Taking a short cut: Drug delivery through the oral mucosa

Drug delivery company NorInvent, based at Medicon Valley, has a focus on delivering drugs through the oral mucosa, with an aim to improve outcomes for patients and support pharma companies through the drug lifecycle

Giving patients drugs as pills goes back to around 1500 BCE, and oral tablets are still one of the most common ways to take drugs. Tablets are low cost to prepare and simple to store, distribute and administer, but they also have their challenges too, including slow absorption, limited bioavailability and potential gastric side effects.

The oromucosal approach: XtriG
Taking drugs as oral tablets is a simple and non-invasive route, but the active ingredients have to pass through the digestive system and liver before they can reach the bloodstream. This can take up to 45 minutes, which is not ideal for rapid relief of symptoms, such as pain, and may require higher doses as some drug is lost or metabolised on route, leading to gastric irritation.
There are a number of drugs on the market that are dosed via the oral mucosa, via gels, films and sublingual tablets. This approach means that drugs can pass more quickly into the bloodstream, bypassing the gut and avoiding the challenges of oral bioavailability. However, existing mucosal delivery systems don't always provide a consistent dose, and drug may also be ingested as well as absorbed.
"We believe that oral mucosal delivery could significantly cut the time to effect and create a better-controlled release profile," said Paul Hasselgren, CEO. "It could also reduce the dose needed, which would have cost and environmental benefits, and could reduce gastric and other side effects."
NorInvent's approach is based around XtriG, a family of chains of carbohydrate linkers that bind to drugs and then release the active ingredients when placed under the upper lip. The drugs pass through the oral mucosa and could potentially begin to enter the blood within five or ten minutes. NorInvent is currently carrying out initial binding studies using ibuprofen, nicotine and sildenafil, and will carry out further binding studies with additional drugs to expand the company's knowledge and support discussions with potential partners. The next step will be to carry out proof-of-mechanism studies with one (or more) selected drugs.

Reducing the risk of drug development
XtriG is a generic platform, and has potential to deliver a wide range of small molecule drugs. As well as applications for new drugs, the XtriG delivery system could allow companies to offer alternative formulations of existing approved drugs, or repurpose agents that have made it through into the clinic but have been pulled because of issues with oral dosing. The risk of development would be lower because of the availability of clinical safety data.
"XtriG could be a way for companies to extend the lifecycle and market for their branded drugs, particularly as they approach patent expiry," said Hasselgren. "We plan to begin in vitro proof-of-mechanism studies in the second half of 2017. These will include drug binding and dissolution, and drug release in saliva. Once we have developed a prototype, we will then take this into animal or human proof-of-concept studies, and use this information to seek partners. We will look for deals based on upfront and milestone payments, and/or royalties."

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