When anticancer drug, paclitaxel, is clinically used, solubility and toxicity are two major problems. To overcome these problems, in the present study, we design a targeted anticancer drug delivery system, which contains drug, drug carrier, and target-differentiated ligand. The key point is that both of paclitaxel and target-differentiated ligand, folate, chemically bond to a biocompatible carrier, heparin, via ester bond and amide bond, respectively. Model reaction indicates that 54% carboxyl groups on the drug carrier are substituted by the model drug and the total yield of model conjugates is ranged from 61 to 66%. The results promise to open a new door for the development of targeted drugs.