Preparation of salinomycin-loaded micelles and the effects on cancer stem cells in vitro / 中国药学杂志

ABSTRACT

OBJECTIVE: To design and prepare a novel polymeric micelles preparation for hydrophobic salinomycin (SAL), then evaluate the effects of SAL micelles on cancer stem cells in vitro. METHODS: SAL was entrapped into polymeric micelles constructed from amphiphilic diblock copolymer of poly (ethylene glycol)-block-poly (ε-caprolactone) (mPEG-b-PCL). Firstly, the process of preparing micelles and formulation composition were optimized. Then, the physicochemical properties such as particle size distribution, shape and surface morphology, stability and release rates of SAL-loaded micelles were studied. Finally, the side population (SP) cells were analyzed to evaluate the effects of SAL micelles on the MCF-7 cells. RESULTS: The optimal formulation of drug-loaded micelles was mPEG-b-PCL copolymers and SAL (201, w/w); the average particle size of SAL-loaded micelles was less than 30 nm, with narrow size distribution, uniform spherical shape and good stability. In vitro studies demonstrated that SAL-loaded micelles were able to decrease the proportion of SP cells. CONCLUSION: Polymeric micelles are capable of overcoming the poor solubility of SAL, and SAL-loaded micelles can selectively deplete breast cancer stem cells.