Enzymatic barriers to peptide and protein absorption

Area of Science:

• Biotechnology and Pharmaceutical Sciences
• Drug Delivery Systems

Background:

• Peptides and proteins represent a growing class of pharmaceuticals with potential for treating various diseases.
• Effective drug delivery remains a significant hurdle for the therapeutic success of these biomolecules.
• Enzymatic degradation poses a major barrier at multiple stages of peptide and protein delivery.

Purpose of the Study:

• To review the enzymatic barriers encountered during peptide and protein drug delivery.
• To examine strategies for overcoming these enzymatic degradation challenges.
• To assess various administration routes and their associated barriers.

Main Methods:

• Literature review of enzymatic barriers in peptide and protein delivery.
• Analysis of enzymatic degradation at different absorption sites.
• Evaluation of strategies to mitigate enzymatic activity and enhance delivery.

Main Results:

• Enzymatic barriers are present at administration sites, in circulation, and during metabolism/elimination.
• Various absorption sites (subcutaneous, intramuscular, intestinal, nasal, buccal, rectal, vaginal, ocular) present distinct enzymatic challenges.
• Strategies exist to perturb these barriers, improving peptide and protein bioavailability.

Conclusions:

• Overcoming enzymatic barriers is critical for the successful development of peptide and protein therapeutics.
• Understanding and targeting these barriers across diverse administration routes is essential for future drug design.
• Developing effective delivery strategies will unlock the full potential of biotechnologically derived pharmaceuticals.