口服脂质体封装金氏化物化合物K用于类风湿性关节炎治疗
Ziwei Li1, Songren Han1, Guilin Cui1
1School of Life Sciences, Jilin University, Changchun 130012, China.
International journal of pharmaceutics
|July 19, 2023
概括
用叶酸 (FA-LP-GCK) 增强的金色化物化合物K (GCK) 脂质体,显示出治疗类风湿性关节炎 (RA) 的前景. 这种有针对性的交付系统改善了GCK.
科学领域:
- 药理学和药物输送 药理学和药物输送
- 免疫学 免疫学 免疫学
- 类风湿病学 类风湿病学
背景情况:
- 金色化物化合物K (GCK) 具有免疫和抗炎性质,对类风湿性关节炎 (RA) 有益.
- GCK的治疗潜力受到溶解性差,肠道透性低和P-葡萄糖蛋白排泄的阻碍.
- 需要新的药物输送系统来克服GCK的局限性,以有效治疗RA.
研究的目的:
- 开发一种针对GCK (FA-LP-GCK) 的叶酸向的脂质体药物递送系统.
- 评估FA-LP-GCK在RA治疗中的物理化学性质,稳定性和体外/体内疗效.
主要方法:
- 根据尺寸,结构和封装效率,FA-LP-GCK被准备和特征化.
- 在人工胃汁中评估了稳定性.
- 在体外研究中,使用激活的RAW 264.7细胞进行了细胞毒性和细胞吸收测定.
- 活体疗效在辅助性关节炎小鼠模型中进行了评估,评估关节胀和炎症标志物.
主要成果:
- FA-LP-GCK 呈现出均的大小 (249.13 nm),球形结构和高封装效率 (93.33%).
- 该系统在模拟的胃条件下表现出良好的稳定性.
- 与单独使用GCK相比,FA-LP-GCK在激活的巨细胞中显示出增强的细胞毒性和细胞吸收.
- 在体内,FA-LP-GCK显著降低了关节胀,促炎性细胞因子表达和辅助性关节炎大鼠的病理变化.
结论:
- FA-LP-GCK代表了一种有希望的有针对性的输送系统,用于提高GCK在RA中的治疗疗效.
- 开发的脂质体系统克服了GCK的药理动力学限制,为类风湿性关节炎提供了潜在的新治疗策略.
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