疏水性离子配对:通过双价离子介导的复合物形成来提高离子大分子的脂性
Sera Lindner1, Fabrizio Ricci1, René Holm2
1Thiomatrix Forschungs- Und Beratungs GmbH, Trientlgasse 65, 6020, Innsbruck, Austria.
Drug delivery and translational research
|December 17, 2024
概括
这项研究开发了一种新的方法,使用双价离子和离子表面活性剂来增加阴离子大分子 (MMs) 的脂性. 这种方法提高了口服药物输送的溶解度,没有有毒的对抗作用.
科学领域:
- 制药科学 制药科学
- 药物运输 药物运输 药物运输
- 材料科学 材料科学 材料科学
背景情况:
- 阴性宏分子 (MMs) 经常表现出不良的脂性,阻碍了口服药物输送.
- 增强脂友性的常规方法可能涉及有毒的阴离子对应物.
- 开发更安全的替代品来增强脂性对口服生物可用性至关重要.
研究的目的:
- 开发一种替代策略来增加阴性MMs的脂性.
- 为了避免使用潜在的有毒的阴离子对应物.
- 创建稳定的自我乳化药物输送系统 (SEDDS),以加强口服输送.
主要方法:
- 阳离子MMs (沙,胰岛素,聚-L-胺酸) 与阳离子表面活性剂 (酸,SDS,SS,SOS) 的离子配对.
- 由双价离子 (Mg2+,Ca2+,Zn2+) 介导的复合形成.
- 评估复杂的降水,脂友性 (logD),SEDDS配方,有效载荷和稳定性.
主要成果:
- 实现了高沉效率 (>90%),特别是使用Zn2+介导的复合物.
- 对于埃诺沙巴林,胰岛素和PLG复合物,观察到脂友性 (logD) 的显著增加.
- 开发的SEDDS显示了小液滴大小 (<200 nm) 和高有效载荷 (高达18.72 mg/ml).
结论:
- 阴离子MMs与阴离子表面活性剂的二元阴离子介导复合是一种可行的策略,以增强脂友性.
- 这种方法为口服药物递送应用提供了一个比传统的counterterions更安全的替代方案.
- 开发的SEDDS配方显示出有望提高离子MMs的口服生物可用性.
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