Yatvin M B, Weinstein J N, Dennis W H, Blumenthal R
Science. 1978 Dec 22;202(4374):1290-3. doi: 10.1126/science.364652.
Liposomes can be designed to release an entrapped drug preferentially at temperatures attainable by mild local hyperthermia. In a test system in vitro, protein synthesis by Escherichia coli is inhibited and killing of the cells is enhanced by heating neomycin-containing liposomes to their phase transition temperature to maximize drug release. In the presence of serum the ratio of release at 44 degrees C to that at 37 degrees C can be made greater than 100:1, suggesting possible applications in the treatment of tumors or local infection.
脂质体可以设计成在温和的局部热疗可达到的温度下优先释放包裹的药物。在体外测试系统中,将含新霉素的脂质体加热到其相变温度以最大化药物释放,可抑制大肠杆菌的蛋白质合成并增强细胞杀伤作用。在有血清存在的情况下,44摄氏度时的释放量与37摄氏度时的释放量之比可大于100:1,这表明在肿瘤治疗或局部感染治疗中可能有应用前景。