草多糖的自组装纳米输送系统:对黄素生物可用性和分子机制的影响
Qiongdan Hu1, Xinxing Tang1, Rui Long1
1State Key Laboratory of Southwestern Chinese Medicine Resources, School of Pharmacy, Chengdu University of Traditional Chinese Medicine, Chengdu 610075, PR China.
International journal of biological macromolecules
|December 4, 2024
概括
公多糖化物FS60通过形成聚合物来提高黄素的生物可用性,从而改善吸收,并在大鼠中显著增加黄素葡萄糖化物水平. 这种自然的输送系统优化了黄素.
科学领域:
- 药理学和药物输送 药理学和药物输送
- 自然产品化学 自然产品化学
- 胃肠道生理学 胃肠道生理学
背景情况:
- 黄素 (Cur) 具有较差的水溶性和较低的生物利用性.
- 公多糖化物FS60显示了改善黄素分散的潜力.
- 在体内评估FS60-curcuminoid的输送对于了解其有效性至关重要.
研究的目的:
- 为了优化FS60-curcuminoid聚合物 (FC) 的配方.
- 评估FC对大鼠库尔库明药理学上的影响.
- 阐明 FS60 介导的黄素生物可用性增强背后的机制.
主要方法:
- 优化FS60-curcuminoid聚合物的配方参数.
- 在老鼠中进行的药理动力学研究,以评估黄素及其代谢物.
- 对黄糖化物 (Cur-O-Glu) 水平,Cmax和AUC0-12h的分析.
- 调查FS60对UGT表达,肠细胞输送体和肠道微生物群的影响.
主要成果:
- 优化FC表现出高封装效率 (88.22%) 和231.48nm的液态动力直径.
- FC的使用显著增加了Cur-O-Glu水平,Cmax是单独的黄素的51倍,AUC0-12h是单独的黄素的19倍.
- FS60干预增强了Cur-O-Glu的吸收速度,并促进了黄素的摄入.
- FS60调节肠道微生物群,以促进黄素的葡萄糖化.
结论:
- FS60-curcuminoid纳米输送系统显著提高了黄素在体内生物可用性.
- 通过多种机制,FS60促进了胃肠道黄素的葡萄糖化和Cur-O-Glu的吸收.
- 这种方法为提高黄素的治疗潜力提供了一个有希望的策略.
相关概念视频
Factors Affecting Dissolution: Particle Size and Effective Surface Area
727
Dissolution kinetics, an essential aspect of oral drug delivery, is significantly influenced by the drug's particle size. According to the Noyes-Whitney dissolution model, the dissolution rate correlates directly with the drug's surface area. The larger the surface area, the higher the drug's solubility in water, leading to a faster drug dissolution rate. Reducing particle size increases the effective surface area, enhancing the dissolution process. Micronization and nanosizing are...
727
Factors Affecting Dissolution: Drug Permeability, Stability and Stereochemistry
174
Orally administered drugs primarily enter the systemic circulation via passive diffusion through the intestinal membranes. The drug's absorption is influenced by drug stability in the gastrointestinal GI tract, membrane permeability, the surface area available for absorption, luminal drug concentration, and residence time in the lumen. Drug permeability can be enhanced by adjusting the lipophilicity, polarity, or molecular size of the drug, promoting its passive transport across intestinal...
174


