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Enzymatic characterization of lipid-based drug delivery systems

Ljusberg, Helena LU ; Nielsen, F S; Brogard, M; Troedsson, Emma and Mullertz, A (2005) In International Journal of Pharmaceutics 298(2). p.328-332
Abstract
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... (More)
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. (Less)
Please use this url to cite or link to this publication:
author
organization
publishing date
type
Contribution to journal
publication status
published
subject
keywords
Self-microemulsifying drug delivery system, Lipolysis, Probucol, Halofantrine
in
International Journal of Pharmaceutics
volume
298
issue
2
pages
328 - 332
publisher
Elsevier
external identifiers
  • pmid:15979260
  • wos:000230856800008
  • scopus:21344438401
ISSN
1873-3476
DOI
10.1016/j.ijpharm.2005.02.038
language
English
LU publication?
yes
id
debf05ff-1b60-4564-bf92-4fe9e6bc33f2 (old id 152846)
date added to LUP
2007-07-18 15:38:46
date last changed
2017-10-08 03:31:51
@article{debf05ff-1b60-4564-bf92-4fe9e6bc33f2,
  abstract     = {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.},
  author       = {Ljusberg, Helena and Nielsen, F S and Brogard, M and Troedsson, Emma and Mullertz, A},
  issn         = {1873-3476},
  keyword      = {Self-microemulsifying drug delivery system,Lipolysis,Probucol,Halofantrine},
  language     = {eng},
  number       = {2},
  pages        = {328--332},
  publisher    = {Elsevier},
  series       = {International Journal of Pharmaceutics},
  title        = {Enzymatic characterization of lipid-based drug delivery systems},
  url          = {http://dx.doi.org/10.1016/j.ijpharm.2005.02.038},
  volume       = {298},
  year         = {2005},
}