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

Abstract

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

A Stable Micellar Formulation of RAD001 for Intracerebroventricular Delivery and the Treatment of Alzheimer’s Disease and Other Neurological Disorders

“…Micelles are already clinically tested to deliver anticancer drugs [53]. In particular, DSPE-PEG2000 micelles have been found to be effective in delivering a broad range of drugs in animal models [54][55][56][57] and RAD001 in vitro [58]. Properties such as a low critical micellar concentration as well as small size increase the appeal of DSPE-PEG2000 micelles since they can enable effective drug accumulation at the site of action [31,32].…”

Male Breast Cancer: Current Scenario and Future Perspectives

“…Yang et al has reported that, Epirubicin (EPI), upon entering the BC cells under the guidance of the targeting NKA-α1 peptide, exhibited a gradual release from the nanocarrier. 149 The controlled delivery and subsequent release of EPI within the BC cells resulted in significant inhibition of cell proliferation and migration in vitro and led to a substantial reduction in tumor volume in vivo. 149 The introduction of lumpectomy as a treatment for BC marked a significant advancement in disease management.…”

“… 149 The controlled delivery and subsequent release of EPI within the BC cells resulted in significant inhibition of cell proliferation and migration in vitro and led to a substantial reduction in tumor volume in vivo. 149 The introduction of lumpectomy as a treatment for BC marked a significant advancement in disease management. Onik in 2004 has suggested that a procedure akin to a “male lumpectomy”—one that precisely targets the cancerous portion of the prostate gland while minimizing patient morbidity—is indeed feasible.…”