Novel dual-drug sulfobutylether-β-cyclodextrin (CD)/chitosan (CS) nanoparticles (NPs) containing docetaxel (DTX) and berbamine were developed and evaluated in this study. These NPs were prepared using ionic gelation method and were characterised for their particle size, polydispersity, zeta potential, drug loading percentage and yield. Cytotoxicity was measured through 3-(4,5-dimethyltiazol-2-ly)-2,5-diphenyltetrazolium bromide assay, and the expression of survivin mRNA in MCF-7 cells was detected using qRT-PCR. Cellular uptake and apoptosis were also analysed. Compared with the other DTX formulations in this study, the dual-drug CD/CS NPs showed better release and intestinal transport profiles in vitro and had improved pharmacokinetics data. The dual-drug CD/CS NPs exhibited higher cytotoxicity, cellular uptake, apoptosis and inhibition with the survivin mRNA expression. The relatively improved oral bioavailability and better antitumour efficacy indicated that the dual-drug CD/CS NPs developed in our study possessed significant advantages and might be a promising strategy for the development of drug, delivery systems for cancer chemotherapy.