Breast cancer is the most common cancer diagnosed in women worldwide. The current treatments for breast cancer, including surgery, radiotherapy and chemotherapy aim to destroy cancer cells, whereas they also cause damage to normal tissues and cells. Thus, an effective, safe and specific breast cancer treatment is urgently needed. The breast cancer-specific gene 1 (BCSG1) has been shown to be specific for the development of breast cancer and is a target for breast cancer diagnosis and treatment. It is expected to silence the expression of BCSG1 at the gene level for the purpose of treating breast cancer. The effect of RNAi technology on silencing target genes is comparable to gene knockout and has been widely used in animal experiments and plant genetic research. In the field of cancer therapy, numerous investigators have used siRNAs to specifically inhibit target genes, demonstrating that siRNAs can treat cancers at the molecular level. However, the delivery of siRNAs into humans needs to overcome multiple physiological barriers, limiting the clinical applications of siRNAs. This review focuses on the application of BCSG1 gene, siRNAs in cancer treatments, and the nanocarrier delivery system of siRNAs. The potential application and research value of BCSG1-specific siRNA in the treatment of breast cancer are discussed.