Scientists make breakthrough in developing an insulin pill for diabetics

by Barbara Hewitt on July 3, 2018

Scientists in the United States have developed an insulin pill which they believe could signal the end to daily jabs for diabetics who need insulin injections.

They say that not only could it improve the quality of life for millions of people with type 1 diabetes, but also mitigate many of the life threatening health issues that can arise when diabetics forget to inject their insulin.

Insulin Pill

(By Photomaxx/Shutterstock.com)

The researchers at the Wyss Institute at Harvard University and the Harvard John A. Paulson School of Engineering and Applied Sciences (SEAS) developed a new formulation of insulin which is suspended in an ionic liquid consisting of food safe choline and geranic acid in a capsule with an acid-resistant enteric coating.

‘Many people fail to adhere to that regimen due to pain, phobia of needles, and its interference with normal activities. The consequences of the resulting poor glycaemic control can lead to serious health complications,’ said senior author Samir Mitragotri, a professor of bioengineering at SEAS.

The pill could have other benefits as orally ingested insulin could more closely mimic the way in which a healthy individual’s pancreas makes and delivers insulin to the liver, where up to 80% is extracted and the rest is circulated through the bloodstream. It could also mitigate the adverse effects of taking injections over long period of time.

However, finding a way to deliver insulin orally has been elusive as it does not work well in contact with the stomach’s acidic environment, and it is poorly absorbed from the intestine. This is why the scientists have worked on the new approach to suspend insulin in an ionic liquid comprised of choline and geranic acid that is then put inside a capsule with an acid-resistant enteric coating.

The formulation is biocompatible, easy to manufacture, and can be stored for up to two months at room temperature without degrading, which is longer than some injectable insulin products currently on the market.

‘Once ingested, insulin must navigate a challenging obstacle course before it can be effectively absorbed into the bloodstream. Our approach is like a Swiss Army knife, where one pill has tools for addressing each of the obstacles that are encountered,’ Mitragotri explained.

By encapsulating the insulin-ionic liquid formulation in an enteric coating, the research team overcame the first obstacle, resisting breakdown by gastric acids in the stomach. This polymer coating dissolves when it reaches a more alkaline environment in the small intestine, where the ionic liquid carrying insulin is released.

‘When a protein molecule such as insulin enters the intestine, there are many enzymes whose function is to degrade the protein into smaller amino acids. But the ionic liquid borne insulin remains stable,’ said first author Amrita Banerjee, who conducted the research while working as a postdoctoral fellow in Mitragotri’s laboratory and is now an assistant professor at North Dakota State University.

The choline geranic acid formulation also was shown to be adept at penetrating two final barriers to insulin absorption, the layer of mucus lining the intestine and the tight cell junctions of the intestinal wall, through which large molecules such as insulin cannot easily pass.

According to Mark Prausnitz, professor of chemical and biomolecular engineering at Georgia Institute of Technology, the implications are enormous. ‘This study shows remarkable results where insulin given by mouth in combination with an ionic liquid works about as well as a conventional injection. The implications of this work to medicine could be huge, if the findings can be translated into pills that safely and effectively administer insulin and other peptide drugs to humans,’ he said.

The researchers now plan to conduct more animal tests of the formulation as well as long term toxicological and bioavailability studies. They are optimistic that if all goes well, gaining approval for eventual clinical trials in humans will be made easier by the fact that the key ingredients in their ionic liquids already considered safe. Choline is a vitamin like essential nutrient, and geranic acid a chemical that naturally occurs in cardamom and lemongrass which is widely used as a food additive.


The opinions expressed in this article do not necessarily reflect the views of the DiabetesForum.com Community and should not be interpreted as medical advice. Please see your doctor before making any changes to your diabetes management plan.

{ 1 comment… read it below or add one }

Ivan July 5, 2018 at 10:04 am

So when are human trials starting?

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