Al Rubeaan Khalid, Rafiullah Mohamed, Jayavanth Sanjay
a Strategic Center for Diabetes Research, University Diabetes Center, College of Medicine , King Saud University , Riyadh , Saudi Arabia.
Expert Opin Drug Deliv. 2016;13(2):223-37. doi: 10.1517/17425247.2016.1107543. Epub 2015 Nov 7.
There are several hurdles to oral insulin delivery (OID): mainly, enzymatic proteolysis, gastric degradation, and an absorption barrier. Researchers have been attempting to overcome these natural barriers through chitosan-based insulin formulations.
In this paper, the authors review OID formulations to elucidate their techniques and evaluate their performance through a set of defined parameters and suggest overall outlooks and future directions. This review covers 86 articles and reveals that most oral insulin formulations were obtained through poly-electrolytic complexation or chemical modification techniques. The in-vitro results reported by the articles are mapped into a '30x70 performance window' to distinguish the best OID formulations. The review shows that most formulations were effective in addressing the gastric and enzymatic barriers but were not as effective in overcoming the absorption barrier of the gastrointestinal tract.
Oral insulin delivery has been a topic of immense research with most efforts dedicated to developing a formidable insulin formulation that overcomes gastrointestinal tract barriers. While most OID formulations perform better under experimental conditions, their performance in in-vivo studies is not as effective. Thus, to make oral insulin delivery a reality, special attention is needed toward improving the in-vivo insulin absorption through the gut.
口服胰岛素给药(OID)存在诸多障碍:主要包括酶促蛋白水解、胃内降解以及吸收屏障。研究人员一直在尝试通过基于壳聚糖的胰岛素制剂来克服这些天然屏障。
在本文中,作者回顾了口服胰岛素给药制剂,以阐明其技术,并通过一组既定参数评估其性能,同时提出总体展望和未来方向。本综述涵盖了86篇文章,结果表明,大多数口服胰岛素制剂是通过聚电解质络合或化学修饰技术获得的。文章报道的体外结果被映射到一个“30×70性能窗口”中,以区分最佳的口服胰岛素给药制剂。该综述表明,大多数制剂在解决胃和酶屏障方面有效,但在克服胃肠道吸收屏障方面效果不佳。
口服胰岛素给药一直是大量研究的主题,大多数努力都致力于开发一种强大的胰岛素制剂,以克服胃肠道屏障。虽然大多数口服胰岛素给药制剂在实验条件下表现更好,但其在体内研究中的性能并不那么有效。因此,要使口服胰岛素给药成为现实,需要特别关注改善胰岛素在肠道内的体内吸收。