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Optimization, physicochemical characterization, and antimicrobial activity of a novel simvastatin nano-niosomal gel against E. coli and S. aureus
Chemistry and Physics of Lipids ( IF 3.4 ) Pub Date : 2020-11-21 , DOI: 10.1016/j.chemphyslip.2020.105019
Iman Akbarzadeh 1 , Maliheh Keramati 2 , Amir Azadi 3 , Elham Afzali 4 , Rasoul Shahbazi 4 , Mohsen Chiani 2 , Dariush Norouzian 2 , Haleh Bakhshandeh 2
Affiliation  

Niosomes, as a kind of drug delivery system, is widely used for the topical delivery of lipophilic drugs. Optimization of niosomes plays an essential role in enhancing their therapeutic efficiencies. This study aims to prepare an optimized niosomal formulation of simvastatin (nSIM), a lipophilic member of statins, through the experiment (Response Surface methodology). Optimized niosomes were characterized in size, polydispersity index (PDI), entrapment efficiency (EE), stability, releasing pattern, and antimicrobial activity. The different molar ratio of surfactant and cholesterol were applied to prepare various formulation of simvastatin loaded niosome. Mean particle size and size distribution were analyzed by dynamic light scattering. Antibacterial activity was determined by MIC and MBC tests against Staphylococcus aureus and Escherichia coli. The release rate of simvastatin from noisome nanoparticles was studied by the Franz diffusion cell method. The release pattern was studied through zero order, first order, Higuchi, Korsmeyer-Peppas, and Hixson-Crowell kinetics models. Optimized niosomes were obtained by span 80, drug to cholesterol ratio of 0.4 with 7 min sonication time. Mean particle size, PDI, zeta potential, and entrapment efficiency (EE%) of optimized nSIM were obtained about 168 nm, 0.34, -32.40, and 96 %, respectively. The niosomes significantly decreased the drug's releasing rate and enhanced antibacterial activity against S. aureus and E. Coli. It was found that the release pattern of drug followed the Higuchi kinetic model which means drug release is by diffusion. Overall, our findings indicated that the prepared simvastatin loaded niosomes showed good stability and biological properties than free drug. Our study suggests that niosomal formulation could be considered as a promising strategy for the delivery of poor water-soluble drugs that enhance antibacterial activity.



中文翻译:

新型辛伐他汀纳米脂质体凝胶对大肠杆菌和金黄色葡萄球菌的优化、理化表征和抗菌活性

Niosomes作为一种药物递送系统,广泛用于亲脂性药物的局部递送。niosomes 的优化在提高其治疗效率方面起着至关重要的作用。本研究旨在通过实验(响应面方法)制备优化的他汀类亲脂性成员辛伐他汀 (nSIM) 的 niosomal 配方。优化后的 niosomes 具有大小、多分散性指数 (PDI)、截留效率 (EE)、稳定性、释放模式和抗菌活性的特征。应用不同摩尔比的表面活性剂和胆固醇制备了多种负载辛伐他汀的niosome制剂。通过动态光散射分析平均粒度和粒度分布。抗菌活性由 MIC 和 MBC 测试确定金黄色葡萄球菌大肠杆菌。通过弗朗兹扩散池法研究了辛伐他汀从噪声性纳米颗粒中的释放速率。通过零级、一级、Higuchi、Korsmeyer-Peppas 和 Hixson-Crowell 动力学模型研究释放模式。通过跨度 80、药物与胆固醇比率为 0.4、超声处理时间为 7 分钟获得优化的 niosome。优化后的 nSIM 的平均粒径、PDI、zeta 电位和截留效率 (EE%) 分别约为 168 nm、0.34、-32.40 和 96%。niosomes 显着降低了药物的释放速率并增强了对金黄色葡萄球菌大肠杆菌的抗菌活性发现药物的释放模式遵循 Higuchi 动力学模型,这意味着药物释放是通过扩散。总的来说,我们的研究结果表明,所制备的辛伐他汀负载的 niosome 比游离药物显示出良好的稳定性和生物学特性。我们的研究表明,niosomal 制剂可以被视为一种有前途的策略,用于递送增强抗菌活性的水溶性差的药物。

更新日期:2020-12-08
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