Peptide Bioavailability Challenges refer to the inherent difficulties in ensuring that therapeutic peptide molecules are effectively absorbed, remain structurally intact, and reach their target receptors in sufficient concentration to elicit a desired physiological effect. Peptides, being chains of amino acids, are often susceptible to rapid enzymatic degradation in the gastrointestinal tract and poor permeability across biological membranes. Overcoming these challenges is a major focus in clinical peptide administration.
Origin
This is a term from pharmaceutical science and clinical pharmacology, combining the biological molecule peptide with bioavailability, which quantifies the fraction of an administered dose that reaches the systemic circulation. The challenges component acknowledges the inherent instability of these molecules compared to small-molecule drugs.
Mechanism
The primary challenges arise from the enzymatic activity of proteases in the gut and liver, which rapidly break down the peptide structure before systemic absorption can occur. Furthermore, the large molecular size and hydrophilic nature of many peptides impede their passive diffusion across the lipid-rich cell membranes of the digestive tract. Clinical strategies, such as injectable administration or specialized oral delivery systems, are employed to circumvent these natural physiological barriers.
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