Lipid excipients to unlock oral bioavailability issues

Many active pharmaceutical ingredients have poor water-solubility and/or low permeability, leading to bioavailability issues. Lipid-based formulation (LBF) is a well-known strategy to overcome these hurdles and increase in vivo drug exposure. Depending on their composition, LBF exhibit different in vivo behaviors.

One of the main advantages of LBF is to present the drug in a solubilized state in the GI tract. As such, the drug molecule solubility and stability in the excipients will dictate the formulation type. Formulation design and excipient choices are also influenced by emulsification capacity in the GI tract, behavior upon digestion, the targeted route of drug absorption (lymphatic or systemic), and potential interactions of the drug with food. In all cases, careful selection of the lipid excipient(s) is necessary for increasing oral bioavailability.

A comprehensive and evidence-based review of the numerous ways in which LBF can enhance oral delivery of therapeutic molecules has been addressed in five chapters:

Chapter 1 describes how lipid-based formulations can increase oral bioavailability of poorly water-soluble APIs, considering their emulsification properties and their interactions with gastro-intestinal lipases
Chapter 2 discusses the physiological barriers limiting drug permeation, focusing on the potential for lipid formulations to increase intestinal absorption
Chapter 3 explains how certain lipid excipients can promote lymphatic absorption of highly lipophilic drugs
Chapter 4 summarizes how food-drug interactions can be mitigated with lipid-based formulations
Chapter 5 provides an overview of Gattefossé excipients used in lipid-based formulations to enhance oral bioavailability of drugs.

Download our e-book published by American Pharmaceutical Review here