Chemical conjugates composed of paclitaxel (PTXL) and hyperbranched polyglycidols (HBP) were synthesized using glutaric anhydride as a "bridge" with esterification in dimethylformamide. A series of HBP-PTXL conjugates (HPCs) were synthesized using different molecular weights of HBP and varying ratios of HBP to PTXL, and they were characterized. An intact form of PTXL was regenerated from HPCs under acidic or basic pH conditions. Furthermore, water-soluble HPCs exhibit a more pronounced cytotoxic effect against cancer cells, suggesting that these HPCs can be utilized as tumor-specific therapeutic agents in the form of an injectable drug.