Carboxymethyl chitosan (CM-chitosan) was prepared and characterized by FTIR and NMR spectroscopy, and its biological safety in tumor application was investigated both in vitro and in vivo. Cytotoxicity studies by MTT assay indicated that CM-chitosan was safe both on normal cell L02 and three tumor cell lines: Bel-7402, SGC-7901 and Hela in vitro. CM-chitosan also improved the TGF-alpha secretion of L02 cell (P < 0.05), whereas decreased levels of TGF-alpha and VEGF secreted by Bel-7402 cell (P < 0.05), which are compatible with the observations at cell levels. In vivo, transplant tumor model of sarcoma 180 was established in mice and CM-chitosan was administered through intraperitoneal injection. Experimental data indicated that CM-chitosan was safe in vivo and slightly inhibited growth of sarcoma 180 and enhanced body immunity via elevation of serum IL-2 and TNF-alpha levels in treated mice (P < 0.05). These results suggest that CM-chitosan is safe in tumor application as biomedical material. (C) 2011 Elsevier Ltd. All rights reserved.