Management of prostate cancer is currently being pursued by systemic delivery of anticancer drugs, but it has drawbacks like nonspecific distribution, decreased bioavailability, coupled with adverse side effects. These problems have been resolved using nanomedicine-based anticancer drug delivery to improve the therapeutic index with higher drug dose and reduced nonspecific distribution. Targeting prostate tumor by delivering nanomedicine through locoregional route is more effective, than the systemic delivery, which can decrease systemic exposure of the therapeutics significantly. Therefore, in this article, we have reviewed the current prospects and challenges of prostate cancer therapy using nanomedicine, by providing a comprehensive description of advantages and limitations of the systemic route and locoregional route. Eventually, we have emphasized on the need for localized prostate cancer therapy developments using nanomedicines. © 2017 Future Medicine Ltd.