The Medical Need
Safe and reliable delivery to the intestine
Oral delivery is the most convenient route for patients to take biopharmaceuticals and prebiotics/probiotics. However, these compounds are prone to low pH and protease digestion in the stomach and must be protected by a gastro-resistant encapsulation in order to be able to exit the stomach without having their efficacy negatively affected.
There is a strong medical need for a gastro-resistant enteric encapsulation made from safe bio-inactive materials that can target early release in the upper parts of the small intestine or late release in the colon.
Safe and reliable delivery to the intestine
Oral delivery is the most convenient route for patients to take biopharmaceuticals and prebiotics/probiotics. However, these compounds are prone to low pH and protease digestion in the stomach and must be protected by a gastro-resistant encapsulation in order to be able to exit the stomach without having their efficacy negatively affected.
There is a strong medical need for a gastro-resistant enteric encapsulation made from safe bio-inactive materials that can target early release in the upper parts of the small intestine or late release in the colon.
The long-standing benchmarks for gastro-resistant encapsulations are the polymethacrylate based encapsulations. However, the methyl acrylate/ethyl acrylate copolymers have major clinical weaknesses. There is a very restricted design space for their pH dependent dissolution profiles, and there are scientific reports that drugs were not released in the intestine as intended.
Further, the polymethacrylates show signs of bioactivity. Ethyl acrylate was observed by the FDA for years after findings of carcinogenicity on forestomach epithelium in rats.
Polymethacrylates may cause irritation with eye contact and skin contact and adverse effects have been reported in patients given high doses of polymethacrylates coated tablets.
EMA and FDA only approve intake of polymethacrylates in very limited amounts.
Their potential bioactivity renders them less desirable for use in pharmaceuticals and unwanted for use with nutraceuticals.
Rybelsus® (semaglutide) tablets from Novo Nordisk is an example of an emerging orally delivered biopharmaceutical. More orally delivered biopharmaceutical are expected to be developed in the coming years.
Oral peptide delivery is already a reality with peptides like Glutathione, Desmopressin, Cyclosporine, Colistin, Vancomycin and Plecanatide and many others with high therapeutic benefits is on the market. A high number of peptides meant for oral delivery are currently in development.
Sensitive pharmaceuticals like proton pump inhibitors Omeprazole, Pantoprazole or Lansoprazole or CNS stimulants like Amphetamine and Dextroamphetamine could benefit from an improved enteric encapsulation
Oral prebiotic/probiotic administration. Companies like EnteroBiotix, Microbiotica, MaatPharma, Sniprbiome, Eligo, Caelus Health and Chainbiotech are examples of biotech companies that have microbiome and microbiota therapeutics in development. In general, there are high expectations to this type of products. Several more classical probiotics, that requires enteric encapsulations, are currently on the market.
Oral delivery of vaccines. Oral administration of non-replicating viral vector vaccines is an emerging approach to vaccination that requires an enteric encapsulation.
Also, certain functional foods, supplements and nutraceuticals benefit from enteric encapsulations. This type of products absolutely require excipients made from safe natural raw materials, as there is no control on their daily intake.