In the present study, the anticancer drug temozolomide (TMZ) was initially loaded into the chitosan (CS) nanoparticles and synthesized CS/TMZ nanoparticles were incorporated into the synthesized poly (epsilon-caprolactone diol) based polyurethane (PCL-Diol-b-PU) nanofibers. The synthesized nanoparticles and nanofibers were characterized using dynamic light scattering, transmission electron microscopy, X-ray powder diffraction and scanning electron microscopy. The obtained results revealed that the CSITMZ nanoparticles were successfully embedded into the PCL-Diol-b-PU nanofibers. The gold nanoparticles with average particle size of 18 nm were synthesized and coated on the nanofibers surface to enhance the antitumor activity of CS/TMZ loaded nanofibers against inhibiting the growth of U-87 MG human glioblastoma cells. The sustained TMZ release for 30 days with the zero order kinetic model were achieved from both CS/TMZ loaded PCL-Diol-b-PU and gold-coated nanofibers. The cell viability results indicated that the gold-coated nanofibers can effectively inhibit the growth of U-87 glioblastoma cells. Therefore, the prepared gold-coated CS/TMZ loaded PCL-Diol-b-PU nanofibers would be a potential candidate for glioblastoma cancer treatment. (C) 2017 Published by Elsevier B.V.