| Project/Area Number |
61870091
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| Research Category |
Grant-in-Aid for Developmental Scientific Research
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| Allocation Type | Single-year Grants |
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| Research Field |
Physical pharmacy
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| Research Institution | Toyama Medical and Pharmaceutical University |
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Principal Investigator |
HORIKOSHI Isamu Department of Hospital Pharmacy Toyama Medical and Pharmaceutical University, Professor, 附属病院, 教授 (70019123)
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| Co-Investigator(Kenkyū-buntansha) |
ADACHI Isao Department of Hospital Pharmacy Toyama Medical and Pharmaceutical University, Re, 附属病院, 助手 (30151070)
UENO Masaharu Department of Hospital Pharmacy Toyama Medical and Pharmaceutical University, As, 附属病院, 助教授 (40080197)
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| Project Period (FY) |
1986 – 1988
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| Project Status |
Completed (Fiscal Year 1988)
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| Budget Amount *help |
¥4,400,000 (Direct Cost: ¥4,400,000)
Fiscal Year 1988: ¥900,000 (Direct Cost: ¥900,000)
Fiscal Year 1987: ¥1,200,000 (Direct Cost: ¥1,200,000)
Fiscal Year 1986: ¥2,300,000 (Direct Cost: ¥2,300,000)
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| Keywords | Liposome / Thermo-Sensitive Liposome / Fibrinolytic Activity / Thermo-Sensitivity / Thrombosis / 新剤型 / ウロキナーゼ / 局所加温 / REV / リポゾーム / 温度感受性リポゾーム / 線溶酵素 / 相転移温度 / 人工血栓 / 界面活性剤除去法 |
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| Research Abstract |
Properties of thermo-sensitive liposome were studied. The drug release from DPPC liposome (dipalmitoyl phosphatidylcholine liposome) was confirmed to increase abruptly near its phase transition temperature both for low molecular and high molecular drugs. The amount of thermo-sensitive drug release from the liposome was dependent on the method of the liposome preparation, and the release from rev (reverse phase evaporated vesicle) was the highest, next was from LUV (large unilamella vesicle), and lowest was from suv (small unilamella vesicle). rev was fractionated into 3 groups according to their average size and calcein release for each group was measured. The temperature, at which calcein release showed maximum, was almost the same with each other in 3 groups, but as the average liposome size of the group was larger, the rate of calcein release was higher and the temperature, at which calcein release began, was lower. The amount of release of a drug entrapped was simply more dependent on the molecular weight of the drug than the sort of the drug.
Thermo-sensitive release of urokinase (UK) encapsulated in REV, which has known to have the highest thermo-sensitivive release of both low and high molecular compounds, was studied for in vitro and in vivo systems. In both systems, the amount of UK release was lower than that of calcein release, but the pattern of uk release was similar with that of calcein release. UK-encapsulating REV showed the remarkable thermo-sensitive fibrinolytic activity on a model thrombosis in vitro. from above results, it was shown that the thermo-sensitive liposome encapsulating a fiblinolytic enzyme has a possibility as a new dosage form for treating a thrombosis.
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