天冬氨酸
溶解度
胶束
共聚物
化学
阿霉素
乙二醇
共轭体系
药物输送
临界胶束浓度
PEG比率
毒品携带者
高分子化学
细胞毒性
体内
聚合物
有机化学
体外
聚乙二醇
纳米载体
核化学
癌细胞
水溶液
氨基酸
生物化学
财务
经济
作者
Masayuki Yokoyama,Mizue Miyauchi,Noriko Yamada,Teruo Okano,Yasuhisa Sakurai,Kazunori Kataoka,Shohei Inoue
出处
期刊:Cancer Research
[American Association for Cancer Research]
日期:1990-03-15
卷期号:50 (6): 1693-700
被引量:88
摘要
Adriamycin (ADR), an anthracycline anticancer drug, was bound to the poly(aspartic acid) chain of poly(ethylene glycol)-poly(aspartic acid) block copolymer by amide bond formation between an amino group of Adriamycin and the carboxyl groups of the poly(aspartic acid) chain. The polymeric drug thus obtained was observed to form a micelle structure possessing diameter of approximately 50 nm, with a narrow distribution, in phosphate-buffered saline and to show excellent water solubility despite a large amount of ADR introduction. Further, it was able to be stored in lyophilized form without losing its water solubility in the redissolving procedure. Increased stability of the bound Adriamycin molecules in phosphate-buffered saline and elimination of binding affinity for bovine serum albumin due to the micelle formation were further advantages of this polymeric drug. In vivo high anticancer activity of this micelle-forming polymeric drug against P 388 mouse leukemia was obtained with less body weight loss than that seen with free ADR, due to low toxicity as compared with free ADR.
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