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.

胃肠道是用于治疗和治疗多种疾病的大多数药物输送和治疗干预措施的所在地。然而，选择性地进入其粘膜，特别是在小肠中，是具有挑战性的。在这里，我们开发了一种口服的肠溶衣配方，可提供肠的瞬时包衣。通过材料筛选活动，我们确定了蔗糖八硫酸铝复合物，并进一步将pH依赖型材料工程化为通过不依赖pH值的静电相互作用连接的复杂凝聚层配方，从而可以在胃肠道粘膜上有效地进行短暂的物理包被，而与胃酸无关接触。我们在两种情况下测试了该技术的治疗价值。口服这种肠溶衣配方可调节营养物质与肠粘膜的接触，从而降低啮齿动物模型中的葡萄糖反应，表明在糖尿病中具有潜在的治疗作用。此外，该制剂保护生物制剂免于胃酸暴露和降解，这使得能够口服递送至小肠粘膜。