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Novel amino-β-Cyclodextrins containing polymers: Fabrication, characterization, and biological evaluation.
Colloids and Surfaces B: Biointerfaces ( IF 5.8 ) Pub Date : 2020-08-12 , DOI: 10.1016/j.colsurfb.2020.111311
Xiao Han 1 , Xin Guo 1 , Yongli Shi 2 , Wenhao Li 1 , Guoquan Zhang 1
Affiliation  

In this study, poly (mPEGMA-co-MAA) (PA) based on monomers of mPEGMA and MAA were synthesized, and different amino-β-Cyclodextrins with various alkyl chains were conjugated to PA through carbodiimide-mediated coupling reactions. The obtained poly (mPEGMA-co-MAA-g-amino-β-CD) (PA-g-amino-β-CD) was characterized by FTIR, NMR and TGA. The fluorescence technique was used to investigate the micellization of PA-g-amino-β-CDs. The results indicated that these polymers could self-assemble into nano-micelles in water, and PA-g-HDA-β-CD possessed the lowest CMC value due to its long alkyl chains. In addition, the PA-g-HDA-β-CD micelles were in spherical shapes with the diameter of 78.5 ± 0.6 nm.The release of the model drug from PA-g-HDA-β-CD micelles was increased as the pH reduced from 7.4–5.5 at 37 °C. Cytotoxicity and cellular uptake experiments were performed in HepG2, which showed that the cargo-free PA-g-HDA-β-CD micelles did not have obvious cytotoxicity and were mainly distributed in the cytoplasm of HepG2 cells by endocytosis. Moreover, the study about in vivo distribution of the experimental rats indicated that the accumulation of PA-g-HDA-β-CD micelles mainly happened in the liver. Therefore, the novel amino-β-CD containing polymers exhibit good potential applications in drug delivery system.



中文翻译:

新型含聚合物的氨基-β-环糊精:制备,表征和生物学评估。

在这项研究中,合成了基于mPEGMA和MAA单体的聚(mPEGMA- co -MAA)(PA),并通过碳二亚胺介导的偶联反应将具有各种烷基链的不同氨基-β-环糊精与PA偶联。得到的聚(mPEGMA--MAA -g氨基β- CD)(PA-氨基β -CD)的特点是FTIR,NMR和TGA。荧光技术用于研究PA- g-氨基-β- CD的胶束化。结果表明,这些聚合物可以在水中自组装成纳米胶束,PA- g - HDA- β-CD由于其长烷基链而具有最低的CMC值。此外,PA- g -HDA - β -CD胶束呈球形,直径为78.5±0.6 nm。随着pH降低,模型药物从PA- g -HDA - β -CD胶束中的释放增加。在37°C下从7.4–5.5。在HepG2中进行了细胞毒性和细胞摄取实验,结果表明,无载货的PA- g - HDA - β -CD胶束没有明显的细胞毒性,并且主要通过内吞作用分布在HepG2细胞的细胞质中。此外,关于实验大鼠体内分布的研究表明,PA- g -HDA-的积累β -CD胶束主要发生在肝脏。因此,含有氨基 -CD的新型聚合物在药物递送系统中显示出良好的潜在应用。

更新日期:2020-08-19
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