Abstract

Nanoparticle-based carriers are increasingly recognized as one of the most promising ways to improve the solubility and permeability of encapsulated drugs, leading to more robust transit across physiological barriers and increased systemic bioavailability. Peptides, owing to their enormous therapeutic value but minimal tolerance for the gastrointestinal tract, have been the subject of intense research to determine what benefit to their oral delivery, if any, can be gained by the incorporation of nanotechnology. Presently, there are no FDA-approved oral nanoparticle formulation for peptides, but a plethora of prototypes, ranging from polymeric to liposomal nanocarriers, are showing translational potential. In this chapter, our focus will be on the oral delivery of insulin, cyclosporine, calcitonin, and exenatide using nanoparticles. We will highlight some of the most recent and illustrative examples with respect to these four peptides of major clinical significance, and for which successful administration by the oral route should be most impactful.

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