Polymer micelles as novel drug carrier: Adriamycin-conjugated poly(ethylene glycol)-poly(aspartic acid) block copolymer
Polymer micelles as novel drug carrier: Adriamycin-conjugated poly(ethylene glycol)-poly(aspartic acid) block copolymer
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DOI：
10.1016/0168-3659(90)90139-k
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发表时间：
1990
影响因子：
10.8
通讯作者：
Yokoyama Masayuki;Miyauchi Mizue;Yamada Noriko;O. Teruo;Sakurai Yasuhisa;Kataoka Kazunori;Inoue Shohei-Inoue-Sh
中科院分区：
文献类型：
--
作者：
Yokoyama Masayuki;Miyauchi Mizue;Yamada Noriko;O. Teruo;Sakurai Yasuhisa;Kataoka Kazunori;Inoue Shohei-Inoue-Sh
以抗癌药物阿霉素和聚乙二醇-聚天冬氨酸嵌段共聚物为原料，合成了一种可形成胶束的高分子药物。胶束具有窄的单峰尺寸分布，其直径约为100 nm。50 nm，对应病毒的范围。这种胶束形成聚合物药物表现出良好的水溶性和良好的抗沉淀稳定性，而与大量的疏水阿霉素结合无关。通过改变嵌段共聚物中聚天冬氨酸链的长度，研究了该高分子药物对P-388小鼠白血病的体内抗癌活性。从治疗小鼠的存活期与对照小鼠的存活期之比（T/C）判断，该聚合物药物显示出良好的体内抗癌活性，且毒性低于阿霉素。这些结果表明，聚合物胶束作为新型药物载体是一个很有前途的数字。
A micelle-forming polymeric drug was synthesized using adriamycin (an anti-cancer drug) and poly(ethylene glycol)-poly(aspartic acid) block copolymers. The micelle had a narrow and unimodal size distribution, and its diameter was observed to be ca. 50 nm, the range corresponding to viruses. This micelle-forming polymeric drug exhibited good water solubility and good stability against precipitation irrespective of the large quantity of incorporated hydrophobie adriamycin. In vivoanti-cancer activity of this polymeric drug against P-388 mouse leukemia was studied by changing the length of the poly(aspartic acid) chain of the block copolymer. The polymeric drug showed excellentin vivoanti-cancer activity, judged from the ratio of the survival period of the treated mice to that of the control (T/C), with lower toxicity than that of adriamycin. These results point to a promising figure of polymeric micelles as novel drug carriers.