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Improved Neuroprotective Effects of Gallic Acid-Loaded Chitosan Nanoparticles Against Ischemic Stroke.
Rejuvenation Research ( IF 2.6 ) Pub Date : 2020-08-14 , DOI: 10.1089/rej.2019.2230
Yongmei Zhao 1 , Duolu Li 1 , Zhenfeng Zhu 1 , Ya Sun 1
Affiliation  

Ischemic stroke is a typical cerebrovascular illness with high morbidity and mortality worldwide. Nevertheless, strategies for the prevention and treatment of cerebral ischemia/reperfusion injury (CIRI) are limited. Gallic acid (GA) is a plant polyphenol that has been used against CIRI. However, the pharmacokinetic (PK) properties of GA, such as its low absorption, poor bioavailability, and quick elimination, have negative effects on its application. To strengthen its effectiveness, a delivery system of GA-loaded o-carboxymethyl chitosan nanoparticles (GA-NPs) was synthesized in our study. In PKs study, GA-NPs apparently increases the area under the curve of plasma concentration–time and prolonged half-life of GA. Then, we measured the in vitro and in vivo effects of the GA-NPs in the oxygen glucose deprivation model and the middle cerebral artery occlusion model. The results from our pharmacodynamic studies, including assessment of neurological deficit, cerebral infarction, levels of inflammation, and oxidative stress, showed that GA-NPs possess better neuroprotection compared with GA. In conclusion, GA-NPs may be used as an efficacious delivery vehicle for GA in the treatment of CIRI.

中文翻译:

没食子酸壳聚糖纳米粒对缺血性中风的改善的神经保护作用。

缺血性中风是一种典型的脑血管疾病,在世界范围内具有较高的发病率和死亡率。然而,预防和治疗脑缺血/再灌注损伤(CIRI)的策略是有限的。没食子酸(GA)是一种已用于抗CIRI的植物多酚。但是,GA的药代动力学(PK)特性,例如其低吸收,不良的生物利用度和快速消除,对其应用具有负面影响。为了增强其有效性,在我们的研究中合成了载有GA的邻羧甲基壳聚糖纳米颗粒(GA-NPs)的递送系统。在PKs研究中,GA-NPs明显增加了血浆浓度-时间曲线下的面积,并延长了GA的半衰期。然后,我们测量了体内体外-NPs在氧葡萄糖剥夺模型和大脑中动脉闭塞模型中的作用 我们的药效学研究结果包括对神经功能缺损,脑梗塞,炎症水平和氧化应激的评估,表明GA-NP比GA具有更好的神经保护作用。总之,GA-NPs可以作为GA在CIRI治疗中的有效载体。
更新日期:2020-08-20
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