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Multifunctional self-assembled micelles of Galactosamine-hyaluronic acid-Vitamin E succinate for targeting delivery of Norcantharidin to Hepatic carcinoma
Carbohydrate Polymers ( IF 10.7 ) Pub Date : 2018-05-31 , DOI: 10.1016/j.carbpol.2018.05.090
Shulong Jiang , Mengying Li , Ying Hu , Zhenhai Zhang , Huixia Lv

A polymer of Galactosamine-hyaluronic acid-Vitamin E succinate (Gal-HA-VES) was designed to prepare multifunctional self-assembled micelles for delivery of Norcantharidin (NCTD) to Hepatic carcinoma. NCTD/Gal-HA-VES showed higher cytotoxicity toward CD44-overexpressing MCF-7 cells, MCF-7/Adr cells and ASGP-R overexpressing HepG2 cells, consistent with the enhanced cellular uptake in the selected cell models, indicating Gal-HA-VES micelles were taken up in MCF-7 and HepG2 cells by CD44 and ASGPR receptor mediated endocytosis, respectively. Moreover, the accumulation of Rhodamine 123 demonstrated that Gal-HA-VES has the same action of TPGS as a P-glycoprotein inhibitor blocked drug efflux-related MDR mechanism in resistant MCF-7/Adr cells. The Cell apoptosis assays indicated that NCTD/Gal-HA-VES were more effective in triggering apoptosis, compared with free NCTD or NCTD/HA-VES groups. In vivo study demonstrated that NCTD/Gal-HA-VES group exhibited enhanced tumor targeting and antitumor activity with lower systemic toxicity. Hence NCTD/Gal-HA-VES micelles system can achieve significant tumor targeting and effective treatment of hepatic carcinoma.



中文翻译:

半乳糖胺-透明质酸-维生素E琥珀酸酯的多功能自组装胶束,用于靶向降冰片素对肝癌的靶向递送

设计半乳糖胺-透明质酸-维生素E琥珀酸酯(Gal-HA-VES)的聚合物,以制备多功能的自组装胶束,以将降冰素(NCTD)递送至肝癌。NCTD / Gal-HA-VES对CD44过表达的MCF-7细胞,MCF-7 / Adr细胞和ASGP-R过表达的HepG2细胞显示出更高的细胞毒性,这与所选细胞模型中细胞摄取的增加相一致,表明Gal-HA- VES胶束分别通过CD44和ASGPR受体介导的内吞作用吸收在MCF-7和HepG2细胞中。此外,若丹明123的积累表明Gal-HA-VES与TP具有与TPGS相同的作用-糖蛋白抑制剂在耐药的MCF-7 / Adr细胞中阻断了与药物外流相关的MDR机制。细胞凋亡试验表明,与游离NCTD或NCTD / HA-VES组相比,NCTD / Gal-HA-VES更有效地触发了细胞凋亡。体内研究表明,NCTD / Gal-HA-VES组表现出增强的肿瘤靶向性和抗肿瘤活性,并具有较低的全身毒性。因此,NCTD / Gal-HA-VES胶束系统可以实现显着的肿瘤靶向和肝癌的有效治疗。

更新日期:2018-05-31
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