Oral capsule administration of biomacromolecules that achieves bioavailability and pharmacokinetics comparable to subcutaneous injection in dogs – the BIONDD® technology

Abstract

Biomacromolecules including peptides, proteins, antibodies, and gene medicines, comprise important classes of therapeutics in treating disease. A drawback of biologics is their inconvenient route of administration, as they are mostly injected. Most patients prefer the oral administration route over injections. To accommodate this need, we developed the BIONDD® technology, which is an oral administration device for biomacromolecules contained in a standard 00 or 0-sized capsule. Upon ingestion and actuation in the stomach, the macromolecule is delivered from the cavity of the device’s spike into the gastric wall, from where it migrates to the blood vessels. Using 0.4 mg liraglutide as a model peptide, a short Tmax and a relative oral bioavailability of 119% compared to subcutaneous administration were achieved over time after oral administration of the BIONDD® capsule to dogs. The pharmacokinetic data from the large animal studies obtained provides proof-of-concept for a convenient oral delivery device for biologics.