Glycyl-l-histidyl-l-lysineCu(II) (GHKCu 2+)-loaded Zn-pectinate microparticles in the form of hydroxypropyl cellulose (HPC) compression-coated tablets were prepared and their in vitro behavior tested. GHKCu 2+ delivery to colon can be useful for the inhibition of matrix metalloproteinase, with the increasing secretion of tissue inhibitors of metalloproteinases (TIMPS),which are the major factors contributing in mucosal ulceration and inflammation in inflammatory bowel disease. The concentration of peptide was determined spectrophotometrically. The results obtained implied that surfactant ratio had a significant effect on percent production yield (1.25 to 1.75 w/w; 72.22% to 80.84%), but cross-linking agent concentration had not. The entrapment efficiency (EE) was found to be in the range of 58.2578.37%. The drug-loading factor significantly increased the EE; however, enhancement of cross-linking agent concentration decreased it. The release of GHKCu 2+ from Zn-pectinate microparticles (F1F8) in simulated intestinal fluid was strongly affected by cross-linking agent concentration and drug amount (50mg for F1F6; 250mg for F7F8), but not particularly affected by surfactant amount. Release profiles represented that the microparticles released 5080% their drug load within 4h. Therefore, the optimum microparticle formulation (F8) coated with a relatively hydrophobic polymer HPC to get a suitable colonic delivery system. The optimum colonic delivery tablets prepared with 700mg HPC-SL provided the expected delayed release with a lag time of 6h. The effects of polymer viscosity and coat weight on GHKCu 2+ release were found to be crucial for the optimum delay of lag time. The invention was found to be promising for colonic delivery. © 2011 Informa Healthcare USA, Inc.