However, the harsh and acidic conditions of the stomach cause the breakdown and neutralization of this important hormone even before it reaches the intestines and from there into the bloodstream. To overcome this, the researchers remove the insulin molecules through the walls of the stomach using a kind of robot
[Translation by Dr. Moshe Nachmani]
For the millions of diabetics, insulin is a life-saving drug. Despite this, and unlike other drugs, insulin cannot be easily taken by mouth, and must be injected under the skin using a syringe or pump. Researchers have made progress towards an insulin capsule to swallow, and now they report in the scientific journalDHW Nano , because they were able to deliver insulin to the intestines of rats using an oral tablet (by mouth, by swallowing) with the help of chemical 'micromotors'.
Diabetics have difficulty balancing the sugar levels in their blood due to the fact that their body produces little or no insulin. Synthetic insulin has been around for over a hundred years, but it is taken with the help of an injection or a pump attached to the patient's body. Diabetic patients are required to take insulin doses several times a day, so the frequent injections may be painful, especially for children, and as a result, some patients fail to take the recommended amounts at the appropriate times.
An oral form of insulin would be the best way to take it, but the harsh and acidic conditions of the stomach cause this important hormone to break down and neutralize before it reaches the intestines and from there into the bloodstream. Previous attempts to take insulin orally were based on protecting the hormone from stomach acids with the help of micro- or nanocarriers. However, these ideas were based on a tolerant pulsation of the insulin into the cells that make up the intestine, a method that proved to be insufficiently effective. Instead, a better approach would be to actively transfer the drug into the body itself, as occurs with the help of a robot-capsule that delivers its cargo (the drug) by "drilling" through the thick, mucous layer of the small intestine.
The team of researchers wanted to achieve a similar result with their mini-tablet that includes insulin, along with chemical "micromotors" capable of delivering insulin to the intestines in a safe and efficient manner. In order to prepare these tablets, the researchers coated magnesium microparticles in a layer of insulin solution and in a layer of liposomes. In the next step, mix these two components together with sodium bicarbonate (baking soda), compress the resulting product into mini-tablets three millimeters long, and then coat them with a starch-ester solution. The starch protects the tablets (the active substance insulin) from the stomach acids, and allows them to reach the intestines. At the moment of their disintegration, the microparticles of magnesium react with water that create a stream of hydrogen gas bubbles, which serve as "micromotors" that push the insulin towards the walls of the intestines for its absorption there efficiently and quickly. The research team also tested these mini-tablets in mice and found that they were able to significantly reduce their blood sugar levels even after about five hours. In fact, the innovative tablets managed to keep sugar levels as low as after an injection of insulin under the skin. Although more research is needed, the researchers say that their findings so far represent a real step toward the development of new preparations to replace drugs that can only be given by injection.
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