High-molecular weight HPMA copolymer-adriamycin conjugates
High-molecular weight HPMA copolymer-adriamycin conjugates
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DOI：
10.1016/s0168-3659(99)00087-5
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发表时间：
1999-08-05
影响因子：
10.8
通讯作者：
Kopecek, J
中科院分区：
文献类型：
--
作者：
Dvorák, M;Kopecková, P;Kopecek, J
通过自由基共聚反应合成了含有溶酶体降解寡肽交联的高分子量（支化）水溶性N-（2-羟丙基）甲基丙烯酰胺（HPMA）共聚物。通过加入链转移剂3-巯基丙酸来控制主链的长度。将抗癌药物阿霉素（ADR）的可聚合衍生物N-甲基丙烯酰甘氨酰苯丙氨酰亮氨酰甘氨酰阿霉素（ADR）加入到某些聚合混合物中。这导致在高分子量，支化，水溶性HPMA共聚物中含有寡肽序列的交联以及在侧链终止于ADR。研究了交联剂的降解性以及从大鼠肝脏中分离的溶酶体酶对ADR的释放。(C)1999 Elsevier Science B. V.保留所有权利。
High-molecular weight (branched) water-soluble N-(2-hydroxypropyl)methacrylamide (HPMA) copolymers containing lysosomally degradable oligopeptide crosslinks were synthesized by radical copolymerization of HPMA and newly designed crosslinking agents, N-2,N-5-bis(N-methacryloylglycylphenylalanylleucylglycyl) with different modification of the carboxy group. The length of the primary chain was controlled by the addition of a chain transfer agent, 3-mercaptopropionic acid, A polymerizable derivative of the anticancer drug adriamycin (ADR), N-methacryloylglycylphenylalanylleucylglycyl adriamycin, was added to some polymerization mixtures. This resulted in high-molecular weight, branched, water-soluble HPMA copolymers containing oligopeptide sequences in the crosslinks as well as in side-chains terminated in ADR. The degradability of the crosslinks as well as the release of ADR by lysosomal enzymes isolated from rat liver were investigated. (C) 1999 Elsevier Science B.V. All rights reserved.