Bassett J B, Anderson R U, Tacker J R
J Urol. 1986 Mar;135(3):612-5. doi: 10.1016/s0022-5347(17)45761-2.
This report describes the release of methotrexate and cis-platinum analogues JM8 and JM9 from phase transition liposomes. Large unilamellar liposomes were able to quickly release the antineoplastic agents employed during in vitro tests. Methotrexate exhibited a 73 per cent release in one second. The cis-platinum analogues JM8 and JM9 were slower, showing 43.5 per cent and 33.5 per cent release at two seconds. In vivo experiments utilizing MBT-2 transitional cell carcinoma-bearing mice were conducted. Methotrexate delivered by the liposome complex showed an 8.4-fold increase in heated tumor uptake when compared to unheated tumors.
本报告描述了甲氨蝶呤和顺铂类似物JM8和JM9从相变脂质体中的释放情况。大单层脂质体能够在体外测试期间快速释放所使用的抗肿瘤药物。甲氨蝶呤在一秒内释放率为73%。顺铂类似物JM8和JM9释放较慢,在两秒时释放率分别为43.5%和33.5%。利用携带MBT - 2移行细胞癌的小鼠进行了体内实验。与未加热的肿瘤相比,脂质体复合物递送的甲氨蝶呤在加热肿瘤中的摄取量增加了8.4倍。