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.

Keywords:

• Diabetes
• micropatch
• oral insulin delivery
• permeation enhancer
• proteolytic inhibitor

Disclosure statement

The authors report no conflicts of interest. The authors alone are responsible for the content and writing of this article.

Additional information

Funding

The study was conducted using funds from National Institutes of Health grant R01DK097379. The authors would like to acknowledge the Biological Nanostructures Laboratory within the California NanoSystems Institute, supported by the University of California, Santa Barbara and the University of California, Office of the President. In addition, thanks to the MRL Shared Experimental Facilities supported by the MRSEC Program of the National Science Foundation under award NSF DMR 1121053, a member of the NSF-funded Materials Research Facilities Network. Research reported here was also supported by the National Institute of General Medical Sciences of the National Institutes of Health under Award Number T34GM113848. SM is a scientific advisor and shareholder of Entrega Bio.