Novel micellar delivery system based on methoxy poly(ethylene glycol)-cholesterol / 中国药学杂志

ABSTRACT

OBJECTIVE: To synthesize methoxy poly(ethylene glycol)-cholesterol(mPEG-Chol), prepare mPEG-Chol micelles and investigate the in vitro cytotoxicity. METHODS: mPEG-Chol was achieved by conjugating cholesterol succinic ester(Chol-suc) with mPEG. mPEG-Chol micelles were constructed through different Methods including co-evaporation method, emulsion evaporation method and film dispersion method. The cytotoxicity of micelles was assessed systemically on different cell lines including MCF-7, MDA-MB-231, 4T1, SKOV-3 and AD293. RESULTS: mPEG-Chol was synthesized successfully with the yield of 70.3% and could form micelles via three different Methods. The size of mPEG-Chol micelles ranged from 20 to 150 nm. mPEG-Chol had no cell growth inhibition activity when set at the concentration of 20 μmol·L-1. The micelles showed different cytotoxicity compared with the mPEG-Chol molecular form. The IC50 values of micelles to SKOV-3 and MCF-7 were significantly lower than molecules. CONCLUSION: The synthesis process of mPEG-Chol is simple, cost-effective and easy to scale up massively. Micelles with low toxicity could be fabricated easily. Therefore, mPEG-Chol would be one of potential biomaterials to encapsulate various drugs with different solubility.