6-2009-2338 | A platform technology for gastric absorption of macromolecules, proteins and peptides in particular
, HUJI, School of Medicine - IMRIC, Developmental Biology and Cancer Research
A platform technology for oral delivery of proteins and peptides, providing a non-invasive alternative to injection, by enhancing gastric absorption
Oral drug-delivery, non-invasive drug administration, gastric absorption, peptide oral formulation, tight junctions (TJs), biopharmaceutical drugs, oral insulin, diabetes treatments, oral bioavailability, pharmacokinetics, drug development.
Pre-clinical proof of concept and initial results
PCT application filed
We have developed a platform technology based on a proprietary formulation, providing a non-invasive, highly effective oral delivery vehicle of proteins and peptides. As opposed to other formulations, our formulation enables the drug to begin its absorption already when reaching the stomach. This method could replace injections of drugs, as exemplified by insulin and GLP1 used for treating diabetes.
Peptides and other large-molecule drugs - cannot pass through the GI wall due to their large size and, therefore, are administered by injection. Moreover, such drugs would be degraded by enzymes instantly if entered the digestive system.
While the number of protein and peptide therapeutics approved for human therapy is increasing steadily, injection still remains the main delivery route for these drugs, and an improved administration method could have a critical impact on the success of new drugs, especially if such agents should be administered several times a day.
The GI tract, covered by a layer of individual cells, is hermetically sealed via tight-junctions (TJs), a zipper-like structure that "glue" neighboring cells. TJs, however, are dynamic structures that can be disassembled and re-formed.
Our proprietary formulation onto which the peptide drug is loaded is enables TJs opening, transiently, and enhances safe penetration of peptide into the blood stream for a period of 15-30 minutes. Moreover, this unique formulation facilitates gastric absorption yet prevents any other gastric content to sneak through these TJ gates.
· Rapid gastric absorption of the medication
· Higher efficacy than competing technologies
· Non-invasive, harmless administration
· Non-aqueous formulation which increase protein’s shelf-life
· Robust formulation-process (Homogeneous solution)
· Low cost
· Storable at room-temperature
· Suitable for soft-gel encapsulation
· Applicable for a broad variety of therapeutic proteins and peptides
· Enhances protein solubility
Formulation's prototype can be readily apply according to client needs, whereby the drug will be delivered orally. In addition, we are currently fine-tuning the formulation further. MoAbs (monoclonal antibodies) would be explored and formulated according to needs.
· A range of injected biologics already on the market (e.g. insulin and GLP-1)
· Future and recently-discovered proteins and peptides