Enzymatic characterization of lipid-based drug delivery systems

Helena Ljusberg-Wahren; Flemming Seier Nielsen; Mattias Brogård; Emma Troedsson; Anette Müllertz

doi:10.1016/j.ijpharm.2005.02.038

Enzymatic characterization of lipid-based drug delivery systems

Helena Ljusberg-Wahren, Flemming Seier Nielsen, Mattias Brogård, Emma Troedsson, Anette Müllertz

41 Citations (Scopus)

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.

Original language	English
Journal	Internation Journal of Pharmaceutics
Volume	298
Issue number	2
Pages (from-to)	328-32
Number of pages	4
ISSN	0378-5173
DOIs	https://doi.org/10.1016/j.ijpharm.2005.02.038
Publication status	Published - 2005

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10.1016/j.ijpharm.2005.02.038

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title = "Enzymatic characterization of lipid-based drug delivery systems",

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 = "Helena Ljusberg-Wahren and {Seier Nielsen}, Flemming and Mattias Brog{\aa}rd and Emma Troedsson and Anette M{\"u}llertz",

note = "Keywords: Animals; Biopharmaceutics; Drug Delivery Systems; Emulsions; Lipase; Lipids; Lipolysis; Pancreas; Particle Size; Phenanthrenes; Probucol; Swine",

year = "2005",

doi = "10.1016/j.ijpharm.2005.02.038",

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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

SN - 0378-5173

VL - 298

SP - 328

EP - 332

JO - Internation Journal of Pharmaceutics

JF - Internation Journal of Pharmaceutics

IS - 2

ER -

Enzymatic characterization of lipid-based drug delivery systems

Abstract

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