In the last century, natural compounds have achieved remarkable achievements in the treatment of tumors through chemotherapy. This inspired scientists to continuously explore anticancer agents from natural compounds. Kaempferol is an ordinary natural compound, the most common flavonoid, which is widely existed in vegetables and fruits. It has been reported to have various anticancer activities, including breast cancer, prostate cancer, bladder cancer, cervical cancer, colon cancer, liver cancer, lung cancer, ovarian cancer, leukemia, etc. Meanwhile, we found that there were more reports on breast cancer among these cancers although there are limited clinical studies that have addressed the benefits of kaempferol as an anti-cancer agent for breast cancer treatment. Then we realize that although kaempferol has been reported to have anti-breast cancer effect many times, it is still far from becoming a real anti-breast cancer agent. Therefore, in this review, we talk about the options for improving the anti-breast cancer effect of kaempferol, including various techniques and methods to improve the bioavailability of kaempferol, the idea of combining other compounds to produce synergistic effects, and the possibility of developing kaempferol into a targeted drug delivery system.