RELEASE BEHAVIOR OF 5-FLUOROURACIL FROM CHITOSAN-GEL NANOSPHERES IMMOBILIZING 5-FLUOROURACIL COATED WITH POLYSACCHARIDES AND THEIR CELL-SPECIFIC CYTOTOXICITY

Citation
Y. Ohya et al., RELEASE BEHAVIOR OF 5-FLUOROURACIL FROM CHITOSAN-GEL NANOSPHERES IMMOBILIZING 5-FLUOROURACIL COATED WITH POLYSACCHARIDES AND THEIR CELL-SPECIFIC CYTOTOXICITY, Pure and applied chemistry, A31(5), 1994, pp. 629-642
Citations number
26
Language
INGLESE
art.tipo
Article
Categorie Soggetti
Polymer Sciences
Journal title
ISSN journal
0033-4545
Volume
A31
Issue
5
Year of publication
1994
Pages
629 - 642
Database
ISI
SICI code
0033-4545(1994)A31:5<629:RBO5FC>2.0.ZU;2-0
Abstract
Small-sized chitosan-gel nanospheres, CNSs (average diameter 250 nm), containing 5-fluorouracil (5FU) or immobilizing 5FU derivatives (amino pentyl-carbamoyl-5FU or aminopentyl-ester-methylene-5FU) were prepared by the glutaraldehyde crosslinking technique and the emulsion method. When chitosan was crosslinked with glutaraldehyde, these 5FU derivati ves were simultaneously immobilized to CNSs by means of Schiff's base formation. The CNSs were coated with anionic polysaccharides, such as boxymethyl-N-acetyl-alpha-1,4-polygalactosamine/Na (CM-NAPGA/Na), 6-O- carboxymethyl-chitin/Na (CM-chitin/Na), and sodium hyaluronate, throug h formation of a polyelectrolyte complex membrane to give CNS/polyanio n, i.e., CNS/G, CNS/C, and CNS/H, respectively. The polyelectrolyte co mplex of polysaccharide was employed to achieve the controlled release and effective targeting of 5FU by the CNSs. The release rate of 5FU f rom the CNSs could be controlled by immobilization of 5FU, degree of d eacetylation of chitosan used and coating with polysaccharides. Since very few galactosamine residues are known to be able to cross-react wi th ligands for galactose, the galactosamine residues on the surface of CNS/Gs are expected to act as the targeting moieties for hepatocyte. The CNS/G showed the lectin mediated aggregation phenomenon by the add ition of APA lectin. Moreover, CNS/G had the highest cytotoxic activit y among the three kinds of CNS/polyanion and CNS in HLE human hepatoma cell culture system in vitro.