Study On Preparation And Acitivity Of Conjugates Of Antitumor Drug And Chitosan Derivatives

In this paper, a high degree of deacetylation of chitosan as raw material to prepare a variety of water-soluble Chitosan derivatives: Norcantharidin-Chitosan, Succinyl-Chitosan, low molecular weight Chitosan, O-Succinyl-N- Norcantharidin-Chitosan et al. In order to extend the in vivo cycle time of Norcantharidin, enhanced the antitumor efficacy and reduce toxicity, we do the experiments to provide preliminary preparation of reference for the controlled release and targeted anti-cancer drugs .Succinyl-Chitosan interests researchers with its affinity with tumor cells. We have synthesized N-Succinyl-Chitosan and O-Succinyl-Chitosan, used Fluorescence-labeled technique, and test the affinity difference of two drug carriers on the HL-60 tumor cells after 48 hours incubation by flow cytometry , we found that O-Succinyl-Chitosan is a better drug carrier of stronger affinity to the HL-60 tumor cells, a large number of free amino makes that norcantharidin has more chance to couple with chitosan. In the Test , the verification of chemical structural of Chitosan derivatives we use infrared, nuclear magnetic resonance and carbon NMR spectrum , according to the characteristic peaks of the integral of Norcantharidin and succinic anhydride and then calculate the substitution degree of chitosan derivatives . Fluorospectrophotometer was used to determine the rate of fluorescent labeling of succinyl-chitosan.We chose several conjugates of Chitosan and Norcantharidin(NCTD) to do the experiment of anti-tumor effect with SPC-A cell . Results show that the conjugates have better anti-tumor effect.