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

被引:49
作者
Kitayama, Hiroki [1 ,2 ]
Takechi, Yuki [1 ,2 ]
Tamai, Nobutake [3 ]
Matsuki, Hitoshi [3 ]
Yomota, Chikako [4 ]
Saito, Hiroyuki [1 ,2 ]
机构
[1] Univ Tokushima, Inst Hlth Biosci, Tokushima 7708505, Japan
[2] Univ Tokushima, Grad Sch Pharmaceut Sci, Tokushima 7708505, Japan
[3] Univ Tokushima, Inst Sci & Technol, Dept Life Syst, Tokushima 7708506, Japan
[4] Natl Inst Hlth Sci, Setagaya Ku, Tokyo 1588501, Japan
关键词
liposome; cholesterol; phase diagram; differential scanning calorimetry; Prodan; DIFFERENTIAL SCANNING CALORIMETRY; X-RAY-DIFFRACTION; PRODAN FLUORESCENCE; BILAYER-MEMBRANE; PHOSPHOLIPIDS; WATER; TRANSITION; MODEL; PRESSURE; DPPC;
D O I
10.1248/cpb.c13-00587
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
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 (X-ch)=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 X-ch=0.40 in the DSC thermograms, indicating the existence of single liquid ordered phase at X-ch>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.
引用
收藏
页码:58 / 63
页数:6
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