Formulation and dosage form for increasing oral bioavailability of hydrophilic macromolecules

A formulation for enhancing the bioavailability of an orally administered hydrophilic macromolecule, the formulation comprising a hydrophilic macromolecule, a permeation enhancer, and a carrier capable of forming a bioadhesive gel, wherein the hydrophilic macromolecule comprises between about 0.01 wt % and about 50 wt % of the formulation, the permeation enhancer comprises between about 11% and about 30% of the formulation, and the carrier comprising between about 35% and 88% of the formulation.

A dosage form comprising:

• a formulation comprising a hydrophilic macromolecule, a permeation enhancer, and a carrier capable of forming a bioadhesive gel, the formulation being formulated such that the formulation is released within the gastrointestinal tract as a liquid and forms a bioadhesive gel in-situ after the formulation has had some opportunity to spread across a surface of a gastrointestinal mucosal membrane;
• and
• a delivery device configured to release the formulation within the gastrointestinal tract of a subject at a controlled rate over a period of time.

A controlled release dosage form comprising:

• a liquid formulation comprising a hydrophilic macromolecule, the formulation being capable of enhancing the oral bioavailability of the hydrophilic macromolecule;
• and
• a deliver device configured to deliver the formulation over a desired period of time.