ドキソルビシン封入温度感受性リポソームに関する基礎的研究

概要

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We prepared temperature-sensitive liposomes containing doxorubicin (DXR) which release the drug at 42℃ required for local hyperthermia. The liposomes were prepared by mixing dipalmitoylphosphatidylcholine (DPPC) with distearoylphosphatidylcholine (DSPC) and cholesterol, according to the procedure of the reverse-phase evaporation method. The drug-releasing properties of the large unilamellar liposomes were measured at 36 to 42℃ around the phase transition temperature of the liposomal lipids. The addition of cholesterol reduced the membrane permeability of the liposomes and completely eliminated DXR release at 50 mol%. The liposomes composed of DPPC alone released approximately 80% of DXR at 39℃. DPPC liposomes containing 20 mol% DSPC, however, showed a sharp increase in DXR release between 40℃ and 42℃. At 42℃, the level of DXR release was approximately 90%. These results indicated that the lipid composition of DPPC/ DSPC=4/1 (molar ratio) was optimum for temperature-sensitive DXR release.
日本医療薬学会の論文
1991-06-20