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Lysine-mediated hydroxyethyl starch-10-hydroxy camptothecin micelles for the treatment of liver cancer.
Drug Delivery ( IF 6.5 ) Pub Date : 2020-03-31 , DOI: 10.1080/10717544.2020.1745329
Guofei Li 1 , Mingming Zhao 1 , Limei Zhao 1
Affiliation  

Liver cancer is a malignant tumor with extremely high morbidity and mortality. At present, traditional chemotherapy is still the most commonly used therapeutic approach. However, serious side effects lead to the treatment of liver cancer is not ideal. Therefore, it is imperative to develop a new drug delivery system based on nanotechnology and liver cancer microenvironment. In this study, a pH/reduction/α-amylase multi-sensitive hydroxyethyl starch-10-hydroxy camptothecin micelles (HES-10-HCPT-SS-Ly) targeting over-expressed amino acid (AA) transporters on the surface of liver cancer cell by applying lysine were successfully synthesized. The prepared micelles showed regular structure, suitable particle size, and intelligent drug release property. Compared with conventional HES-10-HCPT micelles and 10-HCPT injection, HES-10-HCPT-SS-Ly micelles demonstrated better in vitro anti-proliferative capability toward human liver cancer Hep-G2 cells and greater antitumor efficiency against nude mouse with Hep-G2 tumor. These findings suggest that HES-10-HCPT-SS-Ly micelles may be a promising nanomedicine for treatment of liver cancer.

中文翻译:

赖氨酸介导的羟乙基淀粉-10-羟基喜树碱胶束用于治疗肝癌。

肝癌是具有极高的发病率和死亡率的恶性肿瘤。目前,传统化学疗法仍然是最常用的治疗方法。但是,严重的副作用导致肝癌的治疗并不理想。因此,迫切需要开发一种基于纳米技术和肝癌微环境的新型药物递送系统。在这项研究中,针对肝癌表面过表达的氨基酸(AA)转运蛋白的pH /还原/α-淀粉酶多敏感羟乙基淀粉-10-羟基喜树碱胶束(HES-10-HCPT-SS-Ly)通过应用赖氨酸成功合成细胞。制备的胶束具有规则的结构,合适的粒径和智能的药物释放性能。与传统的HES-10-HCPT胶束和10-HCPT注射液相比,HES-10-HCPT-SS-Ly胶束对人肝癌Hep-G2细胞表现出更好的体外抗增殖能力,对具有Hep-G2肿瘤的裸鼠具有更高的抗肿瘤效力。这些发现表明,HES-10-HCPT-SS-Ly胶束可能是治疗肝癌的有前途的纳米药物。
更新日期:2020-04-20
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