Caffeic acid-conjugated chitosan (ChitoCFA) and carboxymethyl dextran-b-poly(ethylene gycol) (CMD-PEG) copolymer were synthesized to fabricate self-organized nanoparticles. Nanoparticles were formed through ion-complex formation between ChitoCFA and CMD-PEG. Nanoparticles have small sizes ranged about 80 nm~300 nm with spherical shapes. Doxorubicin (DOX) was incorporated into the nanoparticles of ChitoCFA/CMD complexes. Particle sizes were increased according to the contents of drug. At drug release experiment, DOX was continuously released over 96 h. Anticancer acticity of nanoparticles were assessed with DOX-resistant CT26 cells. CT26 cells treated with DOX-incorporated nanoparticles revealed strong fluorescence intensity while free DOX revealed weak fluorescence intensity, indicating that DOX-loaded nanoparticles of ChitoCFA/CMD are promising vehicle for anticancer drug targeting.