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

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  • Kitayama Hiroki
    Institute of Health Biosciences and Graduate School of Pharmaceutical Sciences, The University of Tokushima
  • Takechi Yuki
    Institute of Health Biosciences and Graduate School of Pharmaceutical Sciences, The University of Tokushima
  • Tamai Nobutake
    Department of Life System, Institute of Technology and Science, The University of Tokushima
  • Matsuki Hitoshi
    Department of Life System, Institute of Technology and Science, The University of Tokushima
  • Yomota Chikako
    National Institute of Health Sciences
  • Saito Hiroyuki
    Institute of Health Biosciences and Graduate School of Pharmaceutical Sciences, The University of Tokushima

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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.

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