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Modified magnetic core-shell mesoporous silica nano-formulations with encapsulated quercetin exhibit anti-amyloid and antioxidant activity
Journal of Inorganic Biochemistry ( IF 3.9 ) Pub Date : 2020-10-06 , DOI: 10.1016/j.jinorgbio.2020.111271
Eleftherios Halevas 1 , Barbara Mavroidi 1 , Christiane M Nday 2 , Jianhua Tang 3 , Graham C Smith 3 , Nikos Boukos 4 , George Litsardakis 5 , Maria Pelecanou 1 , Athanasios Salifoglou 2
Affiliation  

Targeted tissue drug delivery is a challenge in contemporary nanotechnologically driven therapeutic approaches, with the interplay interactions between nanohost and encapsulated drug shaping the ultimate properties of transport, release and efficacy of the drug at its destination. Prompted by the need to pursue the synthesis of such hybrid systems, a family of modified magnetic core-shell mesoporous silica nano-formulations was synthesized with encapsulated quercetin, a natural flavonoid with proven bioactivity. The new nanocarriers were produced via the sol-gel process, using tetraethoxysilane as a precursor and bearing a magnetic core of surface-modified monodispersed magnetite colloidal superparamagnetic nanoparticles, subsequently surface-modified with polyethylene glycol 3000 (PEG3k). The arising nano-formulations were evaluated for their textural and structural properties, exhibiting enhanced solubility and stability in physiological media, as evidenced by the loading capacity, entrapment efficiency results and in vitro release studies of their load. Guided by the increased bioavailability of quercetin in its encapsulated form, further evaluation of the biological activity of the magnetic as well as non-magnetic core-shell nanoparticles, pertaining to their anti-amyloid and antioxidant potential, revealed interference with the aggregation of β-amyloid peptide (Aβ) in Alzheimer's disease, reduction of Aβ cellular toxicity and minimization of Aβ-induced Reactive Oxygen Species (ROS) generation. The data indicate that the biological properties of released quercetin are maintained in the presence of the host nanocarriers. Collectively, the findings suggest that the emerging hybrid nano-formulations can function as efficient nanocarriers of hydrophobic natural flavonoids in the development of multifunctional nanomaterials toward therapeutic applications.



中文翻译:

槲皮素包封的磁性核-壳介孔二氧化硅纳米制剂具有抗淀粉样蛋白和抗氧化活性

在当代纳米技术驱动的治疗方法中,靶向组织药物的输送是一个挑战,纳米宿主与封装的药物之间的相互作用相互作用塑造了药物在其目的地的转运,释放和功效的最终特性。由于需要进行此类杂化系统的合成的提倡,合成了一系列修饰的磁性核-壳介孔二氧化硅纳米制剂,该制剂与封装的槲皮素(一种具有成熟生物活性的天然类黄酮)合成。新的纳米载体是通过溶胶-凝胶法生产的,使用四乙氧基硅烷作为前体并带有表面改性的单分散磁铁矿胶体超顺磁性纳米粒子的磁芯,随后用聚乙二醇3000(PEG3k)进行了表面改性。在槲皮素胶囊化形式的生物利用度提高的指导下,对磁性和非磁性核壳纳米粒子的生物活性进行进一步评估,涉及其抗淀粉样蛋白和抗氧化剂的潜力,揭示了对β-聚集的干扰。淀粉样肽(Aβ)可以治疗阿尔茨海默氏病,降低Aβ细胞毒性并最小化Aβ诱导的活性氧(ROS)生成。数据表明释放的槲皮素的生物学特性在宿主纳米载体存在下得以保持。总的来说,这些发现表明,在向治疗应用发展多功能纳米材料的过程中,新兴的杂化纳米制剂可以作为疏水性天然类黄酮的有效纳米载体。

更新日期:2020-10-16
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