通过抑制P-glycoprotein流量来提高氨酸的生物可用性:一种自我微乳化药物输送系统
Yimei Zheng1, Boyu Chen2, Xuanxiang Huang2
1College of Food Science and Technology, Guangdong Ocean University, Guangdong Provincial Key Laboratory of Aquatic Product Processing and Safety, Guangdong Province Engineering Laboratory for Marine Biological Products, Guangdong Provincial Engineering Technology Research Center of Seafood, Key Laboratory of Advanced Processing of Aquatic Product of Guangdong Higher Education Institution, Zhanjiang 524088, China; College of Food Science, Fujian Agriculture and Forestry University, Fuzhou, Fujian 350002, China; Fujian Province-Indonesia Marine Food Joint Research and Development Center, Fujian Polytechnic Normal University, Fuqing, Fujian 350300, China.
这项研究开发了一种新的药物输送系统,以改善黄素.
科学领域:
- 纳米技术纳米技术
- 药理学 药理学是指药理学的学科.
- 生物化学 生物化学
背景情况:
- 素是一种具有抗氧化和抗炎性质的黄类化合物,由于溶解度低和P-glycoprotein (P-gp) 排泄,其口服生物可用性较差.
- 这些局限性阻碍了其在炎症条件下治疗的应用.
研究的目的:
- 为了提高白素的口服生物可用性和治疗疗效.
- 为了克服吸收障碍,使用功能性自我微乳化药物递送系统 (SME) 结合D-α-托科菲尔聚乙烯甘1000酸盐 (TPGS).
主要方法:
- 基于TPGS的素-SME的制备和表征.
- 使用Caco-2细胞评估细胞吸收,透性和P-gp抑制.
- 在炎症模型中评估药理动力学,大鼠中的生物分布和治疗疗效.
主要成果:
- 优化的白素-SME形成了稳定的纳米滴 (<50 nm) 与增强释放.
- 显著改善细胞吸收,透性和P-gp抑制.
- 口服生物可用性增加了29倍,体内有强烈的抗炎作用.
结论:
- 通过增强溶解和P-gp抑制,TPGS功能化的SME成功克服了白素的吸收障碍.
- 这种方法产生了前所未有的生物可用性和疗效,建立了一个有前途的输送平台为luteolin.
- 开发的系统提供了一种实际的策略,用于增强与炎症有关的疾病的口服治疗.
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