Delivering therapeutically active large molecules by the oral route has been a challenge and a goal for several decades.  The oral route of administration for these substances is problematic due to many reasons: proteolysis by gastric and pancreatic enzymes, high acidity in the stomach and limited absorption through the GI tract.  However the benefits of oral delivery are clear, with the ease of administration and improved patient compliance being the major advantages.

Encap can employ a number of strategies:

• Formulation is designed for optimal biomolecule chemical and conformational stability in a part aqueous environment which is still compatible with capsules
  
• Avoid exposure to stomach and targeted delivery to small intestine using enteric coating
• Targeted delivery to colon using ENCODE technologies

As well as delivery of proteins and peptides, our approach can also be used for domain antibodies, oligonucleotides and oral vaccines.

Case Study:

A water soluble protein which is stable in an aqueous environment, was provided as a concentrate in an aqueous buffer (phosphate buffer solution (PBS)), which was diluted to the required concentration with water. The diluted protein/buffer solution was then incorporated into a novel formulation containing 28% water. A hard shell gelatine capsule was then filled with the formulation and the capsule was closed and banded. After stability testing, the capsule was found to remain stable without softening or cracking after three months stability storage, and the formulation retained its protein concentration and activity. This therefore provided a viable route for the formulation of proteins (and peptides) in stable aqueous media for administration in capsule form.

Please contact us to find out more