A promising new oral delivery mode for insulin using lipid-filled enteric-coated capsules

Abstract

The treatment of diabetes requires daily administration of the peptide insulin via subcutaneous (SC) injection due to poor stability following oral administration. Enteric capsules, designed to protect against low pH conditions in the stomach by providing a polymeric coating which only breaks down in the small intestine, have failed to significantly increase oral bioavailability for insulin. In parallel, amphiphilic lipid mesophases are versatile carrier materials which can protect encapsulated proteins and peptides from undesirable enzymatic degradation. Here we show the combined delivery capacity of a hydrated bicontinuous cubic lipid mesophase embedded within an enteric capsule. Animal studies demonstrated that the lipid filled enteric capsules could deliver insulin with bioavailabilities (relative to SC injection) as high as 99 % and 150 % for fast and slow acting insulin, respectively. These results provide a promising starting point towards further trials to develop an alternative, non-invasive mode for the delivery of insulin.