首页> 美国卫生研究院文献>Acta Pharmaceutica Sinica. B >Interfacial properties and micellization of triblock poly(ethylene glycol)-poly(ε-caprolactone)-polyethyleneimine copolymers
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Interfacial properties and micellization of triblock poly(ethylene glycol)-poly(ε-caprolactone)-polyethyleneimine copolymers

机译:三嵌段聚(乙二醇)-聚(ε-己内酯)-聚乙烯亚胺共聚物的界面性质和胶束化

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摘要

This study aimed to explore the link between block copolymers’ interfacial properties and nanoscale carrier formation and found out the influence of length ratio on these characters to optimize drug delivery system. A library of diblock copolymers of PEG-PCL and triblock copolymers with additional PEI (PEG-PCL-PEI) were synthesized. Subsequently, a systematic isothermal investigation was performed to explore molecular arrangements of copolymers at air/water interface. Then, structural properties and drug encapsulation in self-assembly were investigated with DLS, SLS and TEM. We found the additional hydrogen bond in the PEG-PCL-PEI contributes to film stability upon the hydrophobic interaction compared with PEG-PCL. PEG-PCL-PEI assemble into smaller micelle-like (such as PEG-PCL4006-PEI) or particle-like structure (such as PEG-PCL8636-PEI) determined by their hydrophilic and hydrophobic block ratio. The distinct structural architectures of copolymer are consistent between interface and self-assembly. Despite the disparity of constituent ratio, we discovered the arrangement of both chains guarantees balanced hydrophilic–hydrophobic ratio in self-assembly to form stable construction. Meanwhile, the structural differences were found to have significant influence on model drugs incorporation including docetaxel and siRNA. Taken together, these findings indicate the correlation between molecular arrangement and self-assembly and inspire us to tune block compositions to achieve desired nanostructure and drug loading.
机译:这项研究旨在探讨嵌段共聚物的界面性能与纳米级载体形成之间的联系,并发现长度比对这些特性的影响,从而优化了药物递送系统。合成了PEG-PCL的二嵌段共聚物和具有额外PEI的三嵌段共聚物(PEG-PCL-PEI)的库。随后,进行了系统的等温研究,以探讨共聚物在空气/水界面处的分子排列。然后,用DLS,SLS和TEM研究了自组装的结构特性和药物封装。我们发现,与PEG-PCL相比,PEG-PCL-PEI中的其他氢键在疏水作用下有助于薄膜的稳定性。 PEG-PCL-PEI组装成较小的胶束状结构(例如PEG-PCL4006-PEI)或颗粒状结构(例如PEG-PCL8636-PEI),取决于它们的亲水和疏水嵌段比率。共聚物的独特结构体系在界面和自组装之间是一致的。尽管构成比例存在差异,但我们发现两条链的排列均确保了自组装中形成平衡的亲水-疏水比率,从而形成稳定的结构。同时,发现结构差异对包括多西他赛和siRNA在内的模型药物掺入具有显着影响。综上所述,这些发现表明了分子排列与自组装之间的相关性,并激发我们调整嵌段组成以获得所需的纳米结构和载药量。

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