Design of crown ether based micelles and their anti-tumor properties by perturbing potassium ion homeostasis

Abstract

Chemotherapy is one of the most used method for cancer therapy, however, brings huge pain to patients as the drugs commonly causes side effects. Inducing tumor cells apoptosis by perturbing ion homeostasis is a novel approach to replace chemotherapy in recent years. Crown ether has been widely used since it was discovered in the last century and has shown its potential in biological applications. The aim of this paper is to design a series of novel nanometer micelles with crown ether on their surface. Crown ether was connected to a commonly used amphiphilic polymeric carrier, PEG-PCL, through ester bond (CPMs). Micelles about 120 nm in diameter were formed in aqueous solution. The micelles could capture potassium ions prominently in both aqueous solution and tumor cells. In vitro and in vivo experiments showed that the CPMs had certain anti-tumor activity, indicating that the CPMs had anti-tumor potential.