用TPGS修改的基酸脂质体的制造和表征及其在老鼠中的生物可用性
Jian-Jun Zhang1, Qiu-Shui Luo1, Qing-Qing Li1
1College of Food Science and Engineer, Jiangxi Agricultural University Nanchang 330045 China 396802874@qq.com 809472384@qq.com.
RSC advances
|August 14, 2024
概括
这项研究开发了TPGS修饰的脂质体,以改善酸 (CGA) 的稳定性和生物可用性. 这种新型配方显著增强了大鼠的CGA口服吸收,为其更广泛的临床应用铺平了道路.
科学领域:
- 药理学 药理学是指药理学的学科.
- 材料科学 材料科学 材料科学
- 药物运输 药物运输 药物运输
背景情况:
- 酸 (CGA) 是一种多,具有多样化的生物活性,但由于不稳定性和低口服生物可用性,体内利用率不佳.
- 现有的局限性阻碍了CGA在临床环境中的全部治疗潜力.
- 需要新的药物输送系统来克服CGA的药理动力学挑战.
研究的目的:
- 准备和表征含有基酸的TPGS修饰脂质体 (CGA-TPGS-LP).
- 评估CGA-TPGS-LP在小鼠口服后的稳定性,持续释放性质和体内药理动力学.
- 评估TPGS修饰脂质体在增强CGA口服生物可用性方面的潜力.
主要方法:
- 使用薄膜分散和离子驱动方法进行CGA-TPGS-LP制造.
- 物理化学表征包括形态,加载和封装效率.
- 实验室稳定性和持续释放性研究在模拟的胃和肠液中.
- 在动物体内用UPLC-QTOF-MS和UPLC-QqQ-MS/MS进行大鼠的药理动力学分析.
主要成果:
- 均的,小的,球形的脂质体与莱西丁,胆固醇和TPGS成功地准备好.
- 实现了高负载 (11.21%) 和封装 (83.22%) 的效率;CGA在脂质体内保持稳定和无形.
- CGA-TPGS-LP表现出更好的稳定性和持续释放性质.
- 在老鼠中,口服药物显示CGA口服生物可用性增加了1.52倍.
- 确定了10种代谢物,其中3种主要代谢物具有较高的血度和较慢的降解速度.
结论:
- 用TPGS修饰的脂质体显著提高了酸的稳定性和口服生物可用性.
- 开发的CGA-TPGS-LP配方表现出有利的持续释放特性.
- 用TPGS修饰的脂质体代表了提高CGA临床适用性的有前途的战略.
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