Phenyl boronic acid-modified lipid nanocarriers of niclosamide for targeting triple-negative breast cancer.

Abstract

Aim: To study the active targeting efficacy of phenylboronic acid-modified niclosamide solid lipid nanoparticles (PBA-Niclo-SLN) in triple-negative breast cancer (TNBC). Materials & methods: PBA-Niclo-SLNs were formulated by an emulsification-solvent evaporation method using PBA-associated stearylamine (PBSA) as lipid. The drug uptake and the anticancer propensity of PBA-Niclo-SLN were studied in TNBC (MDA-MB231) cells and tumor-bearing mice. Results: PBA-Niclo-SLN formulation resulted in greater antitumor efficacy by inducing G0/G1 cell cycle arrest and apoptosis. Besides, PBA-Niclo-SLN effectively inhibited STAT3, CD44+/CD24- TNBC stem cell subpopulation, epithelial-mesenchymal transition markers. Besides, PBA-Niclo-SLN selectively accumulated at the tumor site with more significant tumor regression and improved the survivability in TNBC tumor-bearing mice. Conclusion:PBA-Niclo-SLN formulation would be an effective strategy to eradicate TNBC cells (breast cancer stem cells and nonbreast cancer stem cells) efficiently.