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温度敏感脂质体在甲氨蝶呤和顺铂类似物向小鼠膀胱肿瘤的选择性递送中的应用。

Use of temperature-sensitive liposomes in the selective delivery of methotrexate and cis-platinum analogues to murine bladder tumor.

作者信息

Bassett J B, Anderson R U, Tacker J R

出版信息

J Urol. 1986 Mar;135(3):612-5. doi: 10.1016/s0022-5347(17)45761-2.

Abstract

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.

摘要

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。

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