Structural specificity of mucosal-cell transport and metabolism of peptide drugs: implication for oral peptide drug delivery

The brush border membrane of intestinal mucosal cells contains a peptide carrier system with rather broad substrate specificity and various endo- and exopeptidase activities. Small peptide (di-/tripeptide)-type drugs with or without an N-terminal alpha-amino group, including beta-lactam antibiotics...

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Bibliographic Details
Published in:Pharmaceutical research 1992-08, Vol.9 (8), p.969-978
Main Authors: Bai, J. P., Amidon, G. L.
Format: Article
Language:English
Subjects:
Administration, Oral
Amino Acid Sequence
Angiotensin-Converting Enzyme Inhibitors - administration & dosage
Angiotensin-Converting Enzyme Inhibitors - chemistry
Angiotensin-Converting Enzyme Inhibitors - metabolism
Angiotensin-Converting Enzyme Inhibitors - pharmacokinetics
Animals
Anti-Bacterial Agents - administration & dosage
Anti-Bacterial Agents - chemistry
Anti-Bacterial Agents - metabolism
Anti-Bacterial Agents - pharmacokinetics
Biological and medical sciences
Biological Transport
Endopeptidases - metabolism
Exopeptidases
General pharmacology
Humans
Hydrolysis
Intestinal Mucosa - cytology
Intestinal Mucosa - metabolism
Lactams
Life Sciences (General)
Medical sciences
Microvilli - metabolism
Molecular Sequence Data
Peptide Hydrolases - metabolism
Peptides - administration & dosage
Peptides - chemistry
Peptides - metabolism
Peptides - pharmacokinetics
Pharmacokinetics. Pharmacogenetics. Drug-receptor interactions
Pharmacology. Drug treatments
Prodrugs - metabolism
Space life sciences
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Summary:The brush border membrane of intestinal mucosal cells contains a peptide carrier system with rather broad substrate specificity and various endo- and exopeptidase activities. Small peptide (di-/tripeptide)-type drugs with or without an N-terminal alpha-amino group, including beta-lactam antibiotics and angiotensin-converting enzyme (ACE) inhibitors, are transported by the peptide transporter. Polypeptide drugs are hydrolyzed by brush border membrane proteolytic enzymes to di-/tripeptides and amino acids. Therefore, while the intestinal brush border membrane has a carrier system facilitating the absorption of di-/tripeptide drugs, it is a major barrier limiting oral availability of polypeptide drugs. In this paper, the specificity of peptide transport and metabolism in the intestinal brush border membrane is reviewed.
ISSN:0724-8741
1573-904X
DOI:10.1023/a:1015885823793