Improving In Vitro–In Vivo Correlation (IVIVC) for Lipid-Based Formulations: Overcoming Challenges and Exploring Opportunities
Arnaud Bourderi-Cambon, Khaled Fadhlaoui, Ghislain Garrait, E Laine, Imen Dhifallah, Manon Rossano, Philippe Caisse, Eric Beyssac
Abstract
Lipid-based formulations (LBFs) play a crucial role in enhancing the oral bioavailability of poorly water-soluble drugs by leveraging lipid digestion and solubilization processes. However, developing robust in vitro-in vivo correlations (IVIVCs) for LBFs presents unique challenges due to the complex interplay of digestion, permeation, and dynamic solubilization. This article reviews the construction of IVIVC in the context of LBFs, highlighting the limitations of traditional methods and the need for tailored approaches. It examines the in vitro tools commonly employed for LBF characterization, such as USP dissolution tests, lipolysis assays, and combined models, and discusses their relevance to in vivo performance prediction. The review also explores the sources of in vivo data essential for validating IVIVC and describes the most popular in silico tools for predicting in vivo performance, focusing on lipid-based formulations. This work aims to pave the way for more effective and adaptable IVIVC methodologies for lipid-based drug delivery systems.