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基于椰子油的白藜芦醇纳米乳剂:采用响应面法进行优化、稳定性评估及药代动力学评价

Coconut oil-based resveratrol nanoemulsion: Optimization using response surface methodology, stability assessment and pharmacokinetic evaluation.

作者信息

Kotta Sabna, Mubarak Aldawsari Hibah, Badr-Eldin Shaimaa M, Alhakamy Nabil A, Md Shadab

机构信息

Department of Pharmaceutics, Faculty of Pharmacy, King Abdulaziz University, Jeddah 21589, Saudi Arabia; Center of Excellence for Drug Research and Pharmaceutical Industries, King Abdulaziz University, Jeddah 21589, Saudi Arabia.

Department of Pharmaceutics, Faculty of Pharmacy, King Abdulaziz University, Jeddah 21589, Saudi Arabia; Center of Excellence for Drug Research and Pharmaceutical Industries, King Abdulaziz University, Jeddah 21589, Saudi Arabia; Mohamed Saeed Tamer Chair for Pharmaceutical Industries, King Abdulaziz University, Jeddah 21589, Saudi Arabia.

出版信息

Food Chem. 2021 Apr 5;357:129721. doi: 10.1016/j.foodchem.2021.129721.

Abstract

Phytochemicals are widely studied for therapeutic applications and nanostructured delivery systems for phytochemicals are under spotlight. Resveratrol is a promising candidate for neurodegenerative disorders. In the present study, we aimed to formulate nanoemulsion of resveratrol by ultrasonication process using response surface methodology. The effect of both formulation and ultrasonication process factors were studied for the nanoemulsification process using coconut oil, Pluronic-P107, and Cremophor EL. The time, intensity, and power of ultrasonication were selected as process factors. The globule size, PDI, and zeta potential were the responses selected. The concentrations of oil and surfactant and the intensity were found to significantly influence the globule size. The concentration of resveratrol in the optimized nanoemulsion formulation was 2.6442 mg/ml. The in vitro drug release in pH 6.8 phosphate buffer as well as in vitro permeation study on goat nasal mucosa proved the superiority of the nanoemulsion formulation. On intranasal administration in the rat at a resveratrol dose of 2 mg/kg, the brain targeting efficacy of the nanoemulsion formulation was high. Overall, this research provides the benefit of intake of resveratrol containing fruits and, its incorporation into nanoemulsions system could be a promising alternative for the management of Alzheimer's disease.

摘要

植物化学物质因其治疗应用而受到广泛研究,用于植物化学物质的纳米结构递送系统备受关注。白藜芦醇是神经退行性疾病的一个有前景的候选药物。在本研究中,我们旨在使用响应面法通过超声处理制备白藜芦醇纳米乳剂。使用椰子油、普朗尼克 - P107和聚氧乙烯蓖麻油EL研究了配方和超声处理工艺因素对纳米乳化过程的影响。选择超声处理的时间、强度和功率作为工艺因素。选择球粒大小、多分散指数(PDI)和zeta电位作为响应指标。发现油和表面活性剂的浓度以及强度对球粒大小有显著影响。优化后的纳米乳剂配方中白藜芦醇的浓度为2.6442毫克/毫升。在pH 6.8磷酸盐缓冲液中的体外药物释放以及在山羊鼻黏膜上的体外渗透研究证明了纳米乳剂配方的优越性。以2毫克/千克的白藜芦醇剂量经鼻给药大鼠时,纳米乳剂配方的脑靶向效果良好。总体而言,本研究为摄入含白藜芦醇的水果提供了益处,并且将其纳入纳米乳剂系统可能是治疗阿尔茨海默病的一种有前景的替代方法。

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