Department of Pharmaceutics, Faculty of Pharmacy Cairo University, Cairo, Egypt.
Pharm Dev Technol. 2013 May-Jun;18(3):736-44. doi: 10.3109/10837450.2012.734513.
This study aims at formulating solid lipid nanoparticles (SLNs) of Vinpocetine (VIN) to be used as a brain targeted sustained drug-delivery system. VIN is a derivative of vincamine alkaloid, used for chronic cerebral vascular ischemia. However, it suffers from low bioavailability and short half-life. Its oral bioavailability is recorded to be between 7 and 55%. Its elimination half-life is 1-2 h so it would be a good candidate for a sustained drug-delivery system. VIN SLNs were prepared using modified high shear homogenization followed by ultrasonication technique. The effect of incorporating different lipids at different concentrations of various surfactants was investigated. The VIN SLNs were characterized by entrapment efficiency percent (EE%), particle size distribution, zeta-potential, and cumulative released percent after 96 h. The EE% ranged between 83.34% ± 0.95-94.56% ± 0.11 due to the lipophilic character of VIN. The mean particle size measured ranged from 123 nm-464 nm. The cumulative released percent after 96 h ranged from 23.55% to 75.67% showing a controlled release profile. Formula (F32) composed of 5% glyceryl monostearate (GMS) and stabilized by 2% surfactant mixture [Tween 80, Pluronic F 68 (1:1)] was the most appropriate formula for brain delivery having EE% of 89.09% ± 1.49, zero-order release kinetics with cumulative released percent of 72.12% after 96 h, zeta-potential of -11.3 ± 0.97 mV. It showed a unimodal size distribution with particle size ≈ 90 nm and polydispersity index of 0.121. The formula of choice in this study exhibited a zero-order sustained release profile and met the requirement for a brain targeted SLN so it could be a promising formula to deliver VIN to the brain.
本研究旨在将长春西汀（VIN）制成固体脂质纳米粒（SLN），用作脑靶向的持续药物递送系统。VIN 是长春胺生物碱的衍生物，用于慢性脑血管缺血。然而，它的生物利用度低，半衰期短。其口服生物利用度记录在 7%至 55%之间。其消除半衰期为 1-2 小时，因此它将是持续药物递送系统的良好候选物。VIN SLN 是通过改良的高剪切匀化随后进行超声处理技术制备的。研究了在不同浓度的各种表面活性剂中掺入不同脂质的效果。通过包封效率百分比（EE%）、粒径分布、Zeta 电位和 96 小时后的累积释放百分比来表征 VIN SLN。由于 VIN 的亲脂性，EE% 范围为 83.34%±0.95-94.56%±0.11。测量的平均粒径范围为 123nm-464nm。96 小时后的累积释放百分比范围为 23.55%-75.67%，显示出控制释放的特征。由 5%甘油单硬脂酸酯（GMS）组成并由 2%表面活性剂混合物[Tween 80、Pluronic F 68（1:1）]稳定的配方（F32）是用于脑递送的最合适配方，具有 89.09%±1.49 的 EE%，零级释放动力学，96 小时后的累积释放百分比为 72.12%，Zeta 电位为-11.3±0.97mV。它显示出单峰粒径分布，粒径约为 90nm，多分散指数为 0.121。本研究中选择的配方表现出零级持续释放的特征，符合脑靶向 SLN 的要求，因此它可能是将 VIN 递送到大脑的有前途的配方。
