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葛根素/甘草次酸-聚乙二醇-聚(β-氨基酯)复合物的靶向递送通过调节Toll样受体4/核因子-κB通路减轻肝脏缺血/再灌注损伤。

Targeted delivery of puerarin/glycyrrhetinic acid-PEG-PBLA complex attenuated liver ischemia/reperfusion injury via modulating Toll-like receptor 4/nuclear factor-κB pathway.

作者信息

Xiao Ya, Huang Jiajia, Xu Jiajia, Zeng Liuwei, Tian Jiaran, Lou Yunru, Liu Yuxue, Hu Bo, Tong Fei, Shen Ruilin

机构信息

Grade 2016, Clinical Medicine, Jiaxing University Medical College, Jiaxing 314001, ZJ, PR China.

Department of Physiology & Diabetes Institute, Jiaxing Hospital of Traditional Chinese Medicine, Jiaxing University, Jiaxing 314001, ZJ, PR China.

出版信息

Ther Deliv. 2018 Mar 1;9(4):245-255. doi: 10.4155/tde-2017-0106.

DOI:10.4155/tde-2017-0106
PMID:29540127
Abstract

AIM

To synthesize a puerarin nanoparticle based on glycyrrhetinic acid (GA)-PEG-PBLA and evaluate it in vivo.

MATERIALS & METHODS: In this study, drug nanoparticle was synthesized, characterized and assessed as puerarin delivery system. Nanoparticle GA-PEG-PBLA could combine with puerarin via hydrophobic interaction to form the compound. Puerarin could be quickly and efficiently loaded via the nanoparticle GA-PEG-PBLA at pH 7.4. Further, GA-PEG-PBLA-mediated puerarin delivery system could target for the liver that had GA receptor binding. The antiliver ischemia/reperfusion injury role of puerarin/GA-PEG-PBLA was measured in rats using free puerarin and puerarin/PEG-PBLA as the controls.

RESULTS

GA-PEG-PBLA displayed efficient loading and sustained release. Puerarin/GA-PEG-PBLA showed strengthened antiliver ischemia/reperfusion injury characteristics.

CONCLUSION

Overall, the results show that GA-PEG-PBLA could be regarded as an underlying puerarin nanoparticle.

摘要

目的

基于甘草次酸(GA)-聚乙二醇-聚(β-氨基酯)(PBLA)合成葛根素纳米颗粒并进行体内评价。

材料与方法

在本研究中,合成、表征并评估了作为葛根素递送系统的药物纳米颗粒。纳米颗粒GA-PEG-PBLA可通过疏水相互作用与葛根素结合形成复合物。在pH 7.4条件下,葛根素可通过纳米颗粒GA-PEG-PBLA快速有效地负载。此外,GA-PEG-PBLA介导的葛根素递送系统可靶向具有GA受体结合的肝脏。以游离葛根素和葛根素/PEG-PBLA为对照,在大鼠中测定葛根素/GA-PEG-PBLA对肝脏缺血/再灌注损伤的作用。

结果

GA-PEG-PBLA表现出高效负载和缓释性能。葛根素/GA-PEG-PBLA显示出更强的抗肝脏缺血/再灌注损伤特性。

结论

总体而言,结果表明GA-PEG-PBLA可被视为一种潜在的葛根素纳米颗粒。

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