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Curcumin-loaded PLGA-PEG nanoparticles conjugated with B6 peptide for potential use in Alzheimer's disease.
Drug Delivery ( IF 6 ) Pub Date : 2018-08-16 , DOI: 10.1080/10717544.2018.1461955
Shengnuo Fan 1 , Yuqiu Zheng 1 , Xuan Liu 2 , Wenli Fang 1 , Xiaoyu Chen 1, 3 , Wang Liao 1 , Xiuna Jing 1 , Ming Lei 1 , Enxiang Tao 1 , Qiulan Ma 4 , Xingmei Zhang 5 , Rui Guo 2 , Jun Liu 1, 6, 7
Affiliation  

Alzheimer's disease is a neurodegenerative disorder mainly characterized by β-amyloid deposit and tau hyperphosphorylation with no curative treatments. Curcumin (Cur) has been proved to have potential use in Alzheimer's disease with its anti-amyloid, anti-inflammatory, and anti-oxidant properties, etc. However, its hydrophobicity and low bioavailability hinder its application. In this paper, we designed a novel brain-target nanoparticle, poly(lactide-co-glycolide)-block-poly(ethylene glycol) (PLGA-PEG) conjugated with B6 peptide and was loaded with Cur (PLGA-PEG-B6/Cur) and administered it into HT22 cells and APP/PS1 Al transgenic mice. The in vitro assays including dynamic light scattering (DLS), flow cytometry (FCM), red blood cell (RBC) lysis, and thromboelastography (TEG) analysis indicated that this nanoparticle could narrow the diameter of Cur, increase its cellular uptake and possess good blood compatibility. The results from Morris water maze proved that PLGA-PEG-B6/Cur could tremendously improve the spatial learning and memory capability of APP/PS1 mice, compared with native Cur. The ex vivo assays including Bielschowsky silver staining, immunostaining, and western blotting demonstrated that PLGA-PEG-B6/Cur could reduce hippocampal β-amyloid formation and deposit and tau hyperphosphorylation. Thus, we suggested that PLGA-PEG-B6/Cur nanoparticles would be of potential and promising use for the treatment of Alzheimer's disease.

中文翻译:

姜黄素负载的PLGA-PEG纳米颗粒与B6肽偶联,可用于阿尔茨海默氏病。

阿尔茨海默氏病是一种神经退行性疾病,主要特征是β-淀粉样蛋白沉积和tau过度磷酸化,而没有治愈性疗法。姜黄素(Cur)具有抗淀粉样蛋白,抗炎和抗氧化等特性,已被证明可在阿尔茨海默氏病中使用。但是,其疏水性和低生物利用度阻碍了其应用。在本文中,我们设计了一种新型的脑靶向纳米粒子,与B6肽共轭的聚丙交酯-乙交酯-嵌段-聚乙二醇(PLGA-PEG)并负载了Cur(PLGA-PEG-B6 / Cur),然后将其施用给HT22细胞和APP / PS1 A1转基因小鼠。体外测定包括动态光散射(DLS),流式细胞仪(FCM),红细胞(RBC)裂解,血栓弹力图(TEG)分析表明,该纳米粒子可缩小Cur的直径,增加其细胞摄取并具有良好的血液相容性。莫里斯水迷宫的结果证明,与天然Cur相比,PLGA-PEG-B6 / Cur可以极大地改善APP / PS1小鼠的空间学习和记忆能力。体外试验包括Bielschowsky银染色,免疫染色和Western印迹表明PLGA-PEG-B6 / Cur可以减少海马β-淀粉样蛋白的形成和沉积以及tau蛋白的过度磷酸化。因此,我们认为PLGA-PEG-B6 / Cur纳米颗粒在治疗阿尔茨海默氏病方面具有潜在的前景。莫里斯水迷宫的结果证明,与天然Cur相比,PLGA-PEG-B6 / Cur可以极大地改善APP / PS1小鼠的空间学习和记忆能力。体外试验包括Bielschowsky银染色,免疫染色和Western印迹表明PLGA-PEG-B6 / Cur可以减少海马β-淀粉样蛋白的形成和沉积以及tau蛋白的过度磷酸化。因此,我们认为PLGA-PEG-B6 / Cur纳米颗粒在治疗阿尔茨海默氏病方面具有潜在的前景。莫里斯水迷宫的结果证明,与天然Cur相比,PLGA-PEG-B6 / Cur可以极大地改善APP / PS1小鼠的空间学习和记忆能力。体外试验包括Bielschowsky银染色,免疫染色和Western印迹表明PLGA-PEG-B6 / Cur可以减少海马β-淀粉样蛋白的形成和沉积以及tau蛋白的过度磷酸化。因此,我们认为PLGA-PEG-B6 / Cur纳米颗粒在治疗阿尔茨海默氏病方面具有潜在的前景。
更新日期:2018-08-15
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