Curcumin has multiple biological and pharmacological activities, including antioxidant, anti-inflammatory, antiviral, antibacterial, antifungal, and antitumor activities. However, the clinical use of curcumin is limited because of its poor oral absorption and extremely poor bioavailability. In order to overcome these limitations, we conjugate curcumin chemically into the known biocompatible and biodegradable polymer, poly(glycerol–sebacate), and prepare the unitary poly(glycerol–sebacate–curcumin) polymer. The structure, the in vitro degradation, the drug release, and antitumor activity as well as the in vivo degradation and tissue biocompatibility of poly(glycerol–sebacate–curcumin) polymer are investigated. The in vitro degradation and drug release profile of poly(glycerol–sebacate–curcumin) are in a linear manner. The in vitro antitumor assay shows that poly(glycerol–sebacate–curcumin) polymer significantly inhibits human malignant glioma cells, U87 and T98 cells. In view of the cytotoxicity against brain gliomas, local use of this polymer would be a potential method for brain tumors. © 2012 Wiley Periodicals, Inc. J Biomed Mater Res Part A: 101A:253–260, 2013.