Therapeutic luminal coating of the intestine

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 tha...

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Veröffentlicht in:Nature materials 2018-09, Vol.17 (9), p.834-842
Hauptverfasser: Lee, Yuhan, Deelman, Tara E., Chen, Keyue, Lin, Dawn S. Y., Tavakkoli, Ali, Karp, Jeffrey M.
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container_end_page 842
container_issue 9
container_start_page 834
container_title Nature materials
container_volume 17
creator Lee, Yuhan
Deelman, Tara E.
Chen, Keyue
Lin, Dawn S. Y.
Tavakkoli, Ali
Karp, Jeffrey M.
description 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. The gastrointestinal tract is a therapeutic target for type-2 diabetes. An orally deliverable sucralfate-based material is shown to form a physical coating in the gut, capable of limiting glucose uptake and also administering drugs to the gut lining.
doi_str_mv 10.1038/s41563-018-0106-5
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subjects 631/61/54
639/166/985
639/301/54/990
Aluminum
Biomaterials
Chemistry and Materials Science
Coating effects
Condensed Matter Physics
Diabetes mellitus
Drug delivery systems
Gastrointestinal system
Gastrointestinal tract
Materials Science
Mucous membrane
Nanotechnology
Optical and Electronic Materials
Protective coatings
Sucrose
title Therapeutic luminal coating of the intestine
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