RELEASE BEHAVIOR OF 5-FLUOROURACIL FROM CHITOSAN-GEL MICROSPHERES IMMOBILIZING 5-FLUOROURACIL DERIVATIVE COATED WITH POLYSACCHARIDES AND THEIR CELL SPECIFIC RECOGNITION

被引：85

作者：

OHYA, Y

TAKEI, T

KOBAYASHI, H

OUCHI, T

机构：

[1] Department of Applied Chemistry, Faculty of Engineering, Kansai University, Suita, Osaka

来源：

JOURNAL OF MICROENCAPSULATION | 1993年 / 10卷 / 01期

关键词：

D O I：

10.3109/02652049309015307

中图分类号：

O69 [应用化学];

学科分类号：

081704 ;

摘要：

In order to provide a device releasing drugs in a controlled manner and having targetability to specific organs or cells, chitosan-gel microspheres, CMS, crosslinked with glutaraldehyde, immobolizing 1-[N-(5-aminopentyl) carbamoyl]-5-fluorouracil, 1, coated with anionic polysaccharides, such as 6-O-carboxymethyl-N-acetyl-alpha-1,4-polygalactosamine (CM-NAPGA), 6-O-carboxymethyl-chitin, alginic acid and heparin, by polyelectrolyte complex membrane formation were prepared. When chitosan was crosslinked with glutaraldehyde, 1 was simultaneously immobilized into CMS by Schiffs base formation. Average diameter of CMS obtained was estimated to be about 0.5-1.0 mum by SEM observation. In physiological saline media, only free 5-FU was released from the CMS but 1 and any 5-FU derivative was not. Release rate of 5-FU from the CMS was reduced by coating with polyelectrolyte complex membrane of cationic chitosan and anionic polysaccharides. CMS coated with CM-NAPGA showed a lectin-mediated specific aggregation phenomenon by addition of Abrus precatorius agglutinin. Moreover, the CMS immobilizing 1 coated with CM-NAPGA showed higher growth-inhibitory effect against SK-Hep-1 (human hepatoma) cells in vitro than the CMS coated with other polysaccharides.

引用

页码：1 / 9

页数：9

共 19 条

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