在2型糖尿病治疗中,用于口服输送异构素B的工程微贴片
Yi Chen1, Yuanxing Huang2, Cheneryu Huang3
1State Key Laboratory of Discovery and Utilization of Functional Components in Traditional Chinese Medicine & School of Pharmaceutical Sciences, Guizhou Medical University, Guiyang 561113, China; Guizhou Provincial Key Laboratory of Innovation and Manufacturing for Pharmaceuticals, Guizhou Provincial Engineering Technology Research Center for Chemical Drug R&D, Guizhou Medical University, Guiyang 561113, China.
概括
乙烯基素B通过改善肝脏信号和新陈代谢,有效治疗2型糖尿病. 一种新的口服输送系统提高了其生物可用性和治疗效果,在小鼠模型中表现优于甲福林.
科学领域:
- 药理学和药物输送 药理学和药物输送
- 代谢疾病 代谢疾病
- 生物化学 生物化学
背景情况:
- 2型糖尿病 (T2DM) 是一个全球性的健康问题,需要新的治疗方法.
- 环状的Heterophyllin B (HB) 显示了T2DM治疗的潜力.
- 乙型肝炎的治疗用途受到溶解性差,口服生物可用性低以及P-glycoprotein (P-gp) 排泄的限制.
研究的目的:
- 开发一种有效的口服输送系统,用于乙烯基氨酸B (HB).
- 提高HB的生物可用性和治疗T2DM的疗效.
- 研究HB的抗糖尿病机制及其传递系统.
主要方法:
- 开发了一种针对肝脏的口服输送系统:HB被封装在一个由N-甲基胺 (GalNAc) 修改的支柱[6]arene (P6) 中,在一个粘粘性介聚合物复合物 (IPC) 微补丁 (HBP6-GalNAc/IPC) 中.
- 通过肠道囊进行口服的配方.
- 评估了HB吸收,生物可用性和治疗效果在高脂肪饮食/高脂肪饮食/高脂肪饮食/高脂肪饮食/高脂肪饮食/高脂肪饮食/高脂肪饮食/高脂肪饮食/高脂肪饮食/高脂肪饮食/高脂肪饮食/高脂肪饮食/高脂肪饮食/高脂肪饮食/高脂肪饮食/高脂肪饮食/高脂肪饮食/高脂肪饮食/高脂肪饮食/高脂肪饮食/高脂肪饮食/高脂肪饮食/高脂肪饮食.
主要成果:
- 通过增强肠道吸收,HBP6-GalNAc/IPC配方实现了66.31%的口服生物可用性,是自由HB的3.3倍.
- 机制包括可逆紧接口开放,P-gp流量抑制和克拉斯林/洞穴介导的内细胞分裂.
- 该配方显著改善了T2DM小鼠的血糖控制,胰岛素敏感性,脂质新陈代谢,减少了肝硬化,并保护了胰腺和脏,表现优于甲福林.
结论:
- 这种新的口服输送系统克服了HB的局限性,使得有效的T2DM治疗成为可能.
- 通过调节肝脏的IRS2/PI3K-Akt/FoxO1信号传递和恢复代谢途径,HB可以缓解T2DM.
- 这一策略为口服输送基于的治疗方法提供了一种有前途的方法.
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