Department of Pharmaceutical Engineering, School of Chemistry and Material Science, Heilongjiang University, Harbin 150080, China.
College of Chemistry and Chemical Engineering, Harbin Normal University, Harbin 150025, China.
Int J Mol Sci. 2022 Sep 16;23(18):10801. doi: 10.3390/ijms231810801.
In the present study, an amphiphilic polymer was prepared by conjugating methoxy poly(ethylene glycol) (mPEG) with tetraphenylethene (TPE) via disulfide bonds (Bi(mPEG-S-S)-TPE). The polymer could self-assemble into micelles and solubilize hydrophobic anticancer drugs such as paclitaxel (PTX) in the core. Combining the effect of TPE, mPEG, and disulfide bonds, the Bi(mPEG-S-S)-TPE micelles exhibited excellent AIE feature, reduced protein adsorption, and redox-sensitive drug release behavior. An in vitro intracellular uptake study demonstrated the great imaging ability and efficient internalization of Bi(mPEG-S-S)-TPE micelles. The excellent anticancer effect and low systemic toxicity were further evidenced by the in vivo anticancer experiment. The Bi(mPEG-S-S)-TPE micelles were promising drug carriers for chemotherapy and bioimaging.
在本研究中,通过二硫键(Bi(mPEG-S-S)-TPE)将甲氧基聚乙二醇(mPEG)与四苯乙烯(TPE)偶联制备了一种两亲聚合物。该聚合物可以自组装成胶束,并将疏水性抗癌药物如紫杉醇(PTX)溶解在核心中。结合 TPE、mPEG 和二硫键的作用,Bi(mPEG-S-S)-TPE 胶束表现出优异的聚集诱导发光(AIE)特性、减少蛋白质吸附和氧化还原敏感的药物释放行为。体外细胞内摄取研究表明,Bi(mPEG-S-S)-TPE 胶束具有出色的成像能力和高效的内化能力。体内抗癌实验进一步证明了其优异的抗癌效果和低系统毒性。Bi(mPEG-S-S)-TPE 胶束有望成为用于化疗和生物成像的药物载体。
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