Department of Chemistry, School of Chemical and Life Sciences, Jamia Hamdard, New Delhi, India.
Department of Medical Elementology and Toxicology School of Chemical and Life Science, Jamia Hamdard, New Delhi, India.
Int Immunopharmacol. 2021 Dec;101(Pt A):108287. doi: 10.1016/j.intimp.2021.108287. Epub 2021 Nov 1.
Resveratrol has been found to exert protective effects in neurological disorders, including epilepsy. However, its poor bioavailability and difficulty in reaching the brain's targeted location reduce resveratrol's efficacy substantially. The side effects due to the higher concentration of drugs are another matter of concern. The objective of the present study is to propose solutions to these issues by encapsulating resveratrol in glutathione-coated collagen nanoparticles' core. The collagen nanoparticles increase the resveratrol's bioavailability, and glutathione helps in the passage of the encapsulated resveratrol to the target location in the brain. The concentration also substantially reduces due to resveratrol's encapsulation in glutathione-coated collagen nanoparticles. The encapsulated resveratrol is termed nanoresveratrol. The effectiveness of nanoresveratrol on epilepsy seizures was evaluated through histopathological examinations, ELISA tests, and qRT-PCR tests on the hippocampus of the kindled mice. The novelty of the present study thus lies in (i) the synthesis of nanoresveratrol using glutathione-coated collagen nanoparticles and (ii) the application of synthesized nanoresveratrol in the treatment of epilepsy. The study's outcome shows that nanoresveratrol has a favorable impact in reducing cognitive impairment in kindled mice, and it is more effective in controlling epilepsy seizures than resveratrol. The p-values of all the nanoresveratrol-given groups of mice (compared with the diseased group) were substantially smaller (∼10 to 10) than the significance level (0.05), indicating that the nanoresveratrol-given groups are significantly different from the diseased group, i.e., the nanoresveratrol has a significant effect on the mice. The concentration of resveratrol also decreases substantially in the proposed nanoformulation. It was observed that even 0.4 mg/kg of nanoformulation of resveratrol is performing better than 40 mg/kg of resveratrol.
白藜芦醇已被发现对神经紊乱具有保护作用，包括癫痫。然而，其生物利用度差且难以到达大脑的靶向位置，这大大降低了白藜芦醇的疗效。由于药物浓度较高而产生的副作用是另一个值得关注的问题。本研究的目的是通过将白藜芦醇封装在谷胱甘肽涂层胶原纳米粒子的核心中，来解决这些问题。胶原纳米粒子提高了白藜芦醇的生物利用度，而谷胱甘肽有助于将包裹的白藜芦醇递送到大脑中的靶位。由于白藜芦醇被包裹在谷胱甘肽涂层胶原纳米粒子中，其浓度也大大降低。包裹的白藜芦醇被称为纳米白藜芦醇。通过对点燃小鼠海马的组织病理学检查、ELISA 检测和 qRT-PCR 检测，评估了纳米白藜芦醇对癫痫发作的疗效。本研究的新颖之处在于：（i）使用谷胱甘肽涂层胶原纳米粒子合成纳米白藜芦醇；（ii）将合成的纳米白藜芦醇应用于癫痫的治疗。研究结果表明，纳米白藜芦醇在减少点燃小鼠的认知障碍方面有良好的效果，并且在控制癫痫发作方面比白藜芦醇更有效。所有给予纳米白藜芦醇的小鼠组（与患病组相比）的 p 值都明显小于显著性水平（0.05）（∼10 到 10），表明给予纳米白藜芦醇的组与患病组有显著差异，即纳米白藜芦醇对小鼠有显著效果。在提出的纳米制剂中，白藜芦醇的浓度也大大降低。观察到，即使给予 0.4 mg/kg 的纳米白藜芦醇制剂也比给予 40 mg/kg 的白藜芦醇效果更好。
