Controlled Drug Delivery. Designing Technologies for the by Kinam Park

By Kinam Park

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The challenge to achieve sufficient peptide or protein drug absorption is to overcome the very efficient absorption barriers of the gastro-intestinal tract. ; ACS Symposium Series; American Chemical Society: Washington, DC, 2000. 25 26 controlled by the integrity of intercellular junctions, and 3) the mucus layer which covers the epithelial cells as a blanket and forms a highly viscous network of glycoproteins, hampering the diffusion of peptides. Although different enzyme inhibitors and absorption enhancers, with the disadvantage to display undesired systemic side effects, have been shown to improve the absorption of various peptide drugs, there is still a need for the search of safe absorption enhancing excipients for peroral delivery of peptide drugs.

24. ; Siahaan, T. ; Borchardt, R. T. J. Peptide Res. 1999, 53, 370. 25. ; Pauletti, G. M . ; Borchardt, R. T. Pharm. Res. 1999,16,7. 26. ; Jois, S. D. ; Vander Velde, D. ; Siahaan, T. ; Borchardt, R. T. J. Peptide Res. 1999, 53, 383. 27. ; Siahaan, T. ; Borchardt, R. T. Pharm. Res. 1999,16, 16. 28. ; Siahaan, T. ; Friis, G. ; Borchardt, R T. J. Peptide Res. 1999, 53, 393. 29. ; Vander Velde, D. ; Jois, S. D. ; Siahaan, T. ; Borchardt, R. T. J. Peptide Res. 1999, 53, 403. 30. Hartman, G. ; Egbertson, M .

Blocking of these groups reduces the affinity to a significant extent but they still can be recognized as substrates of peptide transporters. , captopril, enalapril, quinapril, benazepril) have been shown to be transported via the intestinal peptide transport system even though they do not have an N-terminal α-amino group (24-26). Also, thyrotropin releasing hormone (TRH) and some renin inhibitors which do not have a free C-terminal carboxyl group are reported to be transported by the peptide transporters (27, 28).

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