title: Novel delivery system based on complexation hydrogels as delivery vehicles for insulin-transferrin conjugates.
abstract: A variety of approaches have been investigated to address the problems associated with oral insulin delivery, but the bioavailability of oral insulin is still low. Insulin is rapidly degraded by the enzymes in the GI tract and is not transported across the epithelial barrier easily. The oral insulin formulation developed in this work makes use of complexation hydrogels for oral delivery of insulin bioconjugates. The insulin bioconjugates synthesized in this work consist of insulin bound to transferrin molecule which can be uptaken by the epithelial cells. The conjugates can increase the permeability of insulin across the epithelial barrier by receptor-mediated transcytosis. The transferrin in the conjugate is also shown to stabilize insulin in the presence of intestinal enzymes. Use of complexation hydrogels for delivery of insulin-transferrin conjugate may greatly increase the bioavailability of oral insulin. This is because, the complexation hydrogels are known to exhibit characteristics that make them ideal candidates for oral protein delivery. They can also inhibit the degradation of insulin in the GI tract. Thus, combination of these two approaches may provide an innovative platform for oral insulin delivery.
authors.affiliation: Department of Chemical Engineering, University of Texas at Austin, Austin, TX 78712, USA.
authors.forename: Nikhil J
authors.initials: NJ
authors.lastname: Kavimandan
authors.forename: Elena
authors.initials: E
authors.lastname: Losi
authors.forename: Nicholas A
authors.initials: NA
authors.lastname: Peppas
mesh_terms: D000284:Administration, Oral; D000818:Animals; D001672:Biocompatible Materials / Q000008:administration & dosage / Q000737:chemistry / Q000378:metabolism; D001692:Biological Transport / Q000502:physiology; D018938:Caco-2 Cells; D004337:Drug Carriers; D006801:Humans; D020100:Hydrogels / Q000737:chemistry / Q000378:metabolism*; D007328:Insulin / Q000008:administration & dosage* / Q000737:chemistry / Q000378:metabolism; D008422:Materials Testing; D010316:Particle Size; D011092:Polyethylene Glycols / Q000737:chemistry / Q000378:metabolism; D011109:Polymethacrylic Acids / Q000737:chemistry / Q000378:metabolism; D014168:Transferrin / Q000008:administration & dosage* / Q000737:chemistry / Q000378:metabolism
chemical_list: D001672:Biocompatible Materials; D004337:Drug Carriers; D020100:Hydrogels; D007328:Insulin; D011109:Polymethacrylic Acids; D014168:Transferrin; C030613:polymethacrylic acid; D011092:Polyethylene Glycols