Intestinal permeation enhancers

Area of Science:

• Pharmacology
• Drug Delivery
• Biopharmaceutics

Background:

• Oral drug administration is limited by poor bioavailability of many compounds.
• Excipients that enhance intestinal membrane permeability offer a strategy to overcome this limitation.
• Evaluating these enhancers requires consideration of efficacy, influencing factors, toxicity, and mechanisms.

Purpose of the Study:

• To review excipients that improve oral bioavailability by increasing intestinal membrane permeability.
• To discuss critical factors in evaluating permeation enhancement strategies.
• To explore excipients that inhibit secretory transport.

Main Methods:

• Literature review of permeation enhancers.
• Categorization of enhancers including surfactants, fatty acids, glycerides, detergents, and polymers.
• Discussion of mechanisms and toxicity profiles.

Main Results:

• Various classes of excipients demonstrate potential for enhancing oral bioavailability.
• Some enhancers are in early clinical trials, showing promise for poorly absorbed drugs.
• Key considerations include bioavailability enhancement extent, formulation/physiological variables, toxicity, and mechanism.

Conclusions:

• Several permeation enhancers show potential for improving oral drug absorption.
• These excipients may increase bioavailability of poorly absorbed drugs with minimal intestinal damage.
• Inhibition of secretory transport is another potential strategy for bioavailability enhancement.