a Department of Life Science Engineering, Faculty of New Science and Technology , University of Tehran , Tehran , Iran.
b Department of Biomedical Engineering, Faculty of Chemical Engineering , Tarbiat Modares University , Tehran , Iran.
J Liposome Res. 2018 Sep;28(3):226-235. doi: 10.1080/08982104.2017.1349143. Epub 2017 Jul 19.
Rivastigmine hydrogen tartrate (RHT) is a pseudo-irreversible inhibitor of cholinesterase and is used for the treatment of Alzheimer's. However, RHT delivery to the brain is limited by the blood-brain barrier (BBB). The purpose of this study was to improve the brain-targeting delivery of RHT by producing and optimizing rivastigmine hydrogen tartrate-loaded tocopherol succinate-based solid lipid nanoparticles (RHT-SLNs). RHT-SLNs were prepared using the microemulsion technique. The impact of significant variables, such as surfactant concentration and drug/lipid ratio, on the size of RHT-SLNs and their drug loading and encapsulation efficiency was analysed using a five-level central composite design (CCD). The minimum size of particles and the maximum efficiency of loading and encapsulation were defined according to models derived from a statistical analysis performed under optimal predicted conditions. The experimental results of optimized RHT-SLNs showed an appropriate particle size of 15.6 nm, 72.4% drug encapsulation efficiency and 6.8% loading efficiency, which revealed a good correlation between the experimental and predicted values. Furthermore, in vitro release studies showed a sustained release of RHT from RHT-SLNs.
酒石酸氢瑞波西汀（RHT）是一种假性不可逆的乙酰胆碱酯酶抑制剂，用于治疗阿尔茨海默病。然而，由于血脑屏障（BBB）的存在，RHT 向脑部的递送受到限制。本研究旨在通过制备和优化载有酒石酸氢瑞波西汀的生育酚琥珀酸酯固体脂质纳米粒（RHT-SLNs）来提高 RHT 的脑靶向递送。RHT-SLNs 采用微乳液技术制备。采用五水平中心组合设计（CCD）分析了表面活性剂浓度和药物/脂质比等显著变量对 RHT-SLNs 粒径及其药物载药量和包封效率的影响。根据在最佳预测条件下进行的统计分析得出的模型，定义了最小粒径和最大载药量和包封效率。优化后的 RHT-SLNs 的实验结果显示，适当的粒径为 15.6nm，药物包封效率为 72.4%，载药量为 6.8%，这表明实验值与预测值之间具有良好的相关性。此外，体外释放研究表明 RHT-SLNs 具有持续释放 RHT 的能力。
