Using nanomaterials as delivery vehicles of chemotherapeutic drugs enable to reduce their side effects. In this work, BCNNTs were prepared via an improved solid-state reaction method, which were then functionalized by folate (FA) to load doxorubicin (DOX), thereby building a targeted drug delivery system of FA-BCNNTs-DOX. FTIR and UV-Vis analysis results revealed the loading of DOX on FA-BCNNTs, accompanied with the capacity of 87.11 μg/mg. In vitro cytotoxicity test indicated that the antitumor activity of FA-BCNNTs-DOX is significantly higher than those of free DOX and BCNNTs-DOX. Furthermore, FA-BCNNTs-DOX and BCNNTs-DOX were found to possess pH-responsive release characteristic, which helps to improve the bioavailability of DOX and reduce the damage to healthy cells. In addition, cellular uptake research indicated that FA-BCNNTs-DOX entered cancer cells through folate receptor-mediated endocytosis, which greatly enhanced the drug delivery efficiency.