糖酸脂质体封装的塞马格卢提德通过促进肠道吸收来增加口服生物可用性
Yehan Li1, Fei Liu1, Jiajing Che1
1Department of Pharmaceutics, School of Pharmacy, Shenyang Pharmaceutical University, Shenyang, 110016, China.
International journal of pharmaceutics
|September 7, 2024
概括
糖酸盐脂质体增强了西马格卢提德的作用.
科学领域:
- 药品制造 药品制造 药品制造
- 药物运输 药物运输 药物运输
- 生物化学 生物化学
背景情况:
- 塞马格卢提德是一种类似葡萄糖类-1受体激动剂,用于糖尿病治疗.
- 由于酶降解和吸收不良,像西马格卢提德这样的类药物的口服生物可用性通常很低.
- 脂质体是改善药物输送的有希望的载体,但它们的口服疗效需要提高.
研究的目的:
- 为了开发糖酸盐脂质体 (SGC-Lip) 封装半谷氨酸 (Sml).
- 为了增强塞马格卢提德的口服生物可用性和低血糖作用.
- 研究SGC-Lip的肠道吸收机制和口服安全性.
主要方法:
- 使用逆相蒸发方法制备了SGC-Lip封装的赛马格卢提德.
- 描述包括粒子大小,泽塔潜力,形态和稳定性评估.
- 低血糖和肠道吸收效应与大鼠中的含胆固醇脂质体 (CH-Lip) 进行了比较;通过细胞毒性试验评估了口服安全性.
主要成果:
- SGC-Lip表现出最佳的特征:大约140纳米大小,-27mV电位,圆形形态和良好的稳定性.
- SGC-Lip表现出显著的低血糖效应,在12小时内降低了40%的血糖.
- SGC-Lip的曲线下的面积 (AAC) 是CH-Lip的六倍,这表明通过ASBT介导的途径增强了semaglutide的吸收,特别是在大肠.
结论:
- SGC-Lip有效地改善了塞马格卢提德的口服生物可用性.
- 增强的吸收归因于糖酸盐对脂质体的稳定和透促进作用.
- SGC-Lip显示出良好的口腔安全性和改善糖尿病管理的潜力.
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