Microparticles for delivering therapeutic peptides and proteins to the lumen of the small intestine

Several different peptides and proteins, such as the pancreatic trypsin inhibitor, growth factors and trefoil peptides, are known to play important roles in maintaining the structure and function of the gastrointestinal wall. With the advent of recombinant biotechnology, it has become feasible to test some of these proteins as therapeutics in different inflammatory conditions of the intestines. However, the harsh pH and enzymatic conditions of the stomach can lead to their inactivation. This research was aimed at the development of particulate, gastric-resistant pharmaceutical forms, incorporating those bioactive molecules. Mixtures of proteins in powder form were coated with cellulose acetate phthalate, Eudragit® S100 or Eudragit® RS PO, using simple preparation techniques based on single emulsion/solvent evaporation. Using aprotinin as a model drug, it was found that these procedures were effective in microencapsulating protein in the solid form without affecting its biological activity. Furthermore, and in particular with the first two polymers above, particles showed adequate in vitro release patterns for the applications envisioned.