基于透增强剂的离子凝在口服胰岛素输送方面表现出了显著的潜力
Konstantinos Raptis1,2, Joanne Heade1,2, Cristiana Cunha1,2
1Department of Pharmacy, Faculty of Health and Medical Sciences, University of Copenhagen, Universitetsparken 2, Copenhagen, 2100, Denmark.
Advanced healthcare materials
|June 10, 2025
概括
一种新的胆二甲酸盐离子液体 (IL) 配方显著提高了口服胰岛素的生物可用性. 这种递送系统显示持续的吸收和最小的肠损伤,为目前的方法提供了一个有希望的替代方案.
科学领域:
- 制药科学 制药科学
- 生物材料科学 生物材料科学
- 药物输送系统 药物输送系统
背景情况:
- 口服治疗药物由于吸收不良和酶降解而面临挑战.
- 使用酸等透增强剂,但它们的疗效和安全性需要改进.
- 离子液体 (ILs) 显示出增强药物吸收的潜力.
研究的目的:
- 开发和评估一种基于decanoate的离子液体 (IL) 用于口服胰岛素的输送.
- 为了研究新型IL配方的物理化学特性和体内性能.
- 与现有的增强剂相比,评估IL的安全性和有效性.
主要方法:
- 一种基于胆二甲酸盐的离子液体 (chC10 1:2) 与胰岛素加载的配方.
- 在体外鉴定质性质和溶解的特征.
- 在体内评估口服胰岛素的生物可用性和药理动力学概况.
- 管理后肠形态的组织学检查.
主要成果:
- 优化的chC10 1:2配方表现出具有高粘度和疏水性的凝状特性,导致体外溶解速度缓慢.
- 在体内研究表明,与胆甲酸盐 (CAGE) 和甲酸盐相比,口服胰岛素的生物可用性分别增加了7倍和13倍 (6.5%与0.9%和0.5%相比).
- 组织学分析显示,chC10:1:2对小形态没有不良影响,与CAGE不同,导致小高度显著减少.
结论:
- 开发的基于decanoate的离子液体 (chC10 1:2) 是一种有希望的胰岛素口服药物输送载体.
- 这种IL配方与CAGE和酸相比,提供了卓越的生物可用性增强和改善的安全性.
- 对口服输送IL的进一步研究是有必要的.
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