Nature子刊:在肠腔内形成屏障的生物材料

在硫糖铝的基础上研发出一种口服物质LuCI(肠腔覆盖物);
LuCI干粉加水后可形成糊剂,灌胃后1小时内可在大鼠的胃、十二指肠和小肠中形成覆盖层,持续数小时,且该过程可逆;
LuCI有良好的消化道粘膜相容性,给大鼠连续6天灌胃LuCI,未对肠道结构产生明显影响,也未引发腹泻和减重;
大鼠口服LuCI后可减少后续的葡萄糖等营养物质吸收,或能用于改善糖尿病;
LuCI还可作为给药载体,保护口服的蛋白质药物免于被消化液降解。
延伸阅读
Nature Materials [IF:39.235]

Therapeutic luminal coating of the intestine

治疗性肠腔覆盖层

2018-06-11, Article, 10.1038/s41563-018-0106-5more

Abstract:
The gastrointestinal tract is the site of most drug delivery and therapeutic interventions for the management and treatment of numerous diseases. However, selective access to its mucosa, especially in the small bowel, is challenging. Here we develop an orally administered gut-coating formulation that provides a transient coating of the bowel. Through a materials screening campaign, we identified a sucrose octasulfate aluminium complex and further engineered the pH-dependent material into a complex coacervate formulation linked via pH-independent electrostatic interaction, which allowed an effective transient physical coating on the gastrointestinal mucosa, independent of gastric acid exposure. We tested the therapeutic values of this technology in two settings. Oral administration of this gut-coating formulation modulated the nutrient contact with bowel mucosa, which lowered the glucose responses in rodent models indicating a potential therapeutic utility in diabetes. Furthermore, the formulation protected biological agents from gastric acid exposure and degradation, which enabled oral delivery to the small bowel mucosa.

First Authors:
Yuhan Lee

Correspondence Authors:
Yuhan Lee,Ali Tavakkoli,Jeffrey M Karp

All Authors:
Yuhan Lee,Tara E Deelman,Keyue Chen,Dawn S Y Lin,Ali Tavakkoli,Jeffrey M Karp