Preparation, characterization and anticancer activities of resveratrol loaded redox-sensitive F127-SS-TOC micelles

Abstract

Resveratrol (RES), a natural polyphenolic compound existing in plants, exhibits anticancer potential in inhibiting growth of various types of human cancers especially breast cancer. However, the poor aqueous solubility and low bioavailability limit its clinical application. Pluronic F127 (F127)-SS-Tocopherol (TOC) polymer is a redox-sensitive conjugate which has been synthesized by our previous study. Due to the amphiphilic properties of block copolymer F127-SS-TOC, RES was encapsulated by the F127-SS-TOC polymer and formed RES-loaded micelles (F127-SS-TOC/RES) in aqueous solution by self-assembly via a solvent evaporation method. The drug loading of F127-SS-TOC/RES micelles was 13.25 ± 2.29%, which remained stable for 7 days at 25 °C. The particle size and zeta potential of the above-mentioned micelles measured by dynamic light scattering (DLS) were 39.50 ± 1.39 nm and −4.55 ± 0.39 mV, respectively. Besides, F127-SS-TOC/RES micelles have significant cytotoxicity in human breast cancer cells MCF-7 and MDA-MB-231 compared to free RES and non-redox-sensitive F127-TOC/RES micelles. The results also showed that redox-sensitive F127-SS-TOC/RES micelles could induce apoptosis and elevate the intracellular reactive oxygen species (ROS) level against MDA-MB-231 cells. Hence, our results indicated that RES loaded F127-SS-TOC micelles hold potential in improving the treatment of breast cancer.