Contribution of chitosan and its derivatives to cancer chemotherapy

Yoshinori Kato, Hiraku Onishi, Yoshiharu Machida

Research output: Contribution to journalArticlepeer-review

41 Scopus citations


The conjugates of some kinds of anticancer agents with chitin and chitosan derivatives display good anticancer effects with a decrease in the adverse effects of the original drug due to a predominant distribution into the cancer and a gradual release of free drug from the conjugates. For instance, doxifluridine and 1-β-D-arabinofuranosylcytosine (Ara-C) were conjugated with chitosan via glutaric spacer, and the conjugates of Ara-C with chitosan, in particular, showed a good antitumour effect against P388-bearing leukemia model mice. Glycol-chitosan (G-Chi) was distributed mainly in the systemic circulation and the kidney after i.v. administration into normal mice, and retained long in the kidney. The therapeutic effect of the conjugates of mitomycin C (MMC) with G-Chi was not necessarily improved in comparison with that of the free drug, but toxic side-effects appeared to decrease with the conjugates. The conjugates of MMC with 6-O-carboxymethyl-chitin showed almost complete suppression of tumour growth at 10 mg eq. MMC/kg, though a lethal adverse effect was also observed. The conjugates of MMC with N-succinyl-chitosan showed good antitumour activities against various tumour models due to their predominant distribution into the tumour tissue and sustained-release characteristics, irrespective of water-insoluble and -soluble formulations. It is believed that the chitin and chitosan derivatives discussed in this review are good candidates for a polymeric drug carrier in cancer chemotherapy.

Original languageEnglish (US)
Pages (from-to)301-310
Number of pages10
JournalIn vivo (Athens, Greece)
Issue number1
StatePublished - Jan 2005


  • 6-O-carboxymethyl-chitin
  • Anticancer agents
  • Antitumour activity
  • Biodistribution
  • Chitosan
  • Glyco-chitosan
  • N-succinyl-chitosan
  • Review

ASJC Scopus subject areas

  • Medicine(all)


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