Journal of Shandong University (Health Sciences) ›› 2018, Vol. 56 ›› Issue (6): 13-20.doi: 10.6040/j.issn.1671-7554.0.2018.190

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Construction and in vitro anticancer evaluation of redox-sensitive polymeric micelles based on PEO-PPO-SS-DTX conjugate

LIU Xin1,2, ZHANG Pei1, HE Wenxiu1, LUAN Yuxia1   

  1. 1. School of Pharmaceutical Sciences, Shandong University, Jinan 250012, Shandong, China;
    2. Department of Pharmacy, The Second Hospital of Shandong University, Jinan 250033, Shandong, China
  • Published:2022-09-27

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Abstract: Objective To synthesize, characterize and evaluate allyl polyoxyethylene-polyethylene oxide(PEO-PPO)-SS-docetaxel(DTX)conjugate. Methods The PEO-PPO-SS-DTX conjugate was synthesized and confirmed structurally by nuclear magnetic resonance hydrogen spectrum(1H-NMR)and fourier transform infrared spectroscopy(FT-IR). Then the PEO-PPO-SS-DTX micelles were prepared and the assembly behavior of the PEO-PPO-SS-DTX conjugate in aqueous solution was studied. The average size of the micelles, critical micelle concentration(CMC), and drug loading(DL)content and hemolysis rate(HR)were measured by dynamic light scattering instrument, fluorescence, and UV spectrophotometry, respectively. The cytotoxicity experiment and cell uptake experiment were used to evaluate its in vitro anticancer efficacy. Results The PEO-PPO-SS-DTX conjugate and micelles were prepared successfully. The PEO-PPO-SS-DTX conjugate could assemble into the spherical micelles spontaneously in aqueous solution. The average size of the micelles was(159.0±4.4)nm with poly dispersity index(PDI)of 0.18±0.01. The CMC was about 5.0 μg·mL-1, drug loading(DL)content was 8.3%, and the hemolysis rate(HR)was less than 5%. The PEO-PPO- 山 东 大 学 学 报 (医 学 版)56卷6期 -刘新,等.氧化还原敏感PEO-PPO-SS-DTX聚合物胶束的构建及体外抗肿瘤评价 \=-SS-DTX micelles had excellent anti-tumor efficiency and cell uptake rate against Hep1-6 cells. Conclusion The PEO-PPO-SS-DTX conjugate has excellent properties and great potentical for clinical application.

Key words: Redox-sensitivity, PEO-PPO-SS-DTX conjugate, Polymer micelles, Antitumor evaluation

CLC Number: 

  • R944
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