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Nanospheres based on PLGA/amphiphilic cyclodextrin assemblies as potential enhancers of Methylene Blue neuroprotective effect

机译:基于PLGA /两亲环糊精组件的纳米球作为亚甲基蓝神经保护作用的潜在增强剂

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Methylene Blue (MB) has recently showed beneficial effects towards neurological disorders such as Alzheimer’s and Parkinson’s diseases. Intravenous administration of MB could be difficult because of its poor cooperation with patients, thus entrapment in a carrier system could improve compliance. PLGA nanospheres have been proposed as a delivery system for MB, but they suffer from low encapsulation efficiency and rapid release of their cargo. Here, we design nanospheres with high affinity for hydrophilic MB based on PLGA and a non-ionic amphiphilic cyclodextrin (SC6OH) as an additional component. Interaction between MB and SC6OH was firstly investigated by UV-vis spectroscopy and steady-state emission fluorescence in aqueous solution. PLGA/SC6OH nanospheres loaded with MB were prepared by a nanoprecipitation/solvent displacement method and characterized by STEM and FTIR-ATR analysis. They display sizes of about 200 nm, and a higher encapsulation efficiency with respect to PLGA nanospheres prepared without SC6OH. This latter modulates the release profiles of MB from the nanospheres, producing a release sustained for five days. In vitro biological studies on human neuroblastoma SH-SY5Y cells demonstrated that PLGA/SC6OH nanospheres did not affect cell viability. In addition, MB loaded-PLGA/SC6OH nanospheres produced significant neuroprotection against the metabolic effects of iodoacetic acid, especially in the presence of NADH electron donor.
机译:亚甲基蓝(MB)最近对阿尔茨海默氏症和帕金森病等神经系统疾病表现出有益效果。由于其与患者的合作差,因此静脉内施用MB可能是困难的,因此载体系统中的夹杂物可以改善合规性。已经提出了PLGA纳米球作为MB的递送系统,但它们遭受低封装效率和其货物的快速释放。这里,基于PLGA和非离子两亲性环糊精(SC6OH)为另外的组分,为亲水性MB具有高亲和力的纳米球设计。通过UV-Vis光谱和水溶液中的稳态发射荧光首先研究MB和SC6OH之间的相互作用。用纳米沉淀/溶剂位移方法制备装有MB的PLGA / SC6OH纳米球,其特征在于茎和FTIR-ATR分析。它们显示大约200nm的大小,以及相对于没有SC 6OH制备的PLGA纳米球的封装效率较高。后者调节来自纳米球的Mb的释放曲线,产生持续5天的释放。体外生物学研究人神经母细胞瘤SH-SY5Y细胞表明PLGA / SC6OH纳米球不影响细胞活力。此外,Mb负载-PLGA / SC6OH纳米球产生了针对碘乙酸的代谢作用的显着神经保护,特别是在NADH电子给体的存在下。

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