Wu Shichao, Yang Xiangrui
Department of Nuclear Medicine, Xiangya Hosptal, Central South University, Changsha, Hunan, China.
Key Laboratory of Nanobiological Technology of National Health Commission, Xiangya Hospital, Central South University, Changsha, Hunan, China.
Front Chem. 2022 Sep 8;10:1014208. doi: 10.3389/fchem.2022.1014208. eCollection 2022.
With high mortality, stroke has become a serious threat to human health. Nevertheless, the strategy for stroke therapy is quite limited in the clinic till now. In this research, we prepared a novel neuroprotective nanoformulation (OEA Liposomes) via encapsulating endogenous N-oleoylethanolamine (OEA) in liposomes for intravenous administration. The formulation largely increased the solubility and bioavailability of OEA. Then the following systematic experiments stated the excellent neuroprotective effect of OEA Liposomes . The survival rate of the nanodrug group was largely increased to 75%, while that of the Middle Cerebral Artery Occlusion (MCAO) group was only 41.7%. And the severe neurological functional deficit of the MCAO rats was also significantly improved. What's more, the OEA Liposomes could inhibit the apoptosis of neurons and the inflammation of reperfusion to a very slight level, indicating their outstanding neuroprotective effect. These results indicated that the OEA Liposomes have a great potential for clinic anti-stroke application.
由于死亡率高,中风已成为对人类健康的严重威胁。然而,迄今为止,中风治疗策略在临床上相当有限。在本研究中,我们通过将内源性N-油酰乙醇胺(OEA)包裹在脂质体中制备了一种新型神经保护纳米制剂(OEA脂质体)用于静脉给药。该制剂大大提高了OEA的溶解度和生物利用度。随后的一系列实验表明了OEA脂质体具有优异的神经保护作用。纳米药物组的存活率大幅提高到75%,而大脑中动脉闭塞(MCAO)组仅为41.7%。并且MCAO大鼠严重的神经功能缺损也得到了显著改善。更重要的是,OEA脂质体能够将神经元的凋亡和再灌注炎症抑制到非常轻微的程度,表明它们具有出色的神经保护作用。这些结果表明,OEA脂质体在临床抗中风应用中具有巨大潜力。