Ogawa Y, Toguchi H
Pharmaceutics Research Laboratories, Research & Development Division, Takeda Chemical Industries, Ltd.
Gan To Kagaku Ryoho. 1990 Jun;17(6):1127-33.
The characteristics and feasibility of targeting therapy with combination of temperature-sensitive liposomes entrapped antitumor drug with localized hyperthermia were discussed on the theoretical as well as experimental basis. An optimum liposome form and a drug for this delivery were proposed as follows: the liposome is LUV which has a phase transition temperature of 41 to 42 degree and the osmotic pressure of the internal aqueous phase is 1.5 or higher than the physiological one, the drug has a large body clearance and has a synergistic effect with hyperthermia. The LUV preparation containing cisplatin was administered to mice together with tumor heating. The uptake of the drug in the tumor (as a criterion of targeting) were 3 to 5 times greater than those of an aqueous cisplatin solution. The tumor responses were well correlated with the drug-targeting.
在理论和实验基础上，探讨了温度敏感脂质体包裹抗肿瘤药物联合局部热疗靶向治疗的特点和可行性。提出了适合这种给药方式的最佳脂质体形式和药物：脂质体为大单层囊泡（LUV），其相变温度为41至42摄氏度，内部水相渗透压为1.5或高于生理渗透压，药物具有较大的体内清除率且与热疗有协同作用。将含顺铂的LUV制剂与肿瘤加热一起给予小鼠。肿瘤中药物的摄取量（作为靶向的标准）比顺铂水溶液高3至5倍。肿瘤反应与药物靶向性密切相关。
