布鲁西亚 javanica-衍生的天然脂质滴:选择性口腔淋巴细胞向和内细胞运输机制
Xiaofeng Guo1, Shuni Zeng1, Qiwei Chen1
1School of Pharmaceutical Sciences, Guangzhou University of Chinese Medicine, No. 232, Waihuan East Road, Guangzhou 510006, China.
Pharmaceutics
|February 27, 2026
概括
来自Brucea javanica油 (BJO) 的植物性脂质液滴增强了口服药物输送. 这些Brucea javanica脂液滴 (BJLDs) 提高了生物可用性,并在口服后达到80%以上的淋巴向.
科学领域:
- 药理学 药理学是指药理学的学科.
- 生物技术是生物技术.
- 药物输送系统 药物输送系统
背景情况:
- 由于氧化不稳定性和第一通代谢,Brucea javanica油 (BJO) 的口服生物利用性较差.
- 开发BJO有效的口服配方对于治疗应用至关重要.
研究的目的:
- 为BJO开发一种新的,无溶剂的药物递送系统,使用内源性脂质滴.
- 为了评估BJO在脂质滴中封装的稳定性,释放动力学,细胞吸收和淋巴运输.
主要方法:
- 一步式的,无溶剂的 Brucea javanica 脂质滴 (BJLD) 的分离.
- 在体外消化研究以评估脂肪酸释放动力学.
- 卡科-2细胞运输试验以确定吸收机制和P-葡萄糖蛋白 (P-gp) 抑制.
- 鼠标模型研究量化肠道淋巴运输和药物动力学参数.
- 液体染色学-双重质谱学 (LC-MS/MS) 来确认药物保留.
主要成果:
- BJLDs表现出均的大小分布和增强的氧化稳定性.
- 在体外消化过程中,通过一阶动力学,在4小时内释放出80%的长链脂肪酸.
- 卡科-2研究表明,卡韦林依赖性内细胞分裂和显著的P-gp抑制 (药物积累增加2.3倍).
- 在大鼠模型中,淋巴运输率达到89.73%,可延长血半衰期 (t1/2) 和酸的平均停留时间 (MRT).
- LC-MS/MS证实了BJLDs中的布鲁萨托尔和布鲁赛因的完整性.
结论:
- 微米大小的植物性脂质液滴作为一个有效的"药物载体"系统,用于口服.
- BJLDs显著提高口服生物可用性,并实现高淋巴向性 (>80%).
- 这种方法为传统BJO配方提供了一种绿色,可扩展和稳定的替代方案.
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