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增强奎尔素的潜力:用于高海拔肺的纳米脂质体输送系统

Lin Lin^1,2, Baoying Shen^1,2, Jialu Cui^1,2

¹Institute of Traditional Chinese Medicine, Tianjin University of Traditional Chinese Medicine, Tianjin, People's Republic of China.

Drug design, development and therapy

|October 14, 2025

概括

夸斯丁载荷纳米脂质体 (QUL) 增强夸斯丁.

科学领域:

药理学和纳米技术的应用
呼吸系统医学呼吸系统医学
分子生物学分子生物学

背景情况:

奎尔 (QU) 具有预防高海拔肺 (HAPE) 的潜力,但其低口服生物可用性限制了治疗疗效.
开发新的药物输送系统对于提高奎尔丁的生物可用性和HAPE治疗结果至关重要.

研究的目的:

开发氨酸载荷纳米脂质体 (QUL),以提高氨酸 (QU) 的口服生物可用性.
评估 QU 和 QUL 在预防 HAPE 的有效性,并阐明底层的分子机制.

主要方法:

使用薄膜水化方法制备了奎尔胺纳米体 (QUL).
描述包括形态学,颗粒大小,多分散性指数,药物加载和体外释放研究.
开发了一种LC-MS/MS方法,用于量化大鼠血中的QU和QUL;在小鼠HAPE模型中进行了体外和体内疗效研究,以及用于机械分析的西部斑点和免疫光.

主要成果:

QUL表现出最佳的纳米粒子特性 (157.08±1.215 nm大小,0.204±0.012 PDI) 和增强的QU吸收 (Tmax: 1.167±0.408h,Cmax: 0.585±0.032ug/mL).
在小鼠HAPE模型中,QU和QUL都改善了肺透性,降低了死亡率,并降低了肺水含量.
机理学研究显示,通过PI3K/AKT/VEGF和ROCK/HIF/TRPC信号通路抑制低氧诱导的肺动脉平滑肌细胞增殖和迁移.

结论:

奎尔素通过调节关键信号通路来有效降低肺部含水量,这表明其对HAPE的治疗潜力.
克韦尔含有克韦尔的纳米脂酶显著提高了克韦尔的口服生物可用性,从而提高了其在管理HAPE.APE方面的治疗效果.

关键词:

高海拔地区的肺胀.在 nanoliposome 中.药物动力学药物动力学肺动脉平滑肌肉细胞肺动脉平滑肌肉细胞文素 (Quercetin) 是一种文素.

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