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设计利舒脲鼻腔纳米载体系统,以减少帕金森病大脑中氧化损伤并提高多巴胺水平。

Designing lisuride intranasal nanocarrier system for reduction of oxidative damage with enhanced dopamine level in brain for Parkinsonism.

机构信息

Department of Pharmaceutical Technology, Meerut Institute of Engineering and Technology, NH-58, Delhi-Roorkee Highway, Meerut, 250005, Uttar Pradesh, India.

Department of Pharmaceutical Technology, Meerut Institute of Engineering and Technology, NH-58, Delhi-Roorkee Highway, Meerut, 250005, Uttar Pradesh, India; School of Pharmaceutical and Population Health Informatics, DIT University, Dehradun, Uttarakhand, India.

出版信息

J Psychiatr Res. 2023 Sep;165:205-218. doi: 10.1016/j.jpsychires.2023.07.030. Epub 2023 Jul 21.

DOI:10.1016/j.jpsychires.2023.07.030
PMID:37517241
Abstract

In the present study, nanoemulsion (NE) loaded with lisuride were formulated for delivering drug to brain via intranasal route. Dopamine levels, pharmacokinetic, and antioxidant activity were estimated. Antioxidant effect of lisuride NE was assessed in-vivo using oxidative stress models revealing symptoms like those of Parkinson's disease. Intranasally administered lisuride NE-treated group revealed a greater number of antioxidant enzymes, such as superoxide dismutase (SOD) and glutathione (GSH) as compared to the intravenously administered lisuride suspension in haloperidol rat model. Additionally, it was observed that lisuride NE can decrease dopamine loss. When lisuride NE was administered intranasally resulted in considerably higher dopamine concentrations (17.48 ± 0.05 ng/mL) in comparison to rats receiving haloperidol (7.28 ± 0.02 ng/mL). From study, it is suggested that NE is a possible strategy to deliver lisuride intranasally to lower free radical damage and prevent the biochemical alterations associated with Parkinson's disease.

摘要

在本研究中,通过鼻腔途径给药,用纳米乳(NE)包载利舒脲。评估了多巴胺水平、药代动力学和抗氧化活性。使用体内氧化应激模型评估利舒脲 NE 的抗氧化作用,这些模型显示出类似于帕金森病的症状。与静脉内给予氟哌啶醇大鼠模型中的利舒脲混悬液相比,经鼻腔给予利舒脲 NE 治疗组的超氧化物歧化酶(SOD)和谷胱甘肽(GSH)等抗氧化酶数量增加。此外,还观察到利舒脲 NE 可以减少多巴胺的损失。当利舒脲 NE 经鼻腔给药时,与接受氟哌啶醇的大鼠相比,多巴胺浓度(17.48±0.05ng/mL)显著升高(7.28±0.02ng/mL)。研究表明,NE 可能是一种通过鼻腔给予利舒脲的策略,以降低自由基损伤并防止与帕金森病相关的生化改变。

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