Design of Chitosan-5Fu Conjugate Exhibiting Antitumor Activity |
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| Authors: | Tatsuro Ouchi Toshio Banba Hiroshi Masuda Tatsuji Matsumoto Shigeo Suzuki Masuko Suzuki |
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| Affiliation: | 1. Department of Applied Chemistry Faculty of Engineering Kansai , University Suita , Osaka, 564, Japan;2. Department of Microbiology and The Second Department of Hygienic Chemistry Tohoku , College of Pharmacy Sendai , Miyagi, 983, Japan;3. Department of Applied Chemistry Faculty of Engineering Kansai , University Suita , Osaka, 564, Japan |
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| Abstract: | In order to provide a macromolecular prodrug of 5-fluorouracil (5FU) reducing the side effects, having an affinity for tumor cells, and exhibiting strong antitumor activity, the covalent attachments of 5FUs to chitosan and chitosamino-oligosaccharide (COS) through hexamethylene spacer groups via urea, urea bonds were carried out. The effect of prolongation of life was tested in vivo against p388 lyrnphocytic leukemia in female CDF, mice by intra-peritoneal (i.p.) transplantation/i.p. injection and the growth-inhibitory effect on Meth-A fibrosarcoma or MH-134Y heputoma was evaluated in vivo in SPF-C3H/He scl male or Balb/c male mice by subcutaneous (s.c.) implantation/intravenous (i.v.) injection. The effects of the degree of polymerization of chitosan and |
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| Keywords: | Nanoparticles salt bridges pH-sensitive temperature-sensitive |
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