While clinical data suggest an oral insulin product may finally be within reach, the technology struggles to compete with injectables on price and efficacy. A handful of academics and companies are pushing preclinical innovation in formulation and device design, aiming to solve the commercial conundrum.
Despite numerous setbacks over at least 50 years, the allure of an oral insulin product that eliminates frequent injections and reduces the risk of dangerous hypoglycemic episodes has continued to spur research in the field.
While needle technology has improved, making injections less burdensome for patients, developers argue that an oral product would produce fewer side effects and provide an opportunity to start therapy earlier in Type II diabetes.
The challenge of orally delivering insulin -- or any biologic -- has always been bioavailability. The acidity in the stomach destroys proteins long before they reach the circulation.
Over the last decade, several companies have developed formulations that shield a portion of the peptides from stomach acid and promote their uptake in the intestines.
The problem is that although these modifications achieve bioavailability high enough to control glucose levels, it may not be high enough to achieve cost-effective dosing.
“The result of the oral delivery approaches in the clinic is that you get bioavailability in the 1% or sub 1% range. 99.5% of the drug is going to get destroyed, so if you’re trying to deliver 10 units of insulin orally, you would need to package 1,000