Enzymatic characterization of lipid-based drug delivery systems.
The present work introduces a simple and robust in vitro method for enzymatic characterisation of surface properties of lipid dispersions in aqueous media. The initial lipolysis rate in biorelevant media, using pancreatic lipase and a self-microemulsifying formulation (SMEDDS) containing digestible lipids as substrate, was determined. The impact of incorporating two sparingly water soluble model drugs, probucol and halofantrine, into the SMEDDS was studied. It was found that both model drugs reduced the initial rate of lipolysis compared with the vehicle, probucol having a larger effect than halofantrine. The reduction of initial lipolysis rate indicates that probucol and halofantrine are bound in the water/emulsion interface limiting the substrate availability.
Camurus AB, Ideon, Gamma 2, Sölvegatan 41, SE-223 70 Lund, Sweden.
Helena
H
Ljusberg-Wahren
Flemming
F
Seier Nielsen
Mattias
M
Brogård
Emma
E
Troedsson
Anette
A
Müllertz
D000818:Animals; D001702:Biopharmaceutics; D016503:Drug Delivery Systems; D004655:Emulsions; D008049:Lipase / Q000737:chemistry; D008055:Lipids / Q000737:chemistry*; D008066:Lipolysis; D010179:Pancreas / Q000201:enzymology; D010316:Particle Size; D010616:Phenanthrenes / Q000737:chemistry; D011341:Probucol / Q000737:chemistry; D013552:Swine
D004655:Emulsions; D008055:Lipids; D010616:Phenanthrenes; D008049:Lipase; D011341:Probucol; C023768:halofantrine