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用聚山梨酯80包被的胸腺醌壳聚糖纳米粒作为利血平诱导的抑郁动物模型中的新型治疗剂。

Thymoquinone-encapsulated chitosan nanoparticles coated with polysorbate 80 as a novel treatment agent in a reserpine-induced depression animal model.

作者信息

Fahmy Heba M, Khadrawy Yasser A, Abd-El Daim Taiseer M, Elfeky Amena S, Abd Rabo Amera A, Mustafa Amira B, Mostafa Islam T

机构信息

Biophysics Department, Faculty of Science, Cairo University, Egypt.

Medical Physiology Department, Medical Division, National Research Centre, Egypt.

出版信息

Physiol Behav. 2020 Aug 1;222:112934. doi: 10.1016/j.physbeh.2020.112934. Epub 2020 Apr 27.

DOI:10.1016/j.physbeh.2020.112934
PMID:32353367
Abstract

Depression is a mental illness with a high prevalence in humans reaching 21% of the worldwide population.The present study aims to evaluate the antidepressant effect of different formulations of Thymoquinone; free Thymoquinone (TQ), Thymoquinone-loaded Chitosan nanoparticles (TQ-TPP-Cs NPs) and Thymoquinone-loaded Chitosan nanoparticles coated with polysorbate 80 (TQ-TPP-Cs NPs-PSb80) that have been prepared to avoid the low bioavailability of TQ. Rats were randomly separated into control rats, depression control induced by reserpine, rat model treated with TQ, rat model treated with TQ-TPP-Cs NPs and rat model treated with TQ-TPP-Cs NPs-PSb80. The results indicate that TQ-TPP-Cs NPs loaded with polysorbate 80 was more efficient in ameliorating the behavioral and neurochemical changes induced by reserpine than TQ and TQ-TPP-Cs NPs. Formulationswere characterized for size, morphology, encapsulation efficiency and in vitro drug release before their use in treatment. Reserpine induced a reduction in motor activity and swimming time and increased immobility time as indicated from the open field test (OFT) and forced swimming test (FST). In addition, a significant decrease in the monoamine neurotransmitters serotonin (5-HT), norepinephrine (NE) and dopamine (DA) was recorded in the cortex, hippocampus and striatum of reserpine-treated rats. The present data suggest that the antidepressant efficacy of TQ could be enhanced by engaging TQ with chitosan nanoparticles as a drug carrier and the formulations were modified by coating with polysorbate 80.

摘要

抑郁症是一种在人类中高发的精神疾病,全球患病率达21%。本研究旨在评估不同制剂的百里醌(游离百里醌(TQ)、负载百里醌的壳聚糖纳米粒(TQ-TPP-Cs NPs)和负载百里醌且包被聚山梨酯80的壳聚糖纳米粒(TQ-TPP-Cs NPs-PSb80))的抗抑郁作用,制备这些制剂是为了避免TQ生物利用度低的问题。将大鼠随机分为对照大鼠、利血平诱导的抑郁对照组、用TQ治疗的大鼠模型、用TQ-TPP-Cs NPs治疗的大鼠模型和用TQ-TPP-Cs NPs-PSb80治疗的大鼠模型。结果表明,负载聚山梨酯80的TQ-TPP-Cs NPs在改善利血平诱导的行为和神经化学变化方面比TQ和TQ-TPP-Cs NPs更有效。在用于治疗前,对制剂的大小、形态、包封率和体外药物释放进行了表征。如旷场试验(OFT)和强迫游泳试验(FST)所示,利血平导致运动活动和游泳时间减少,不动时间增加。此外,在利血平处理的大鼠的皮质、海马和纹状体中,单胺神经递质5-羟色胺(5-HT)、去甲肾上腺素(NE)和多巴胺(DA)显著减少。目前的数据表明,通过将TQ与壳聚糖纳米粒作为药物载体结合,可以提高TQ的抗抑郁疗效,并且通过用聚山梨酯80包被对制剂进行了改良。

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