Traveling the Vitamin B₁₂ Pathway: Oral Delivery of Protein and Peptide Drugs

• Published in: Angewandte Chemie (International ed.) Vol. 48; no. 6; pp. 1022 - 1028
• Main Authors: Petrus, Amanda K, Fairchild, Timothy J, Doyle, Robert P
• Format: Journal Article
• Language: English
• Published: Weinheim Wiley-VCH Verlag 26.01.2009; WILEY-VCH Verlag; WILEY‐VCH Verlag
• Subjects: Administration, Oral; Animals; bioconjugates; drug delivery; Insulin - blood; Insulin - chemistry; medicinal chemistry; Nanoparticles - chemistry; Peptides - administration & dosage; Peptides - chemical synthesis; Peptides - chemistry; Protein Structure, Tertiary; Proteins - administration & dosage; Proteins - chemical synthesis; Proteins - chemistry; proteins/peptides; Rats; Transcobalamins - chemistry; Transcobalamins - metabolism; Vitamin B 12 - chemical synthesis; Vitamin B 12 - chemistry; Vitamin B 12 - metabolism; vitamin B12
• ISSN: 1433-7851; 1521-3773
• DOI: 10.1002/anie.200800865

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 B₁₂. Recent progress in this field includes the delivery of erythropoietin, granulocyte-colony-stimulating factor, luteinizing-hormone-releasing hormone, and insulin.