• mucosal drug delivery;
  • gastrointestinal;
  • macromolecular drug delivery;
  • oral drug delivery;
  • membrane transport;
  • microneedles;
  • pill;
  • drug delivery systems

Both patients and physicians prefer the oral route of drug delivery. The gastrointestinal (GI) tract, though, limits the bioavailability of certain therapeutics because of its protease and bacteria-rich environment as well as general pH variability from pH 1 to 7. These extreme environments make oral delivery particularly challenging for the biologic class of therapeutics. Here, we demonstrate proof-of-concept experiments in swine that microneedle-based delivery has the capacity for improved bioavailability of a biologically active macromolecule. Moreover, we show that microneedle-containing devices can be passed and excreted from the GI tract safely. These findings strongly support the success of implementation of microneedle technology for use in the GI tract. © 2014 Wiley Periodicals, Inc. and the American Pharmacists Association J Pharm Sci 104:362–367, 2015