Abstract: Recent advances in nanotechnology raises exciting opportunities for generating new cancer therapies that might allow more efficient targeted delivery of anticancer agents to kill tumors and imaging agents for diagnosis of various cancers. In this article, some new perspectives were provided on the development of targeted nano-drug carriers for cancer treatment. The focus was not to review research articles published on the subject, but to discuss issues we considered critical concerning target selection, targeting mechanism, and carrier structure design. We hope such discussions would encourage more detailed and careful studies to support product development of targeted drug carriers for cancer treatment.