作为改善生物可用性的超分子载体的支柱[n]与环氧:Idebenone作为模型药物
Dina Yeffet1, Boris Smolkin2, Ishay Columbus2
1Department of Organic Chemistry, Israel Institute for Biological Research, Ness-Ziona 74100, Israel; School of Chemistry, Tel Aviv University, Ramat Aviv 69978, Tel Aviv, Israel.
水溶性柱状 (PA) 有效复合Idebenone (IDE),具有不同的结合强度. 这些复合物根据溶液和不同影响药物透性,提供了新的生物可用性增强策略.
科学领域:
- 超分子化学
- 制药科学
- 药物输送系统
背景情况:
- 循环素 (CD) 广泛用于提高药物的生物可用性.
- 伊德本 (IDE) 是一种具有潜在治疗应用的示范药物.
- 了解药物溶解剂相互作用对于药物配方至关重要.
研究的目的:
- 评估水溶性柱状 (PAs) 的复合和溶解Idebenone (IDE).
- 为了比较PAs和循环素 (CDs) 与IDE的结合亲和力.
- 研究IDE-PA复合物对药物的透性和生物可用性的影响.
主要方法:
- 水溶性柱状的合成和表征.
- 使用结合常数对PAs和CDs进行IDE复杂化研究.
- 使用血脑屏障 (BBB) 模型和口服透气®模型进行体外透气性测试.
主要成果:
- 皮拉拉伦P[5]与IDE结合的强度明显超过了环极的结合.
- 皮拉拉伦P[6]对IDE的结合最弱,结合常数差两倍以上.
- 观察到溶解性- 透性的相互作用:较弱的复合物增强了不和溶液的透性,而较强的复合物则改善了和溶液的透性.
结论:
- 在改善药物的生物可用性方面,水溶性柱状是一种有前途的替代品.
- 可以优化柱烯结构和溶液条件的选择,以调节药物的溶解性和透性.
- 皮拉拉伦 - 伊德本复合物为增强药物输送应用提供可调节的特性.
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