Enzymatic characterization of lipid-based drug delivery systems

Helena Ljusberg; F S Nielsen; M Brogard; Emma Troedsson; A Mullertz

doi:10.1016/j.ijpharm.2005.02.038

Enzymatic characterization of lipid-based drug delivery systems

Helena Ljusberg, F S Nielsen, M Brogard, Emma Troedsson, A Mullertz

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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
Pages (from-to)	328-332
Journal	International Journal of Pharmaceutics
Volume	298
Issue number	2
DOIs	https://doi.org/10.1016/j.ijpharm.2005.02.038
Publication status	Published - 2005

Subject classification (UKÄ)

Other Engineering and Technologies

Free keywords

Self-microemulsifying drug delivery system
Lipolysis
Probucol
Halofantrine

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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.",

keywords = "Self-microemulsifying drug delivery system, Lipolysis, Probucol, Halofantrine",

author = "Helena Ljusberg and Nielsen, {F S} and M Brogard and Emma Troedsson and A Mullertz",

year = "2005",

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

language = "English",

volume = "298",

pages = "328--332",

journal = "International Journal of Pharmaceutics",

issn = "1873-3476",

publisher = "Elsevier",

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TY - JOUR

T1 - Enzymatic characterization of lipid-based drug delivery systems

AU - Ljusberg, Helena

AU - Nielsen, F S

AU - Brogard, M

AU - Troedsson, Emma

AU - Mullertz, A

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.

KW - Self-microemulsifying drug delivery system

KW - Lipolysis

KW - Probucol

KW - Halofantrine

U2 - 10.1016/j.ijpharm.2005.02.038

DO - 10.1016/j.ijpharm.2005.02.038

M3 - Article

SN - 1873-3476

VL - 298

SP - 328

EP - 332

JO - International Journal of Pharmaceutics

JF - International Journal of Pharmaceutics

IS - 2

ER -

Enzymatic characterization of lipid-based drug delivery systems

Abstract

Subject classification (UKÄ)

Free keywords

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