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经鼻内给予含洋葱提取物脂质体改善小鼠缺血再灌注诱导的脑损伤。

Amelioration of ischaemia reperfusion-induced cerebral injury in mice by liposomes containing Allium cepa fraction administered intranasally.

机构信息

a Department of Pharmaceutical Sciences and Drug Research , Punjabi University , Patiala , India.

b Maharaja Agrasen School of Pharmacy , Maharaja Agrasen University , Baddi, Solan , Himachal Pradesh , India.

出版信息

Artif Cells Nanomed Biotechnol. 2018;46(sup3):S982-S992. doi: 10.1080/21691401.2018.1523181. Epub 2018 Nov 19.

Abstract

Neuroprotection in ischaemic stroke prevents neuronal injury and subsequent death. Our earlier work revealed the neuroprotective effect of ethylacetate fraction (EF) obtained from Allium cepa outer scales in a mouse model of cerebral ischaemia-reperfusion (I-R) injury. The present study was designed to develop and optimize a liposomal delivery system for EF, along with its biological assessment. Thin film hydration method was used for the preparation of liposomal formulation. The prepared liposomes were optimized with respect to particle size, size distribution and encapsulation efficiency (EE) and characterised on the basis of zeta potential, in vitro release, morphology (TEM) and physical stability. The biological activity of the optimized liposomal formulation (EF-L; 8.5 mg/kg, intra-nasal) was evaluated after induction of cerebral injury in the experimental animals. Neuroprotective effects were assessed in terms of improvement of cognitive/sensorimotor functions and reduction of cerebral infarct size and brain oxidative stress. EF-L (particle size of 204.93 ± 7.96 nm; EE of 88.02 ± 2.09%; zeta potential of -20.8 ± 1.24 mV) showed controlled release pattern; spherical shape and were physically stable for 60 days at 4 °C. Intra-nasal administration of EF-L produced significant neuroprotection in mice at 1/10th the oral dose. Thus, EF-L may be developed as a neuroprotective formulation.

摘要

神经保护在缺血性中风中可预防神经元损伤和随后的死亡。我们之前的工作揭示了从洋葱鳞片中获得的乙酸乙酯部分(EF)在脑缺血再灌注(I-R)损伤的小鼠模型中的神经保护作用。本研究旨在开发和优化 EF 的脂质体传递系统,并对其进行生物学评估。薄膜水化法用于制备脂质体配方。根据 Zeta 电位、体外释放、形态(TEM)和物理稳定性,对制备的脂质体进行了粒径、粒径分布和包封效率(EE)的优化。在实验动物诱导脑损伤后,评估了优化的脂质体配方(EF-L;8.5mg/kg,鼻内)的生物活性。神经保护作用是通过改善认知/感觉运动功能以及减少脑梗死面积和脑氧化应激来评估的。EF-L(粒径为 204.93±7.96nm;EE 为 88.02±2.09%;Zeta 电位为-20.8±1.24mV)显示出控制释放模式;球形,在 4°C 下 60 天内物理稳定。鼻内给予 EF-L 可使小鼠在口服剂量的 1/10 时产生显著的神经保护作用。因此,EF-L 可开发为一种神经保护制剂。

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