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标题：Properties of Water-Insoluble Mitomycin C-Albumin Conjugate as a Sustained Release Drug Delivery System in Mice Inoculated with Sarcoma 180
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作者：Tetsuro TANAKA ; Yoshiharu KANEO ; Masahide MIYASHITA 等
期刊名称：Biological and Pharmaceutical Bulletin
印刷版ISSN：0918-6158
电子版ISSN：1347-5215
出版年度：1995
卷号：18
期号：12
页码：1724-1728
DOI：10.1248/bpb.18.1724
出版社：The Pharmaceutical Society of Japan
摘要：In order to improve the deposition of mitomycin C (MMC) in the administered site, water-insoluble mitomycin C-albumin conjugate (MMC-G-BSA) was prepared. MMC was covalently attached to the glutarylated bovine serum albumin (G-BSA) in the presence of 1-ethyl-3-(3-dimethyl-aminopropyl) carbodiimide hydrochloride (EDC) to give MMC-G-BSA. The MMC content of the conjugate (16.3% (w/w)) was higher than that of water-soluble mitomycin C-albumin conjugates. MMC was liberated from MMC-G-BSA suspended in a phosphate buffer (pH 7.4, 37°C) with a half-life of 155.3 h. In the same buffer system containing α-chymotrypsin, MMC-G-BSA was dissolved perfectly within 24h due to enzymatic degradation, and the liberation of MMC from the conjugate was significantly accelerated (t_1/2=24.5 h). After intraperitoneal injection in mice, most of the MMC-G-BSA was retained in the abdominal cavity. Furthermore, the survival time of mice inoculated with Sarcoma 180 was significantly increased by the intraperitoneal injection of MMC-G-BSA. These findings suggest that MMC-G-BSA is a biodegradable macromolecular hybrid which acts as a sustained release delivery system of MMC.
关键词：macromolecular conjugate;mitomycin C;serum albumin;drug release;antitumor activity;Sarcoma 180