Doxorubicin-loaded human serum albumin-based nanoclusters produced by ball-milling technology and decorated with ALN (HSA-AD/DOX) showed ~5-fold higher affinity compared to the HSA/DOX in the hydroxyapatite-containing heterotopic human osteosarcoma cell line (HOS/MNNG) in vitro, as well as in a mouse xenograft model. The gene discussed is ALB; the disease is osteosarcoma.