Oral insulin – for ever a dream – but maybe not…
For years, the thought of taking insulin by injection tortured diabetes patients with visions of older relatives using barbaric and tedious methods for self injection. Fortunately, these can now only be seen in museums, as since the production of microfine needles and disposable pens, injectables are now a major way in which medication is taken for many different diseases – and not just diabetes.
Insulin taken orally gets destroyed in the stomach’s acid environment and is poorly absorbed from the intestine. Packaging it in an ionic liquid of choline and geranic acid and protected by a capsule round it that is acid-resistant may be the answer. This protects the insulin from destruction in the stomach after ingestion. This polymer coating dissolves when it reaches a more alkaline environment in the small intestine, where the ionic liquid carrying insulin is released.
The choline-geranic acid formulation also helps insulin go through two final barriers — the layer of mucus lining the intestine and the tight cell junctions of the intestine wall, through which large-molecule drugs such as insulin usually cannot pass.
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.
Inhaled insulin was hailed as an advance but failed to become popular and so caution is needed before we hope that oral insulin becomes a commercial reality. Is it going to be as good, as accurate and fine tunable, and cheaper, or have problems? Every route of entry into the body – whether skin, lung or the gastrointestinal tract will have its own difficulties.
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. Long term toxicological and bioavailability studies and human clinical trials have yet to be done.
The research was published in the Proceedings of the National Academy of Sciences.
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