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将芝麻酚负载固体脂质纳米粒递送至大脑治疗与绝经相关的情绪和认知性中枢神经系统紊乱。

Delivery of sesamol-loaded solid lipid nanoparticles to the brain for menopause-related emotional and cognitive central nervous system derangements.

机构信息

Department of Pharmaceutics, University Institute of Pharmaceutical Sciences, Panjab University, Chandigarh, India.

出版信息

Rejuvenation Res. 2011 Dec;14(6):597-604. doi: 10.1089/rej.2011.1193. Epub 2011 Oct 6.

Abstract

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.

摘要

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。

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