Abstract: OBJECTIVE To introduce the development of study on active targeting drug delivery system for prostate cancer. METHODS To review the domestic and foreign articles in recent years and summarize the active targeting drug delivery system based on the action sites of prostate cancer. RESULTS The target sites included prostate specific antigen and prostate specific membrane antigen. Active targeting drug delivery system, including liposome, micelle, nanoparticle, prodrug which was modified by antibody, aptamer or peptides, could effectively delivery the drug to prostate cancer tissue and cells, and improve the antitumor activity of drug. CONCLUSION There are broad prospects on the study and exploitation of active targeting drug delivery system for prostate cancer.