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淋巴向的CUR-NLCs递送增强了口服生物可用性:来自双导管老鼠模型的证据

Haoming Chi¹, Xiaorui Zhang^1,2, Zhiyuan Chen¹

¹Fujian Key Laboratory of Traditional Chinese Veterinary Medicine and Animal Health, College of Animal Sciences, Fujian Agriculture and Forestry University, Fuzhou 350002, China.

|November 27, 2025

概括

含有黄素的纳米结构脂质载体 (CUR-NLCs) 通过利用肠道淋巴运输显著增强口服吸收. 这种方法提供了一个有前途的策略,用于输送像黄素这样的溶解不良药物.

科学领域:

药理学和药物输送药理学和药物输送
纳米技术在医学中的应用
胃肠道吸收机制胃肠道吸收机制

背景情况:

黄素 (CUR) 由于溶解度低和广泛的第一通代谢,具有较差的口服生物利用性.
载有CUR的纳米结构脂质载体 (CUR-NLCs) 显示出改善口服吸收的潜力,但淋巴运输机制需要直接证据.
目前对CUR-NLCs口服吸收的理解主要基于间接证据.

研究的目的:

直接调查CUR-NLCs的肠道淋巴运输机制.
评估CUR-NLCs的药理动力学益处,与口服后的自由CUR相比.
提供通过淋巴运输介导的增强口服生物利用性的直接证据.

主要方法:

合成了CUR-NLC并对其物理化学性质进行了表征 (大小,泽塔潜力,EE,DL,稳定性,释放).
用一个带有中腔淋巴管-状静脉分流的老鼠模型来收集淋巴和评估药物运输.
使用传输电子显微镜 (TEM) 可视化细胞吸收和胆米克朗形成.

主要成果:

CUR-NLCs表现出有利的物理化学特性 (117.28 nm大小,99.99% EE,1.73% DL) 与持续释放.
口服CUR-NLCs导致相对生物利用率增加5.13倍,Cmax增加5.25倍,与自由CUR相比.
在CUR-NLC给药后,黄素仅在淋巴中检测到,这证实了淋巴运输,并得到了米克龙的TEM发现的支持.

结论:

通过直接的肠道淋巴吸收,CUR-NLCs有效地提高了口服生物可用性.
这项研究为CUR-NLCs的淋巴运输途径提供了直接证据.
CUR-NLCs代表了一种可行的策略,用于改善可溶性差的疏水性药物的口服输送.

关键词:

库尔库明是一种黄素.淋巴运输是指淋巴运输的过程.纳米结构的脂质载体 (NLCs)口服生物可用性口服生物可用性药物动力学药物动力学

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