Reduction‐sensitive carrier containing disulfide bond based on Pluronic F68 with cholesterol for drug delivery,Polymer International

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Reduction‐sensitive carrier containing disulfide bond based on Pluronic F68 with cholesterol for drug delivery
Polymer International ( IF 2.9 ) Pub Date : 2020-08-09 , DOI: 10.1002/pi.6099
Yichen Zhang ₁ , Xiaoshan Fan ₁ , Yongjie Yu ₁ , Wenqiang Li ₁ , Hongpan Huang ₁ , Weiwei Zhang ₁ , Zhiguo Hu ₁ , Zibiao Li ₂

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The reduction‐sensitive amphiphilic polymer chol‐SS‐F68‐SS‐Chol (F68‐CDEC. chol, SS and F68 represent cholesterol, disulfide bond and Pluronic F68, respectively) was easily synthesized by two steps of esterification reactions. The self‐assembly behavior of the polymer was studied by fluorescence spectrophotometry, dynamic light scattering and TEM. Impressively, the critical micelle concentration of F68‐CDEC was 58‐fold smaller than that of F68. Besides, the drug loading content (LC = 20.25%) was higher than that of F68 (LC = 13.42%). In vitro release experiments showed that the reductant dithiothreitol triggered rapid disintegration of micelles with an accumulated drug amount of 55%, compared with an accumulated drug amount of 20% in phosphate‐buffered saline solution. These good abilities were further proved by cell uptake experiments. More importantly, almost no cytotoxicity was observed by 3‐(4,5‐dimethylthiazol‐2‐yl)‐2,5‐diphenyltetrazolium bromide (MTT) colorimetric assay and immunofluorescence staining experiments. There are reasons to believe that the polymer F68‐CDEC can be used as a reduction‐sensitive drug delivery material. © 2020 Society of Industrial Chemistry

中文翻译：

含有Pluronic F68和胆固醇的二硫键的还原敏感型载体，可用于药物输送

易还原的两亲聚合物chol-SS-F68-SS-Chol（F68-CDEC。chol，SS和F68分别代表胆固醇，二硫键和Pluronic F68）易于通过两步酯化反应合成。通过荧光分光光度法，动态光散射和TEM研究了聚合物的自组装行为。令人印象深刻的是，F68-CDEC的临界胶束浓度比F68小58倍。此外，载药量（LC = 20.25％）高于F68（LC = 13.42％）。体外释放实验表明，还原剂二硫苏糖醇引发了胶束的快速崩解，药物累积量为55％，而磷酸盐缓冲盐溶液中的药物累积量为20％。通过细胞摄取实验进一步证明了这些良好的能力。更重要的是，通过3-（4,5-二甲基噻唑-2-基）-2-溴5-二苯基四唑鎓（MTT）比色法和免疫荧光染色实验未观察到细胞毒性。有理由相信，聚合物F68-CDEC可用作还原敏感性药物传递材料。©2020工业化学学会

更新日期：2020-08-09

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