title: Intestinal micropatches for oral insulin delivery.
abstract: Diabetes mellitus has become a major public health issue that has almost reached epidemic proportions worldwide. Injectable insulin has been typically utilized for the management of this chronic disease. However, lack of patient compliance with injectable formulations has spurred the development of oral insulin formulations, which although appealing, face several delivery challenges. We have developed novel mucoadhesive intestinal patches, several hundred micrometers in dimension (micropatches) that address the challenges of oral insulin delivery. The micropatches adhere to the intestinal mucosa, release their drug load rapidly within 30 min and are effective in lowering blood glucose levels in vivo. When insulin-loaded micropatches were administered with a permeation enhancer and protease inhibitor, a peak efficacy of 34% drop in blood glucose levels was observed within 3 h. Efficacy further improved to 41% when micropatches were administered in multiple doses. Here, we describe the design of micropatches as an oral insulin formulation and report their in vivo efficacy.
authors.affiliation: a Department of Chemical Engineering , University of California , Santa Barbara , CA , USA.
authors.forename: Amrita
authors.initials: A
authors.lastname: Banerjee
authors.affiliation: a Department of Chemical Engineering , University of California , Santa Barbara , CA , USA.
authors.forename: Jessica
authors.initials: J
authors.lastname: Wong
authors.affiliation: b College of Letters and Science, University of California , Santa Barbara , CA , USA.
authors.forename: Rohan
authors.initials: R
authors.lastname: Gogoi
authors.affiliation: c Interdepartmental Program in Biomolecular Science and Engineering , University of California , Santa Barbara , CA , USA.
authors.forename: Tyler
authors.initials: T
authors.lastname: Brown
authors.affiliation: a Department of Chemical Engineering , University of California , Santa Barbara , CA , USA.|d Center for Bioengineering, University of California Santa , Barbara , CA , USA.
authors.forename: Samir
authors.initials: S
authors.lastname: Mitragotri
mesh_terms: D000284:Administration, Oral; D000818:Animals; D016503:Drug Delivery Systems; D007328:Insulin / Q000008:administration & dosage* / Q000378:metabolism; D007413:Intestinal Mucosa / Q000378:metabolism*; D008297:Male; D051381:Rats; D017208:Rats, Wistar
chemical_list: D007328:Insulin
keywords: Diabetes; micropatch; oral insulin delivery; permeation enhancer; proteolytic inhibitor