Intestinal absorption-modifying excipients: A current update on preclinical in vivo evaluations.

Area of Science:

• Pharmacology
• Drug Delivery
• Biopharmaceutics

Background:

• Pharmaceutical excipients are typically inactive but can influence drug absorption.
• Absorption-modifying excipients (AMEs) are specifically used to enhance drug permeation across mucosal membranes.

Purpose of the Study:

• To review the mechanisms by which AMEs enhance intestinal drug absorption.
• To evaluate the suitability of preclinical models for assessing AME performance and clinical relevance.

Main Methods:

• Focus on in situ and in vivo intestinal absorption models for AME evaluation.
• Review of five key factors influencing AME efficacy and safety in preclinical studies.

Main Results:

• AMEs can significantly impact drug absorption rates and extent.
• Preclinical models need to account for AME dilution, transit, mucosal recovery, and variability for clinical validity.

Conclusions:

• Accurate preclinical assessment of AMEs is crucial for reliable bioequivalence studies and enabling oral delivery of challenging therapeutics.
• Failure to consider critical factors in preclinical models limits the clinical value of AME research.