oral insulin delivery covalent organic frameworks

• Published in: Chemical science (Cambridge) 2021-05, Vol.12 (17), p.637-647
• Main Authors: Benyettou, Farah, Kaddour, Nawel, Prakasam, Thirumurugan, Das, Gobinda, Sharma, Sudhir Kumar, Thomas, Sneha Ann, Bekhti-Sari, Fadia, Whelan, Jamie, Alkhalifah, Mohammed A, Khair, Mostafa, Traboulsi, Hassan, Pasricha, Renu, Jagannathan, Ramesh, Mokhtari-Soulimane, Nassima, Gándara, Felipe, Trabolsi, Ali
• Format: Article
• ISSN: 2041-6520; 2041-6539
• DOI: 10.1039/d0sc05328g

With diabetes being the 7th leading cause of death worldwide, overcoming issues limiting the oral administration of insulin is of global significance. The development of imine-linked-covalent organic framework (nCOF) nanoparticles for oral insulin delivery to overcome these delivery barriers is herein reported. A gastro-resistant nCOF was prepared from layered nanosheets with insulin loaded between the nanosheet layers. The insulin-loaded nCOF exhibited insulin protection in digestive fluids in vitro as well as glucose-responsive release, and this hyperglycemia-induced release was confirmed in vivo in diabetic rats without noticeable toxic effects. This is strong evidence that nCOF-based oral insulin delivery systems could replace traditional subcutaneous injections easing insulin therapy. We report the successful use of a gastro-resistant covalent organic framework for in vivo oral delivery of insulin.