Supercooled smectic nanoparticles

influence of the matrix composition and in vitro cytotoxicity

Judith Kuntsche, Michel H J Koch, Alfred Fahr, Heike Bunjes

Publikation: Bidrag til tidsskriftTidsskriftartikelForskningpeer review

Resumé

Cholesteryl nonanoate (CN), myristate (CM), palmitate (CP) and oleate (CO) alone or in combination were evaluated as matrix lipids for the preparation of supercooled smectic nanoparticles with a high stability against recrystallization during storage. The phase behavior of the cholesterol esters in the bulk was studied by polarizing light microscopy, differential scanning calorimetry (DSC) and small angle X-ray scattering (SAXS). Colloidal dispersions with pure and mixed cholesterol ester matrices were prepared by high-pressure melt homogenization and characterized by photon correlation spectroscopy, laser diffraction combined with polarizing intensity differential scattering, DSC and SAXS. The morphology of selected formulations was studied by freeze-fracture electron microscopy. All smectic nanoparticles with a mixed cholesterol ester matrix were stable against recrystallization when stored at room temperature. Nanoparticles with a pure CN and mixed CM/CN matrix with a high fraction of CN (60% of the whole lipid matrix) could even be stored at 4 degrees C for at least 18 months without any recrystallization. As smectic nanoparticles are studied especially with regard to parenteral administration of lipophilic drugs, the cytotoxicity of selected formulations was compared with that of a clinically used colloidal fat emulsion (Lipofundin MCT) in the murine fibroblast cell line L929 using the sulforhodamine B assay. The supercooled smectic nanoparticle formulations display a good overall cell compatibility although in some cases their cytotoxicity was slightly higher than that of Lipofundin MCT.
OriginalsprogEngelsk
TidsskriftEuropean Journal of Pharmaceutical Sciences
Vol/bind38
Udgave nummer3
Sider (fra-til)238-248
ISSN0928-0987
DOI
StatusUdgivet - 2009

Fingeraftryk

Cholesterol Esters
lissamine rhodamine B
X-Rays
Lipids
Palmitates
Myristic Acid
Photons
Microscopy
Electron Microscopy
Fibroblasts
Fats
In Vitro Techniques
Cell Line
Pharmaceutical Preparations
Lipofundin

Citer dette

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title = "Supercooled smectic nanoparticles: influence of the matrix composition and in vitro cytotoxicity",
abstract = "Cholesteryl nonanoate (CN), myristate (CM), palmitate (CP) and oleate (CO) alone or in combination were evaluated as matrix lipids for the preparation of supercooled smectic nanoparticles with a high stability against recrystallization during storage. The phase behavior of the cholesterol esters in the bulk was studied by polarizing light microscopy, differential scanning calorimetry (DSC) and small angle X-ray scattering (SAXS). Colloidal dispersions with pure and mixed cholesterol ester matrices were prepared by high-pressure melt homogenization and characterized by photon correlation spectroscopy, laser diffraction combined with polarizing intensity differential scattering, DSC and SAXS. The morphology of selected formulations was studied by freeze-fracture electron microscopy. All smectic nanoparticles with a mixed cholesterol ester matrix were stable against recrystallization when stored at room temperature. Nanoparticles with a pure CN and mixed CM/CN matrix with a high fraction of CN (60{\%} of the whole lipid matrix) could even be stored at 4 degrees C for at least 18 months without any recrystallization. As smectic nanoparticles are studied especially with regard to parenteral administration of lipophilic drugs, the cytotoxicity of selected formulations was compared with that of a clinically used colloidal fat emulsion (Lipofundin MCT) in the murine fibroblast cell line L929 using the sulforhodamine B assay. The supercooled smectic nanoparticle formulations display a good overall cell compatibility although in some cases their cytotoxicity was slightly higher than that of Lipofundin MCT.",
keywords = "Animals, Cell Line, Tumor, Cell Survival, Chemistry, Pharmaceutical, Cold Temperature, Colloids, Crystallization, Cytotoxins, Fibroblasts, Mice, Nanoparticles, Particle Size, Phase Transition, X-Ray Diffraction",
author = "Judith Kuntsche and Koch, {Michel H J} and Alfred Fahr and Heike Bunjes",
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Supercooled smectic nanoparticles : influence of the matrix composition and in vitro cytotoxicity. / Kuntsche, Judith; Koch, Michel H J; Fahr, Alfred; Bunjes, Heike.

I: European Journal of Pharmaceutical Sciences, Bind 38, Nr. 3, 2009, s. 238-248.

Publikation: Bidrag til tidsskriftTidsskriftartikelForskningpeer review

TY - JOUR

T1 - Supercooled smectic nanoparticles

T2 - influence of the matrix composition and in vitro cytotoxicity

AU - Kuntsche, Judith

AU - Koch, Michel H J

AU - Fahr, Alfred

AU - Bunjes, Heike

PY - 2009

Y1 - 2009

N2 - Cholesteryl nonanoate (CN), myristate (CM), palmitate (CP) and oleate (CO) alone or in combination were evaluated as matrix lipids for the preparation of supercooled smectic nanoparticles with a high stability against recrystallization during storage. The phase behavior of the cholesterol esters in the bulk was studied by polarizing light microscopy, differential scanning calorimetry (DSC) and small angle X-ray scattering (SAXS). Colloidal dispersions with pure and mixed cholesterol ester matrices were prepared by high-pressure melt homogenization and characterized by photon correlation spectroscopy, laser diffraction combined with polarizing intensity differential scattering, DSC and SAXS. The morphology of selected formulations was studied by freeze-fracture electron microscopy. All smectic nanoparticles with a mixed cholesterol ester matrix were stable against recrystallization when stored at room temperature. Nanoparticles with a pure CN and mixed CM/CN matrix with a high fraction of CN (60% of the whole lipid matrix) could even be stored at 4 degrees C for at least 18 months without any recrystallization. As smectic nanoparticles are studied especially with regard to parenteral administration of lipophilic drugs, the cytotoxicity of selected formulations was compared with that of a clinically used colloidal fat emulsion (Lipofundin MCT) in the murine fibroblast cell line L929 using the sulforhodamine B assay. The supercooled smectic nanoparticle formulations display a good overall cell compatibility although in some cases their cytotoxicity was slightly higher than that of Lipofundin MCT.

AB - Cholesteryl nonanoate (CN), myristate (CM), palmitate (CP) and oleate (CO) alone or in combination were evaluated as matrix lipids for the preparation of supercooled smectic nanoparticles with a high stability against recrystallization during storage. The phase behavior of the cholesterol esters in the bulk was studied by polarizing light microscopy, differential scanning calorimetry (DSC) and small angle X-ray scattering (SAXS). Colloidal dispersions with pure and mixed cholesterol ester matrices were prepared by high-pressure melt homogenization and characterized by photon correlation spectroscopy, laser diffraction combined with polarizing intensity differential scattering, DSC and SAXS. The morphology of selected formulations was studied by freeze-fracture electron microscopy. All smectic nanoparticles with a mixed cholesterol ester matrix were stable against recrystallization when stored at room temperature. Nanoparticles with a pure CN and mixed CM/CN matrix with a high fraction of CN (60% of the whole lipid matrix) could even be stored at 4 degrees C for at least 18 months without any recrystallization. As smectic nanoparticles are studied especially with regard to parenteral administration of lipophilic drugs, the cytotoxicity of selected formulations was compared with that of a clinically used colloidal fat emulsion (Lipofundin MCT) in the murine fibroblast cell line L929 using the sulforhodamine B assay. The supercooled smectic nanoparticle formulations display a good overall cell compatibility although in some cases their cytotoxicity was slightly higher than that of Lipofundin MCT.

KW - Animals

KW - Cell Line, Tumor

KW - Cell Survival

KW - Chemistry, Pharmaceutical

KW - Cold Temperature

KW - Colloids

KW - Crystallization

KW - Cytotoxins

KW - Fibroblasts

KW - Mice

KW - Nanoparticles

KW - Particle Size

KW - Phase Transition

KW - X-Ray Diffraction

U2 - 10.1016/j.ejps.2009.07.012

DO - 10.1016/j.ejps.2009.07.012

M3 - Journal article

VL - 38

SP - 238

EP - 248

JO - European Journal of Pharmaceutical Sciences

JF - European Journal of Pharmaceutical Sciences

SN - 0928-0987

IS - 3

ER -