In the past several decades, various types of nanostructured biomaterials have been developed. These nanostructured biomaterials have promising applications in biomedical fields such as bone repair, tissue engineering, drug delivery, gene delivery, antibacterial agents, and bioimaging. Nanostructured biomaterials with high biocompatibility, including calcium phosphate, hydroxyapatite, and calcium silicate, are ideal candidates for drug delivery. This review article is not intended to offer a comprehensive review of the nanostructured biomaterials and their application in drug delivery but rather presents a brief summary of the recent progress in this field. Our recent endeavors in the research of nanostructured biomaterials for drug delivery are also summarized. Special attention is paid to the synthesis and properties of nanostructured biomaterials and their application in drug delivery with the use of typical examples. Finally, we discuss the problems and future perspectives of nanostructured biomaterials in the drug delivery field.