The preparation of the luminescent hydroxyapatite (HAP)-loaded biocompatible nanoparticles (NPs) for targeted imaging of cancer cells is described. Currently, cellular imaging using fluorescent probes is an important technique for the early diagnosis of cancer. Compared with the quantum dots, luminescent HAP is a new fluorescent material with many advantages such as low toxicity, biocompatibility, thermal stability, resistance to erosion, and low prices. Thus, luminescent HAP has enormous potential to be used as biological fluorescent probes. However, luminescent HAP is water-insoluble, low sensitivity, which limit its application in the field of cellular imaging. Surface modification of NPs with targeting molecule was carried out to achieve its target function. Thus, novel fluorescent NPs with low toxicity, high sensitivity, and good photostability were prepared to be used for targeted imaging of cancer cells. This study initially explored the applications of luminescent HAP in the field of targeted cellular imaging. This NPs platform will be a promising tool for molecular imaging and medical diagnostics, especially the detection of cancer at its early stage. (c) 2013 American Institute of Chemical Engineers AIChE J, 59: 4494-4501, 2013