Despite the various types of nanocarriers, the widespread application of nanocarrier-based drug delivery systems is usually limited by problems such as drug burst release, low drug loading efficiency, and poor stability. The prodrug strategy specifically aims to modify the structures of the drugs themselves, and the majority of existing prodrugs have achieved clinical success, with new ones emerging. Meanwhile, the prodrug nanocarrier strategy integrates prodrugs with nanocarriers to enable effective drug loading and targeted delivery with controlled drug release both in vitro and in vivo, which is critical for improving drug efficacy. Numerous prodrug nanocarriers have been developed in response to the pathogenic features of various diseases, particularly in the treatment of tumors. This chapter primarily summarizes recent research progress in prodrug nanocarriers, including construction, stimuli-responsive strategies, conclusions, and future perspectives.