Oral Insulin Choline, Geranate Ionic Liquid Shows Promise

TUESDAY, July 3, 2018 — An oral insulin formulation has been developed using choline and geranate (CAGE) ionic liquid, which significantly reduces blood glucose levels in vivo for a sustained period, according to a study published online June 25 in the Proceedings of the National Academy of Sciences.

Noting that there is an urgent need for the development of efficient oral insulin formulations, but that the gastrointestinal tract presents a barrier to oral delivery of biologics, Amrita Banerjee, Ph.D., from the University of California in Santa Barbara, and colleagues report on the development of an oral insulin formulation using CAGE ionic liquid.

The researchers found that CAGE significantly enhanced paracellular transport of insulin, protecting insulin from enzymatic degradation and interacting with the mucus layer, causing it to thin. After jejunal administration in rats, in vivo insulin-CAGE showed exceptional pharmacokinetic and pharmacodynamic outcome. A significant decrease in blood glucose levels was seen with low insulin doses (3 to 10 U/kg), which were sustained for longer periods of up to 12 hours. A sustained decrease in blood glucose of up to 45 percent was seen when 10 U/kg insulin-CAGE was orally delivered in enterically coated capsules using an oral gavage. High biocompatibility was seen for the formulation, and it was stable for two months at room temperature and for at least four months under refrigeration.

“The results indicate that CAGE is a promising oral delivery vehicle and should be further explored for oral delivery of insulin and other biologics that are currently marketed as injectables,” the authors write.

One author is an inventor on patents of ionic liquids for oral delivery and a shareholder of Liquideon.

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Posted: July 2018

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