Researchers are working hard for decades to find a holy grail of drug delivery: a way to give protein and peptide drugs like insulin through mouth, instead of the painful injection. Harvard scientist researchers have made huge stride forward by carrying insulin in an ionic liquid that prevents stomach enzymes from breaking down the drug. This approach more closely mimics the way in which a healthy person’s pancreas makes and delivers insulin to the liver, thereby mitigating some of the adverse effects of injecting insulin over a long time.
Approximately 40 million people have type-1 diabetes worldwide and surviving on an insulin injection to keep their glucose levels in control. Type-1 diabetic patients at starting require two injections of insulin injected per day of two different types of insulin and then gradually progress to three or four injections per day of different types of insulin. This makes type-1 diabetic patients normal life messed up and many people fail to face this very strict regime. Phobia of injections, painful injection and uncomfortable with each injection, making it an ordeal.
Senior author Samir Mitragotri, a Professor of Bioengineering at the Harvard John A. Paulson School of Engineering and Applied Sciences (SEAS) said that the consequences of the resulting poor glycemic control can lead to serious health complications. But with the success of delivering insulin by mouth can solve many problems and would make easy as popping any tablet.
The reason behind the non-availability of an insulin pill is that stomach’s acidic environment broken down the protein and the intestines can’t absorb it properly. Scientists have attempted so many trials to remove these obstacles by re-engineering with the insulin molecule, coating it in protective polymers, and introducing additives to inhibit breakdown by enzymes or to enhance absorption. Currently, no such treatment is clinically available, where insulin is giving in a pill form.
Proceedings of the National Academy of Science.published a recent report which is about the new method that carries insulin in an ionic liquid comprised of choline and geranic acid that is then put inside a capsule with an acid-resistant enteric coating.
Samir Mitragotri, Professor at the Harvard University and his colleagues followed a different route to formulate a pill alternative of the insulin. Samir also added that their approach is like a Swiss Army knife, where one pill has the capability for addressing each of the problems that are encountered. They encapsulated an insulin-ionic liquid formulation in an enteric coating — a barrier that prevents the medication’s dissolution or disintegration in the gastric environment. The ionic liquid is comprised of choline and geranic acid, a biocompatible formulation that is an easy and low price to manufacture. What’s more, it can be stored for up to two months without degrading, which is longer than some injectable medications on the market.
Once it makes its way to the small intestine, where the environment is more alkaline, the ionic liquid carrying the insulin is automatically released. The implications of this work in the medical field could be huge — the approach could potentially be applied to many other proteins besides insulin.
In the future, the Harvard researchers want to conduct more animal tests of the formulation in order to monitor the long-term toxicological effects. If all goes well, clinical trials in humans could gain approval faster than they normally would since the key ingredients of the ionic liquids are already considered safe. Choline is a vitamin-like essential nutrient and geranic acid, a widely used food additive, naturally occurs in cardamom and lemongrass.