Recent advances in applying poly-epsilon-caprolactone for controlled delivery and targeting release of chemical anti-tumor drugs were summarized in this mini-review. Benefited from the efforts of scientists all over the world, various chemotherapeutic drug delivery systems based on different formulations of poly-epsilon-caprolactone related materials have been evaluated. It has been widely recognized that the introduction of of poly-epsilon-caprolactone components into drug delivery systems would increase drug loading capacity, decrease leakage, prolong releasing period and result in controllable releasing rate. Especially with the development of environment-responsive delivery systems (pH-, thermo-, magnetic field- and light-responsive drug carriers), enhanced tumor cell targeting potential, as well as decreased systemic toxicity would be realized.