PREPARATION OF MICELLE-FORMING POLYMER DRUG CONJUGATES
PREPARATION OF MICELLE-FORMING POLYMER DRUG CONJUGATES
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DOI：
10.1021/bc00016a007
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发表时间：
1992-07-01
影响因子：
4.7
通讯作者：
KATAOKA, K
中科院分区：
文献类型：
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作者：
YOKOYAMA, M;KWON, GS;KATAOKA, K
将疏水抗癌药物阿霉素与聚环氧乙烷-聚天冬氨酸嵌段共聚物偶联，嵌段共聚物的分子量分别为1000 ~ 12000和10 ~ 80个单位。通过调整嵌段共聚物中阿霉素与天冬氨酸残基的比例和用于反应的DMF的量，在没有沉淀的情况下实现了偶联。这样得到的缀合物显示出高水溶性，而不考虑大量的缀合阿霉素。此外，发现这些共轭物形成具有疏水内核和亲水外壳的胶束结构。这种胶束结构可用于有效的药物靶向。
Adriamycin, a hydrophobic anticancer drug, was conjugated with poly(ethylene oxide)-poly(aspartic acid) block copolymers composed of various lengths of each block copolymer segment ranging from 1000 to 12 000 in molecular weight and from 10 to 80 units, respectively. Conjugation was achieved without precipitation by adjusting the ratio of adriamycin to aspartic acid residues of the block copolymer and the quantity of DMF used for the reaction. Thus obtained conjugates showed high water solubility irrespective of a large amount of the conjugated adriamycin. Furthermore, these conjugates were found to form micellar structures with a hydrophobic inner core and a hydrophilic outer shell. This micellar architecture may be utilized for effective drug targeting.