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疏水性药物颗粒在体外胃肠液中采用复杂的生物分子冠状

Anas Aljabbari¹, Shinji Kihara¹, Thomas Thymann²

¹Department of Pharmacy, Faculty of Health and Medical Sciences, University of Copenhagen, Universitetsparken 2, 2100 Copenhagen Ø, Denmark.

Journal of controlled release : official journal of the Controlled Release Society

|October 24, 2025

概括

药物颗粒上的胃肠 (GI) 生物分子冠状体取决于药物的特性和位于胃肠道内的位置. 肠液蛋白质主导着冠状体,影响药物行为.

科学领域:

制药科学制药科学
生物材料科学生物材料科学
蛋白质组学是指蛋白质组学.

背景情况:

血液粒子界面上的生物分子冠状体得到了很好的研究.
在摄入药物颗粒上的胃肠道 (GI) 生物分子冠状体是最近的一个研究重点.
了解这种冠状病毒对于药物配方和预测体内行为至关重要.

研究的目的:

为了研究药物颗粒上GI生物分子冠状的组成.
为了确定药物身份和固态形式对冠状形成的影响.
分析不同 ex vivo 猪肠道液体 (胃,肠道,结肠) 中的冠状形成.

主要方法:

使用了猪的胃,肠和结肠液体 (PGF,PIF,PCF).
采用液体染色学-并联质谱学 (LC-MS/MS) 蛋白质组学.
研究的克洛特里马 (CMZ),里托纳维尔 (RTV) 和印梅他辛 (IND) 颗粒,包括无形和晶体形式.

主要成果:

胃肠道冠状元的组成是分区特定的,PGF显示了最多的蛋白质.
PIF冠状很快达到平衡,并且独立于时间.
连续暴露表明PIF蛋白质在冠状病毒中占主导地位,无论之前的暴露情况如何.
在药物 (CMZ,RTV与IND) 和IND固态形式 (无形与晶体) 之间,冠状病毒的组成有所不同.
无形IND形成了比晶体IND更多样化的冠状.

结论:

药物颗粒的身份和固态形式显著影响肠道液体中的生物分子冠状体组成.
肠液中的蛋白质在冠状体中起着主导作用,特别是在连续暴露后.
这些发现为设计针对胃肠道的药物输送系统提供了关键的见解.

关键词:

生物分子冠状病毒药物颗粒的药物颗粒在胃肠道上,胃肠道.蛋白质吸附蛋白质的吸附.蛋白质组学蛋白质组学

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