Controllable Drug Delivery by Na+/K+ ATPase α1 Targeting PeptideConjugated DSPE-PEG Nanocarriers for Breast Cancer

摘要

Although Epirubicin (EPI) is a commonly used anthracycline for the treatment ofbreast cancer in clinic, the serious side effects limit its long-termadministration including myelosuppression and cardiomyopathy. Nanomedicines havebeen widely utilized as drug delivery vehicles to achieve precise targeting ofbreast cancer cells. Herein, we prepared a DSPE-PEG nanocarrier conjugated apeptide, which targeted the breast cancer overexpression protein Na+/K+ ATPaseα1 (NKA-α1). The nanocarrier encapsulated the EPI and grafted with the NKA-α1targeting peptide through the click reaction between maleimide and thiol groups.The EPI was slowly released from the nanocarrier after entering the breastcancer cells with the guidance of the targeting NKA-α1 peptide. The precise andcontrollable delivery and release of the EPI into the breast cancer cellsdramatically inhibited the cells proliferation and migration invitro and suppressed the tumor volume in vivo.These results demonstrate significant prospects for this nanocarrier as apromising platform for numerous chemotherapy drugs.