Corticosteroid solubility and lilpid polarity control release from solid lipid nanoparticles

Louise B. Jensen; Emily Magnusson; Linda Gunnarsson; Charlotte Vermehren; Hanne Mørck Nielsen; Karsten Petersson

doi:10.1016/j.ijpharm.2009.10.022

Corticosteroid solubility and lilpid polarity control release from solid lipid nanoparticles

Louise B. Jensen, Emily Magnusson, Linda Gunnarsson, Charlotte Vermehren, Hanne Mørck Nielsen, Karsten Petersson

73 Citations (Scopus)

Abstract

Solid lipid nanoparticles (SLN) show promise as a drug delivery system for skin administration. The solid state of the lipid particle enables efficient drug encapsulation and controlled drug release. The present study addresses the influence of lipid composition and drug substance lipid solubility on the in vitro release profile of corticosteroids from SLN for topical administration. Firstly, the effect of lipid composition on the lipid solubility and in vitro release of betamethasone-17-valerate (BMV) was determined by varying the lipid monoglyceride content and the chain length of the fatty acid moiety. Secondly, the effect of drug substance physicochemical properties was determined by studying five different corticosteroid derivatives with different lipophilicity. A high concentration of monoglyceride in SLN increased the amount of BMV released. The corticosteroid release rate depended on the drug substance lipophilicity and it was clear that the release profiles depended on drug partitioning to the aqueous phase as indicated by zero order kinetics. The results emphasize that the corticosteroid solubility in the lipid phase greatly influence drug distribution in the lipid particles and release properties. Thus knowledge of drug substance solubility and lipid polarity contributes to optimize SLN release properties.

Original language	English
Journal	Internation Journal of Pharmaceutics
Volume	390
Issue number	1
Pages (from-to)	53-60
ISSN	0378-5173
DOIs	https://doi.org/10.1016/j.ijpharm.2009.10.022
Publication status	Published - May 2010

Keywords

Former Faculty of Pharmaceutical Sciences

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10.1016/j.ijpharm.2009.10.022

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title = "Corticosteroid solubility and lilpid polarity control release from solid lipid nanoparticles",

abstract = "Solid lipid nanoparticles (SLN) show promise as a drug delivery system for skin administration. The solid state of the lipid particle enables efficient drug encapsulation and controlled drug release. The present study addresses the influence of lipid composition and drug substance lipid solubility on the in vitro release profile of corticosteroids from SLN for topical administration. Firstly, the effect of lipid composition on the lipid solubility and in vitro release of betamethasone-17-valerate (BMV) was determined by varying the lipid monoglyceride content and the chain length of the fatty acid moiety. Secondly, the effect of drug substance physicochemical properties was determined by studying five different corticosteroid derivatives with different lipophilicity. A high concentration of monoglyceride in SLN increased the amount of BMV released. The corticosteroid release rate depended on the drug substance lipophilicity and it was clear that the release profiles depended on drug partitioning to the aqueous phase as indicated by zero order kinetics. The results emphasize that the corticosteroid solubility in the lipid phase greatly influence drug distribution in the lipid particles and release properties. Thus knowledge of drug substance solubility and lipid polarity contributes to optimize SLN release properties.",

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T1 - Corticosteroid solubility and lilpid polarity control release from solid lipid nanoparticles

AU - Jensen, Louise B.

AU - Magnusson, Emily

AU - Gunnarsson, Linda

AU - Vermehren, Charlotte

AU - Nielsen, Hanne Mørck

AU - Petersson, Karsten

PY - 2010/5

Y1 - 2010/5

N2 - Solid lipid nanoparticles (SLN) show promise as a drug delivery system for skin administration. The solid state of the lipid particle enables efficient drug encapsulation and controlled drug release. The present study addresses the influence of lipid composition and drug substance lipid solubility on the in vitro release profile of corticosteroids from SLN for topical administration. Firstly, the effect of lipid composition on the lipid solubility and in vitro release of betamethasone-17-valerate (BMV) was determined by varying the lipid monoglyceride content and the chain length of the fatty acid moiety. Secondly, the effect of drug substance physicochemical properties was determined by studying five different corticosteroid derivatives with different lipophilicity. A high concentration of monoglyceride in SLN increased the amount of BMV released. The corticosteroid release rate depended on the drug substance lipophilicity and it was clear that the release profiles depended on drug partitioning to the aqueous phase as indicated by zero order kinetics. The results emphasize that the corticosteroid solubility in the lipid phase greatly influence drug distribution in the lipid particles and release properties. Thus knowledge of drug substance solubility and lipid polarity contributes to optimize SLN release properties.

AB - Solid lipid nanoparticles (SLN) show promise as a drug delivery system for skin administration. The solid state of the lipid particle enables efficient drug encapsulation and controlled drug release. The present study addresses the influence of lipid composition and drug substance lipid solubility on the in vitro release profile of corticosteroids from SLN for topical administration. Firstly, the effect of lipid composition on the lipid solubility and in vitro release of betamethasone-17-valerate (BMV) was determined by varying the lipid monoglyceride content and the chain length of the fatty acid moiety. Secondly, the effect of drug substance physicochemical properties was determined by studying five different corticosteroid derivatives with different lipophilicity. A high concentration of monoglyceride in SLN increased the amount of BMV released. The corticosteroid release rate depended on the drug substance lipophilicity and it was clear that the release profiles depended on drug partitioning to the aqueous phase as indicated by zero order kinetics. The results emphasize that the corticosteroid solubility in the lipid phase greatly influence drug distribution in the lipid particles and release properties. Thus knowledge of drug substance solubility and lipid polarity contributes to optimize SLN release properties.

KW - Former Faculty of Pharmaceutical Sciences

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DO - 10.1016/j.ijpharm.2009.10.022

M3 - Journal article

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SP - 53

EP - 60

JO - International Journal of Pharmaceutics

JF - International Journal of Pharmaceutics

IS - 1

ER -

Corticosteroid solubility and lilpid polarity control release from solid lipid nanoparticles

Abstract

Keywords

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