Department of Basic Medical Science, Medical College, Xiamen University, Xiamen, 361102, China.
Department of Chemistry, College of Chemistry and Chemical Engineering, Xiamen University, Xiamen, 361005, China.
J Nanobiotechnology. 2019 Jan 19;17(1):8. doi: 10.1186/s12951-019-0442-x.
Leading to more and more deaths and disabilities, stroke has become a serious threat to human health. What's more, few effective drugs are available in clinic till now.
In this research, we prepared a novel neuroprotective nanoformation (OEA-SPC NPs) via the combination of the nanoparticle drug delivery system with the endogenous N-oleoylethanolamine (OEA). By forming hydrogen bond between OEA and the carrier-soybean phosphatidylcholine (SPC), the form of OEA was turned into amorphus state when loading to the nanoparticles, which greatly improved its bioavailability. Then the following systematic experiments revealed the efficient neuroprotective effect of OEA-SPC NPs in vivo. Compared with the MCAO group, the cerebral infarct volume was reduced by 81.1%, and the edema degree by 78.4% via the oral administration of OEA-SPC NPs. And the neurological deficit scores illustrated that the MCAO rats treated with OEA-SPC NPs exhibited significantly less neurological dysfunction. The Morris water maze test indicated that the spatial learning and memory of cerebral ischemia model rats were almost recovered to the normal level. Besides, the OEA-SPC NPs could inhibit the inflammation of reperfusion to a very slight level.
These results suggest that the OEA-SPC NPs have a great chance to be a potential anti-stroke formation for clinic application and actually bring hope to thousands of stroke patients.
中风导致的死亡和残疾人数不断增加，已成为严重威胁人类健康的疾病。更糟糕的是，目前临床上几乎没有有效的治疗药物。
本研究通过将纳米药物递送系统与内源性 N-油酰乙醇胺（OEA）结合，制备了一种新型神经保护纳米制剂（OEA-SPC NPs）。通过 OEA 与载体大豆磷脂酰胆碱（SPC）之间形成氢键，当 OEA 加载到纳米粒子中时，其形式转变为无定形状态，从而大大提高了其生物利用度。随后的系统实验揭示了 OEA-SPC NPs 在体内的有效神经保护作用。与 MCAO 组相比，通过口服 OEA-SPC NPs，脑梗死体积减少了 81.1%，脑水肿程度减少了 78.4%。神经功能缺损评分表明，用 OEA-SPC NPs 治疗的 MCAO 大鼠的神经功能障碍明显减轻。Morris 水迷宫试验表明，脑缺血模型大鼠的空间学习和记忆几乎恢复到正常水平。此外，OEA-SPC NPs 可将再灌注炎症抑制在非常轻微的水平。
这些结果表明，OEA-SPC NPs 很有希望成为一种用于临床应用的潜在抗中风药物，为成千上万的中风患者带来希望。
