Globally, ischemic stroke is a leading cause of death and adult disability. Previous efforts to repair damaged brain tissue following ischemic events have been hindered by the relative isolation of the central nervous system. We have developed a gelatin nanoparticle-mediated intranasal drug delivery system as an efficient, non-invasive method for delivering 17β-estradiol (E2) specifically to the brain, enhancing neuroprotection, and limiting systemic side effects. Young adult male C57BL/6 J mice subjected to 30 min of middle cerebral artery occlusion (MCAO) were administered intranasal preparations of E2-GNPs, water soluble E2, or saline as control 1 h after reperfusion. Following intranasal administration of 500 ng E2-GNPs, brain E2 content rose by 5.24 fold (P < 0.0001) after 30 min and remained elevated by 2.5 fold at 2 h (P < 0.05). The 100 ng dose of E2-GNPs reduced mean infarct volume by 54.3% (P < 0.05, n = 4) in comparison to saline treated controls, demonstrating our intranasal delivery system's efficacy.

在全球范围内，缺血性中风是导致死亡和成人残疾的主要原因。中枢神经系统的相对隔离阻碍了缺血事件后修复受损脑组织的先前工作。我们已经开发了一种明胶纳米颗粒介导的鼻内给药系统，作为一种有效的，非侵入性的方法，可专门将17β-雌二醇（E2）输送至大脑，增强神经保护作用并限制全身性副作用。在再灌注后1 h，对接受30分钟大脑中动脉闭塞（MCAO）的成年雄性C57BL / 6 J小鼠进行鼻腔内E2-GNPs，水溶性E2或盐水的控制。鼻内施用500 ng E2-GNP后，脑E2含量增加了5.24倍（P 30分钟后<0.0001），并在2小时时保持2.5倍的升高（P  <0.05）。 与经盐水处理的对照组相比，100 ng剂量的E2-GNP可使平均梗死体积减少54.3％（P <0.05，n = 4），这证明了我们鼻内给药系统的功效。