The targeted delivery of therapeutic drugs into cancer cells is a facile method to improve therapeutic efficacy. Focusing on this point, doxorubicin (DOX)-loaded hydroxyapatite (HAP) nanorods with folic acid (FA) modification (DOX@HAP-FA) have been developed for efficient antitumor treatment. In this study, DOX@HAP-FA exhibited satisfactory drug loading efficiency and significantly reduced the viability of the MCF-7 cells. Western blot assays demonstrated that DOX@HAP-FA could increase the expression of Bax (a pro-apoptotic protein) and decrease the expression of Bcl-2 (an anti-apoptotic protein). Furthermore, DOX@HAP-FA could markedly enhance mitochondrial cytochrome C leakage and thereby activate an apoptotic cascade associated with it. Thus, the designed DOX@HAP-FA nanorods showed promising potentials for targeted drug delivery in cancer therapy.