Department of Pharmaceutics, University Institute of Pharmaceutical Sciences, Panjab University, Chandigarh, India.
Rejuvenation Res. 2011 Dec;14(6):597-604. doi: 10.1089/rej.2011.1193. Epub 2011 Oct 6.
The physicochemical nature of sesamol (logP 1.29; solubility 38.8 mg/mL) substantially enhances its tissue distribution, minimizing its brain delivery. Sesamol-loaded solid lipid nanoparticles (S-SLNs) with an average particle size of 122 nm and an entrapment efficiency of 75.9 ± 2.91% were developed. Biochemical and behavioral paradigms clearly established the superiority of orally administered S-SLNs. The same was confirmed evidently by scintigraphic images of rabbits administered radiolabeled SLNs and confocal microscopy of brain sections of rats administered similarly prepared SLNs with a fluorescent marker. This study indicates the special importance of using phosphatidylcholine (as co-surfactant) in the preparation of SLNs for improving memory deficits. The aim of the present work was to develop sesamol as a therapeutic agent for central nervous system derangements.
芝麻酚（logP1.29；溶解度 38.8mg/mL）的物理化学性质极大地增强了其组织分布，最大限度地减少了其向大脑的传递。开发了平均粒径为 122nm 和包封效率为 75.9±2.91%的芝麻酚负载固体脂质纳米粒（S-SLNs）。生化和行为范式清楚地确立了口服 S-SLNs 的优越性。同样，通过给兔子施用放射性标记的 SLNs 的闪烁成像和通过给用荧光标记类似制备的 SLNs 处理的大鼠的脑切片的共聚焦显微镜，明显证实了这一点。这项研究表明，在制备 SLNs 时使用磷脂酰胆碱（作为助表面活性剂）对于改善记忆缺陷具有特殊的重要性。本工作的目的是将芝麻酚开发为治疗中枢神经系统紊乱的药物。
