Oral routes of administration for therapeutic peptides and proteins face two major barriers: proteolytic degradation in the stomach and an inadequate absorption mechanism for polypeptides within the intestinal lumen. As a result, peptide-based therapeutics are administered by injection, a painful process associated with lower patient compliance. The development of a means of overcoming these two major obstacles and enabling the successful delivery of peptide therapeutics by the oral route of administration has therefore been the target of extensive scientific endeavor. This Minireview focuses on oral peptide/protein delivery by the dietary uptake pathway for vitamin B(12). Recent progress in this field includes the delivery of erythropoietin, granulocyte-colony-stimulating factor, luteinizing-hormone-releasing hormone, and insulin.