印度甲与在现场形成难以捉摸的纳米颗粒,导致生物模拟屏障的增强透
Mikkel Højmark Tønning1, Annette Bauer-Brandl1, Martin Brandl1
1Department of Physics, Chemistry & Pharmacy, University of Southern Denmark, Odense, Denmark.
International journal of pharmaceutics
|September 7, 2025
概括
在2nm以下,新发现的印梅他辛盐纳米颗粒在特定的缓冲区中形成. 这些难以捉摸的纳米颗粒增强了药物穿透生物模拟屏障,提高了生物可用性.
科学领域:
- 制药科学 制药科学
- 物理化学 物理化学
- 生物材料科学 生物材料科学
背景情况:
- 印米他辛是一种难溶的弱酸,是配方开发的典范药物.
- 使用过的常规溶解性研究可能会错过关键的纳米粒子形成.
- 微透析采样揭示了以前未被检测到的印梅他辛盐纳米颗粒.
研究的目的:
- 为了研究纳米颗粒在印梅他辛配方分析过程中的形成和影响.
- 了解缓冲组合和分子相互作用在纳米粒子形成中的作用.
- 评估这些纳米颗粒对药物穿透通过生物模拟屏障的影响.
主要方法:
- 从含的缓冲剂中取微透析样本.
- 动态光散射 (DLS) 用于纳米粒子尺寸的确定.
- 分子动力学模拟用于研究药物缓冲区相互作用.
- 通过生物模拟屏障进行透研究 (Permeapad®).
主要成果:
- 在tris-maleate缓冲体中形成水溶性较差的印梅他辛盐纳米颗粒 (<2 nm).
- 纳米颗粒的形成与强烈的印米他辛与tris和maleate的相互作用有关.
- 在Permeapad®中观察到印米他辛透的显著增强.
- 微透析采样排除了体药物结构,与过不同.
结论:
- 三酸缓冲和离子可以诱导超小的印美纳米颗粒的形成.
- 这些纳米颗粒可以意外地增强药物透,这可能解释体内生物可用性.
- 微透析对于检测这些纳米颗粒和了解脂解中的药物释放动态至关重要.
- 结合采样方法揭示了自由和合相关药物之间的相互作用.
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