Absorption of poorly water soluble drugs subject to apical efflux using phospholipids as solubilizers in the Caco-2 cell model

• Published in: European journal of pharmaceutics and biopharmaceutics Vol. 66; no. 1; pp. 146 - 158
• Main Authors: Kapitza, Susanne B., Michel, Bettina R., van Hoogevest, Peter, Leigh, Mathew L.S., Imanidis, Georgios
• Format: Journal Article
• Language: English
• Published: Amsterdam Elsevier B.V 01.04.2007; Elsevier Science
• Subjects: Absorption; Biological and medical sciences; Biological Transport; Caco-2; Caco-2 Cells; Cell Membrane Permeability; Cell Survival - drug effects; Chromatography, High Pressure Liquid; Dose-Response Relationship, Drug; Drug absorption; Efflux; General pharmacology; HIV Protease Inhibitors - chemistry; HIV Protease Inhibitors - pharmacokinetics; HIV-protease inhibitors; Humans; Hydrophobic and Hydrophilic Interactions; Indinavir - chemistry; Indinavir - pharmacokinetics; Kinetic modeling; Liposomes; Liposomes - chemistry; Medical sciences; Models, Theoretical; Pharmaceutical Preparations - chemistry; Pharmaceutical Preparations - metabolism; Pharmaceutical technology. Pharmaceutical industry; Pharmacology. Drug treatments; Phospholipids; Phospholipids - chemistry; Regression Analysis; Saquinavir - chemistry; Saquinavir - pharmacokinetics; Solubility; Time Factors; Efflux; Kinetic modeling; Caco-2; Drug absorption; Phospholipids; HIV-protease inhibitors; Liposomes; Drug; Antiretroviral agent; Pharmaceutical technology; Gut; Liposome; Phospholipid; Modeling; Water solubility; Antiviral; Water absorption; Kinetics; Protease inhibitor

The purpose of this work was to determine the influence of liposomal solubilization of poorly water soluble drugs exhibiting apical efflux on permeation kinetics and cell toxicity in Caco-2 cells. The HIV-protease inhibitors indinavir and saquinavir were incorporated in phosphatidylcholine liposomes...