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首页> 外文期刊>RSC Advances >Surface functionalization of superparamagnetic nanoparticles by an acid-liable polysaccharide-based prodrug for combinatorial monitoring and chemotherapy of hepatocellular carcinoma
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Surface functionalization of superparamagnetic nanoparticles by an acid-liable polysaccharide-based prodrug for combinatorial monitoring and chemotherapy of hepatocellular carcinoma

机译：基于酸的多糖类前药对超顺磁性纳米粒子的表面功能化，用于肝细胞癌的联合监测和化疗

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For combinatorial monitoring and chemotherapy of hepatocellular carcinoma, the macromolecular prodrug based on hyaluronic acid and doxorubicin hydrochloride was prepared by an acid-labile hydrazone linkage, and then conjugated with amine-modified iron oxide nanoparticles by a carbodiimide mediated coupling reaction. The resultant hybrid nanoparticles have the characteristics of good water dispersibility, superparamagnetic property and high magnetic relaxivity for magnetic resonance imaging. In particular, they demonstrated significant cellular uptake and specific accumulation in human hepatocellular liver carcinoma HepG2 cells due to specific biological recognition of hyaluronic acid. In addition, in vitro cumulative release of doxorubicin hydrochloride from the resultant hybrid nanoparticles was significantly accelerated at a mildly acidic pH of 5.0–6.0 when compared to its release at the physiological pH of 7.4, suggesting the pH-responsive feature of this conjugated prodrug for effective chemotherapy of hepatocellular carcinoma. In vivo antitumor efficacy of the mice further confirmed the effect.
机译：为了对肝细胞癌进行组合监测和化学疗法，通过酸不稳定的linkage键制备了透明质酸和阿霉素盐酸盐的大分子前药，然后通过碳二亚胺介导的偶联反应与胺修饰的氧化铁纳米粒子偶联。所得的杂化纳米颗粒具有良好的水分散性，超顺磁性和对磁共振成像具有高磁弛豫性的特征。特别地，由于透明质酸的特异性生物学识别，它们在人肝细胞肝癌HepG2细胞中显示出明显的细胞摄取和特异性积累。此外，与在生理pH值为7.4的释放相比，在5.0-6.0的弱酸性pH下，阿霉素盐酸盐从体外杂种纳米粒子的体外累积释放显着加速。该共轭前药对肝细胞癌有效化疗的反应特征。小鼠的体内抗肿瘤功效进一步证实了该作用。

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