经疾病的基于纳米技术的药物的开发。

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