Owing to high efficacy and safety, natural medicines have found their way into the field of cancer therapy over the past few decades. However, the effective ingredients of natural medicines have shortcomings of poor solubility and low bioavailability. Nanoparticles can not only solve the problems above but also have outstanding targeting ability. Targeting preparations can be classified into three levels, which are target tissues, cells, and organelles. On the premise of clarifying the therapeutic purpose of drugs, one or more targeting methods can be selected to achieve more accurate drug delivery and consequently to improve the anti-tumor effects of drugs and reduce toxicity and side effects. The aim of this review is to summarize the research status of natural medicines' nano-preparations in tumor-targeting therapies to provide some references for further accurate and effective cancer treatments.