Targeting the epidermal growth factor receptor (EGFR) is an alternative therapeutic strategy for the treatment of triple-negative breast cancer (TNBC). Here, we designed EGFR-targeting micelles for the specific delivery of gefitinib (Gef), an EGFR tyrosine kinase inhibitor, to TNBC cells. EGFR-targeting-polyethylene glycol-1, 2-distearoyl-sn-glycero-3-phosphoethanolamine (EGFp-PEG-DSPE) was synthesized and characterized by mass analysis and 1H-nuclear magnetic spectroscopy (1H-NMR). The prepared EGFR-targeting micelles formed self-assembled nano-sized structures and released Gef in a sustained manner. More importantly, they specifically delivered Gef into TNBC cells (MDA-MB-468; EGFR + + +) and exerted better therapeutic effects compared to low or negative EGFR expressing TNBC cells [MDA-MB-231 (EGFR +) and MDA-MB-453 (EGFR–)].

Graphical Abstract

Targeting the epidermal growth factor receptor (EGFR) is an alternative therapeutic strategy for the treatment of triple-negative breast cancer (TNBC). Here, we designed EGFR-targeting micelles for the specific delivery of gefitinib (Gef), an EGFR tyrosine kinase inhibitor, to TNBCs. The prepared EGFR-targetable micelles with Gef formed self-assembled nano-sized structures and released Gef from the micelles in a sustained manner. Moreover, they specifically deliver Gef into TNBC cells (MDA-MB-468; EGFR + + +) and exerted better therapeutic effects compared to low or negative EGFR-expressing TNBC cells [MDA-MB-231 (EGFR +) and MDA-MB-453 (EGFR–)].