Currently, one of the significant challenges remaining in the field of drug delivery research is insufficient targeting to diseased tissues or cells. The massive research indicated that, targeted drug delivery systems based on nanoparticles have shown a new hope in cancer treatment, but there still exist some problems including poor biocompatibility, uncontrollable degradation, high cytotoxicity and immunogenicity. In contrast, living cells usually have innate targeting ability, high drug loading capability and biological barrier penetration ability, and can be used as drug delivery vehicles to control drug release, so as to improve the accumulation and treatment efficiency of drugs on the focal tissues or cells. This review dwelled on the researches of immune cells, anucleated cells, stem cells, bacteria and their derivatives as drug delivery carriers. Meanwhile, the mechanism, advantages and disadvantages of different drug delivery systems were also discussed. Finally, the potential for clinical transformation and the prospect of live cells and their derivatives as drug delivery carriers were proposed.