Transdermal delivery of brucine-encapsulated liposomes significantly enhances anti-tumor outcomes in treating triple-negative breast cancer.

Triple-negative breast cancer (TNBC) is always the most challenging breast cancer subtype. Herein, brucine, encapsulated in peptide-modified liposomes, was proposed for treating TNBC by transdermal delivery. For the TD peptide-modified brucine-loaded liposome (Bru-TD-Lip) we developed, it presents high encapsulation efficiency of brucine and stability. In vitro, Bru-TD-Lip shows the enhanced percutaneous permeability of brucine, is able to readily enter TNBC cells, and significantly inhibits the proliferation, migration, and invasion of these cells. In vivo, through transdermal delivery, Bru-TD-Lip presents good biosafety and anti-tumor efficacy. The transdermal delivery of Bru-TD-Lip effectively targets and inhibits subcutaneous mammary carcinogenesis in female nude mice. Compared with oral administration, the transdermal delivery significantly reduces the damage of brucine to major organs and enhances the antitumor outcomes of brucine in treating TNBC. This study provides a new therapeutic strategy for treating triple-negative breast cancer by brucine.