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

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 diagra...

Full description

Saved in:
Bibliographic Details
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
Citations: Items that cite this one
Online Access:Get full text
Tags: Add Tag
No Tags, Be the first to tag this record!
Description
Summary: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.
ISSN:0378-5173
1873-3476
DOI:10.1016/j.ijpharm.2006.08.022