Enzymatic characterization of lipid-based drug delivery systems
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Enzymatic characterization of lipid-based drug delivery systems. / Ljusberg-Wahren, Helena; Seier Nielsen, Flemming; Brogård, Mattias; Troedsson, Emma; Müllertz, Anette.
In: Internation Journal of Pharmaceutics, Vol. 298, No. 2, 2005, p. 328-32.Research output: Contribution to journal › Journal article › peer-review
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TY - JOUR
T1 - Enzymatic characterization of lipid-based drug delivery systems
AU - Ljusberg-Wahren, Helena
AU - Seier Nielsen, Flemming
AU - Brogård, Mattias
AU - Troedsson, Emma
AU - Müllertz, Anette
N1 - Keywords: Animals; Biopharmaceutics; Drug Delivery Systems; Emulsions; Lipase; Lipids; Lipolysis; Pancreas; Particle Size; Phenanthrenes; Probucol; Swine
PY - 2005
Y1 - 2005
N2 - 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.
AB - 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.
U2 - 10.1016/j.ijpharm.2005.02.038
DO - 10.1016/j.ijpharm.2005.02.038
M3 - Journal article
C2 - 15979260
VL - 298
SP - 328
EP - 332
JO - International Journal of Pharmaceutics
JF - International Journal of Pharmaceutics
SN - 0378-5173
IS - 2
ER -
ID: 9012768