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Quercetin lipid nanoparticles functionalized with transferrin for Alzheimer's disease.
European Journal of Pharmaceutical Sciences ( IF 4.3 ) Pub Date : 2020-03-19 , DOI: 10.1016/j.ejps.2020.105314 R G R Pinheiro 1 , A Granja 1 , J A Loureiro 2 , M C Pereira 2 , M Pinheiro 1 , A R Neves 3 , S Reis 1
European Journal of Pharmaceutical Sciences ( IF 4.3 ) Pub Date : 2020-03-19 , DOI: 10.1016/j.ejps.2020.105314 R G R Pinheiro 1 , A Granja 1 , J A Loureiro 2 , M C Pereira 2 , M Pinheiro 1 , A R Neves 3 , S Reis 1
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Quercetin was encapsulated in lipid nanoparticles (SLN and NLC) to take advantage of its neuroprotective properties in Alzheimer's disease. The nanoparticles were functionalized with transferrin to facilitate the passage across the blood-brain barrier through the transferrin receptors overexpressed in brain endothelial cells. NMR and FTIR confirmed the functionalization of the nanoparticles with transferrin. TEM results showed all nanoparticles presented spherical morphology. Nanoparticles exhibited size around 200 nm and zeta potential values higher than -30 mV. Quercetin entrapment efficiency was around 80-90%. LDH cytotoxicity assays in hCMEC/D3 cell line demonstrated that even for the highest concentration (30 μM) nanoparticles did not reveal cytotoxicity after 4 h of incubation. Permeability studies across hCMEC/D3 cell monolayers showed NLC permeate more the blood-brain barrier, while amyloid-beta studies demonstrated NLC-transferrin have the capacity to inhibit fibril formation. Nanoparticles seem to be suitable for brain applications, mainly for Alzheimer's disease due to inhibition of amyloid-beta aggregation.
中文翻译：
用运铁蛋白功能化的槲皮素脂质纳米颗粒可治疗阿尔茨海默氏病。
槲皮素被包裹在脂质纳米颗粒（SLN和NLC）中，以利用其在阿尔茨海默氏病中的神经保护特性。用转铁蛋白对纳米颗粒进行功能化，以利于在脑内皮细胞中过表达的转铁蛋白受体穿过血脑屏障。NMR和FTIR证实了转铁蛋白对纳米颗粒的功能化。TEM结果表明，所有纳米颗粒均呈球形。纳米颗粒表现出约200 nm的大小，ζ电势值高于-30 mV。槲皮素的包封率约为80-90％。hCMEC / D3细胞系中的LDH细胞毒性试验表明，即使在4 h孵育后，即使是最高浓度（30μM）的纳米颗粒也未显示出细胞毒性。跨hCMEC / D3细胞单层的渗透性研究表明NLC渗透血脑屏障的能力更大，而β淀粉样蛋白研究表明NLC-转铁蛋白具有抑制原纤维形成的能力。由于抑制了β淀粉样蛋白的聚集，纳米颗粒似乎适用于大脑应用，主要适用于阿尔茨海默氏病。
更新日期：2020-04-21
中文翻译：
用运铁蛋白功能化的槲皮素脂质纳米颗粒可治疗阿尔茨海默氏病。
槲皮素被包裹在脂质纳米颗粒（SLN和NLC）中，以利用其在阿尔茨海默氏病中的神经保护特性。用转铁蛋白对纳米颗粒进行功能化，以利于在脑内皮细胞中过表达的转铁蛋白受体穿过血脑屏障。NMR和FTIR证实了转铁蛋白对纳米颗粒的功能化。TEM结果表明，所有纳米颗粒均呈球形。纳米颗粒表现出约200 nm的大小，ζ电势值高于-30 mV。槲皮素的包封率约为80-90％。hCMEC / D3细胞系中的LDH细胞毒性试验表明，即使在4 h孵育后，即使是最高浓度（30μM）的纳米颗粒也未显示出细胞毒性。跨hCMEC / D3细胞单层的渗透性研究表明NLC渗透血脑屏障的能力更大，而β淀粉样蛋白研究表明NLC-转铁蛋白具有抑制原纤维形成的能力。由于抑制了β淀粉样蛋白的聚集，纳米颗粒似乎适用于大脑应用，主要适用于阿尔茨海默氏病。
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