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首页> 外文期刊>Nanotechnology >Synergistic antioxidant action of vitamin E and rutin SNEDDS in ameliorating oxidative stress in a Parkinson's disease model
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Synergistic antioxidant action of vitamin E and rutin SNEDDS in ameliorating oxidative stress in a Parkinson's disease model

机译：维生素E和芦丁SNEDDS在减轻帕金森病模型中的氧化应激中的协同抗氧化作用

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Purpose. Oxidative stress is the leading cause in the pathogenesis of Parkinson's disease. Rutin is a naturally occurring strong antioxidant molecule with wide therapeutic applications. It suffers from the problem of low oral bioavailability which is due to its poor aqueous solubility. Methods. In order to increase the solubility self-nanoemulsifying drug delivery systems (SNEDDS) of rutin were prepared. The oil, surfactant and co-surfactant were selected based on solubility/miscibility studies. Optimization was done by a three-factor, four-level (34) Box-Behnken design. The independent factors were oil, surfactant and co-surfactant concentration and the dependent variables were globule size, self-emulsification time, % transmittance and cumulative percentage of drug release. The optimized SNEDDS formulation (RSE6) was evaluated for various release studies. Antioxidant activity was assessed by various in vitro tests such as 2,2-diphenyl-1-picrylhydrazyl and reducing power assay. Oxidative stress models which had Parkinson's-type symptoms were used to determine the antioxidant potential of rutin SNEDDS in vivo. Permeation was assessed through confocal laser scanning microscopy. Results. An optimized SNEDDS formulation consisting of Sefsol + vitamin E-Solutol HS 15-Transcutol P at proportions of 25: 35: 17.5 (w/w) was prepared and characterized. The globule size and polydispersity index of the optimized formulation was found to be 16.08 +/- 0.02 nm and 0.124 +/- 0.01, respectively. A significant (p < 0.05) increase in the percentage of drug release was achieved in the case of the optimized formulation as compared to rutin suspension. Pharmacokinetic study showed a 2.3-fold increase in relative oral bioavailability. The optimized formulation had significant in vitro and in vivo antioxidant activity. Conclusion. Rutin SNEDDS have been successfully prepared and they can serve as an effective tool in enhancing the oral bioavailability and efficacy of rutin, thus helping in ameliorating oxidative stress in neurodegenerative disorders like Parkinson's disease.
机译：目的。氧化应激是帕金森氏病发病机理的主要原因。芦丁是天然存在的强抗氧化剂分子，具有广泛的治疗应用。由于其水溶性差，存在口服生物利用度低的问题。方法。为了增加溶解度，制备了芦丁的自纳米乳化药物递送系统（SNEDDS）。基于溶解度/混溶性研究选择了油，表面活性剂和助表面活性剂。通过三因素四级（34）Box-Behnken设计进行了优化。独立因素是油，表面活性剂和辅助表面活性剂的浓度，因变量是小球尺寸，自乳化时间，透光率百分比和药物释放的累积百分比。针对各种释放研究评估了优化的SNEDDS配方（RSE6）。通过各种体外试验，例如2，2-二苯基-1-吡啶并肼和还原能力测定法评估抗氧化活性。具有帕金森氏型症状的氧化应激模型用于确定芦丁SNEDDS在体内的抗氧化能力。通过共聚焦激光扫描显微镜评估渗透。结果。制备并表征了由Sefsol +维生素E-Solutol HS 15-Transcutol P比例为25：35：17.5（w / w）组成的优化SNEDDS配方。发现优化配方的小球尺寸和多分散指数分别为16.08 +/- 0.02 nm和0.124 +/- 0.01。与芦丁悬浮液相比，在优化配方的情况下，药物释放百分比显着提高（p <0.05）。药代动力学研究表明，相对口服生物利用度提高了2.3倍。优化的制剂具有显着的体外和体内抗氧化活性。结论。芦丁SNEDDS已成功制备，它们可作为增强芦丁口服生物利用度和功效的有效工具，从而有助于缓解神经退行性疾病（如帕金森氏病）中的氧化应激。

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