Prostate cancer (PCa) is the most common malignant tumor in men and, after lung cancer, the second leading cause of cancer death. Currently, androgen deprivation therapy (ADT) has become the standard of care for men with locally advanced or metastatic prostate cancer. However, after undergoing ADT for 18 to 24 months, most patients develop castration-resistant prostate cancer (CRPC). Depending on the stage of CRPC, the recommended first-line treatment regimens include chemotherapy with docetaxel (DTX) and novel hormonal agents, such as enzalutamide (ENZ). Combination therapy with DTX and ENZ for CRPC is expected to be successful in the future. To achieve this goal, it is critical to design a drug delivery system with distinct pharmacokinetic actions for both drugs.