Thermotropic Phase Behavior of Hydrogenated Soybean Phosphatidylcholine–Cholesterol Binary Liposome Membrane

By combination of differential scanning calorimetry (DSC) and fluorescence spectroscopy of 6-propionyl-2-(dimethylamino)naphthalene (Prodan), we elucidated the thermotropic phase behavior of hydrogenated soybean phosphatidylcholine (HSPC)–cholesterol binary liposome membrane which has similar lipid...

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Published inChemical & pharmaceutical bulletin Vol. 62; no. 1; pp. 58 - 63
Main Authors Kitayama, Hiroki, Takechi, Yuki, Tamai, Nobutake, Matsuki, Hitoshi, Yomota, Chikako, Saito, Hiroyuki
Format Journal Article
LanguageEnglish
Japanese
Published Japan The Pharmaceutical Society of Japan 01.01.2014
Pharmaceutical Society of Japan
Japan Science and Technology Agency
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Abstract By combination of differential scanning calorimetry (DSC) and fluorescence spectroscopy of 6-propionyl-2-(dimethylamino)naphthalene (Prodan), we elucidated the thermotropic phase behavior of hydrogenated soybean phosphatidylcholine (HSPC)–cholesterol binary liposome membrane which has similar lipid composition to Doxil®, the widely used liposome product in treatment of various tumors. We found that the characteristic points at cholesterol mole fraction (Xch)=0.023 and 0.077 correspond to the hexagonal lattice, in which cholesterol molecules are considered to be regularly distributed in all regions of HSPC lipid bilayer with 1 : 42 and 1 : 12 units, respectively, as static averaged structures. Apparent endothermic peak disappeared at Xch=0.40 in the DSC thermograms, indicating the existence of single liquid ordered phase at Xch>0.40. In addition, fluorescence measurements of Prodan and its lauroyl derivative in poly(ethylene glycol) (PEG)-modified liposomes indicated that PEG modification has a negligible effect on the phase behavior of HSPC–cholesterol binary liposome membrane. These results may provide useful information in developing novel liposome products whose stability and encapsulated drug release are controlled.
AbstractList By combination of differential scanning calorimetry (DSC) and fluorescence spectroscopy of 6-propionyl-2-(dimethylamino)naphthalene (Prodan), we elucidated the thermotropic phase behavior of hydrogenated soybean phosphatidylcholine (HSPC)-cholesterol binary liposome membrane which has similar lipid composition to Doxil(R), the widely used liposome product in treatment of various tumors. We found that the characteristic points at cholesterol mole fraction (Xch)=0.023 and 0.077 correspond to the hexagonal lattice, in which cholesterol molecules are considered to be regularly distributed in all regions of HSPC lipid bilayer with 1:42 and 1:12 units, respectively, as static averaged structures. Apparent endothermic peak disappeared at Xch=0.40 in the DSC thermograms, indicating the existence of single liquid ordered phase at Xch>0.40. In addition, fluorescence measurements of Prodan and its lauroyl derivative in poly(ethylene glycol) (PEG)-modified liposomes indicated that PEG modification has a negligible effect on the phase behavior of HSPC-cholesterol binary liposome membrane. These results may provide useful information in developing novel liposome products whose stability and encapsulated drug release are controlled.
By combination of differential scanning calorimetry (DSC) and fluorescence spectroscopy of 6-propionyl-2-(dimethylamino)naphthalene (Prodan), we elucidated the thermotropic phase behavior of hydrogenated soybean phosphatidylcholine (HSPC)-cholesterol binary liposome membrane which has similar lipid composition to Doxil®, the widely used liposome product in treatment of various tumors. We found that the characteristic points at cholesterol mole fraction (Xch)=0.023 and 0.077 correspond to the hexagonal lattice, in which cholesterol molecules are considered to be regularly distributed in all regions of HSPC lipid bilayer with 1 : 42 and 1 : 12 units, respectively, as static averaged structures. Apparent endothermic peak disappeared at Xch=0.40 in the DSC thermograms, indicating the existence of single liquid ordered phase at Xch>0.40. In addition, fluorescence measurements of Prodan and its lauroyl derivative in poly(ethylene glycol) (PEG)-modified liposomes indicated that PEG modification has a negligible effect on the phase behavior of HSPC-cholesterol binary liposome membrane. These results may provide useful information in developing novel liposome products whose stability and encapsulated drug release are controlled.
Author Kitayama, Hiroki
Saito, Hiroyuki
Tamai, Nobutake
Takechi, Yuki
Matsuki, Hitoshi
Yomota, Chikako
Author_xml – sequence: 1
  fullname: Kitayama, Hiroki
  organization: Institute of Health Biosciences and Graduate School of Pharmaceutical Sciences, The University of Tokushima
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  fullname: Takechi, Yuki
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  fullname: Tamai, Nobutake
  organization: Department of Life System, Institute of Technology and Science, The University of Tokushima
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  fullname: Matsuki, Hitoshi
  organization: Department of Life System, Institute of Technology and Science, The University of Tokushima
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  fullname: Yomota, Chikako
  organization: National Institute of Health Sciences
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  fullname: Saito, Hiroyuki
  organization: Institute of Health Biosciences and Graduate School of Pharmaceutical Sciences, The University of Tokushima
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Snippet By combination of differential scanning calorimetry (DSC) and fluorescence spectroscopy of 6-propionyl-2-(dimethylamino)naphthalene (Prodan), we elucidated the...
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SubjectTerms cholesterol
Cholesterol - chemistry
differential scanning calorimetry
Fluorescence
Glycine max - chemistry
Lipid Bilayers - chemistry
liposome
Liposomes - chemistry
Membranes - chemistry
phase diagram
Phosphatidylcholines - chemistry
Prodan
Title Thermotropic Phase Behavior of Hydrogenated Soybean Phosphatidylcholine–Cholesterol Binary Liposome Membrane
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