Schizophyllan having folate-appendages was synthesized from native schizophyllan through NaIO4-oxidation and the subsequent reductive amination in aqueous ammonia followed by amido-coupling with folic acid. The resulting folate-appended schizophyllan can form stable complex with poly(dA), show specific affinity toward folate binding protein, and mediate effective antisense activity in cancer cells. (C) 2004 Elsevier Ltd. All rights reserved.