Abstract |
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, immobilizing 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 Schiff's base formation. Average diameter of CMS obtained was estimated to be about 0.5-1.0 micron 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.
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Authors | Y Ohya, T Takei, H Kobayashi, T Ouchi |
Journal | Journal of microencapsulation
(J Microencapsul)
1993 Jan-Mar
Vol. 10
Issue 1
Pg. 1-9
ISSN: 0265-2048 [Print] England |
PMID | 8383199
(Publication Type: Journal Article, Research Support, Non-U.S. Gov't)
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Chemical References |
- Delayed-Action Preparations
- Galactans
- Gels
- Lectins
- Polysaccharides
- Chitin
- 6-O-carboxymethyl-N-acetyl-1,4-polygalactosamine
- Chitosan
- Fluorouracil
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Topics |
- Carcinoma, Hepatocellular
(drug therapy, metabolism, pathology)
- Cell Division
(drug effects)
- Chemistry, Pharmaceutical
- Chitin
(analogs & derivatives, chemistry)
- Chitosan
- Delayed-Action Preparations
- Drug Delivery Systems
- Fluorouracil
(chemistry, pharmacokinetics, pharmacology)
- Galactans
(chemistry)
- Gels
- Humans
- Lectins
- Liver Neoplasms
(drug therapy, metabolism, pathology)
- Microspheres
- Polysaccharides
(chemistry)
- Sensitivity and Specificity
- Tumor Cells, Cultured
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