Roles of adriamycin and adriamycin dimer in antitumor activity of the polymeric micelle carrier system

被引：28

作者：

Fukushima, S

Machida, M

Akutsu, T

Skimizu, K

Tanaka, S

Okamoto, K

Mashiba, H

Yokoyama, M

Okano, T

Sakurai, Y

Kataoka, K

机构：

[1] Nippon Kayaku Co Ltd, Takasaki, Gumma 3701208, Japan

[2] Nippon Kayaku Co Ltd, Kita Ku, Tokyo 1158588, Japan

[3] Tokyo Womens Med Univ, Inst Biomed Engn, Shinjuku Ku, Tokyo 1620054, Japan

[4] Univ Tokyo, Grad Sch Engn, Dept Mat Sci, Bunkyo Ku, Tokyo 1138656, Japan

来源：

COLLOIDS AND SURFACES B-BIOINTERFACES | 1999年 / 16卷 / 1-4期

关键词：

adriamycin; adriamycin dimer; anticancer drug; drug targeting; polymeric micelle;

D O I：

10.1016/S0927-7765(99)00073-9

中图分类号：

Q6 [生物物理学];

学科分类号：

071011 ;

摘要：

Adriamycin (ADR) dimer was prepared and its antitumor activity was evaluated with mouse colon adenocarcinoma 26 (C 26). As compared with original ADR, the dimer did not show significant antitumor activity, either in vitro or in vivo. Furthermore, polymeric micelles containing varied ratios of the dimer to the original ADR were prepared. Polymeric micelles with a higher dimer/ADR ratio (9.7) showed significant antitumor activity, but the effective dose shifted higher. Effective doses were found to largely depend on the concentration of the original ADR, rather than that of the dimer at the tumor sites. Therefore, it was presumed that the original ADR played a major role in antitumor activity, and the dimer played a supplementary role to contribute selective delivery of ADR to the tumor sites. (C) 1999 Elsevier Science B.V. All rights reserved.

引用

页码：227 / 236

页数：10

共 25 条

[1] Anthracycline antibiotics non-covalently incorporated into the block copolymer micelles: In vivo evaluation of anti-cancer activity [J].