Novel poloxamer-based nanoemulsions to enhance the intestinal absorption of active compounds

• Published in: International journal of pharmaceutics 2007-02, Vol.329 (1), p.173-181
• Main Authors: Brüsewitz, Carsten, Schendler, Andreas, Funke, Adrian, Wagner, Torsten, Lipp, Ralph
• Format: Article
• Language: English
• Subjects: Absorption enhancer; Biological and medical sciences; Caco-2 Cells; Danazol - administration & dosage; Danazol - pharmacokinetics; Emulsions; Estrogen Antagonists - administration & dosage; Estrogen Antagonists - pharmacokinetics; General pharmacology; Humans; Intestines - metabolism; Medical sciences; Nanoemulsion; Nanomedicine; Particle Size; Pharmaceutical technology. Pharmaceutical industry; Pharmacology. Drug treatments; Poloxamer
• ISSN: 0378-5173; 1873-3476
• DOI: 10.1016/j.ijpharm.2006.08.022

On the basis of Pluronic ® P104 as primary emulsifier and Lauroglycol ® 90 as amphiphilic oil phase, two nanoemulsion systems were developed with Pluronic ® L62 or L81 as secondary emulsifiers. The possible nanoemulsion region of combinations of these excipients was described in ternary phase diagrams. Three formulations were selected from the nanoemulsion region and their potential impact on oral absorption was examined in the Caco-2 monolayer model of the small intestine. The apparent permeability of the BCS class III compound Atenolol was enhanced 2.5-fold, of BCS class II compound Danazol 3.2-fold and of BCS class I compound Metoprolol 1.4-fold. The three formulations were very well tolerated by the Caco-2 cells, which was confirmed by TEER measurements, a MTT test and a LDH release test.