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首页> 外文期刊>Cancer biology & therapy >Preliminary pharmacology of galactosylated chitosan/5-fluorouracil nanoparticles and its inhibition of hepatocellular carcinoma in mice
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Preliminary pharmacology of galactosylated chitosan/5-fluorouracil nanoparticles and its inhibition of hepatocellular carcinoma in mice

机译：半乳糖基化壳聚糖/ 5-氟尿嘧啶纳米颗粒的初步药理作用及其对小鼠肝细胞癌的抑制作用

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摘要

Biodegradable polymer nanoparticle drug delivery systems are characterized by targeted drug delivery, improved pharmacokinetic and biodistribution, enhanced drug stability and lowered side effects; these drug delivery systems are widely used for delivery of cytotoxic agents. The galactosylated chitosan (GC)/5-fluorouracil (5-FU) nanoparticle is a nanomaterial made by coupling GC, a polymer known to have the advantages described above, and 5-FU. The GC/5-FU nanoparticle is a sustained release system, it was showed that the peak time, half-life time, mean residence time (MRT) and area of under curve (AUC) of GC/5-FU were longer or more than those of the 5-FU group, but the maximum concentration (Cmax) was lower. The distribution of GC/5-FU in vivo revealed the greatest accumulation in the hepatic cancer tissues, and the hepatic cell was the target of the nanoparticles. Toxicology research showed that the toxicity of GC-5-FU was lower than that of 5-FU in mice. In vivo experiments showed that GC/5-FU can significantly inhibit tumor growth in an orthotropic liver cancer mouse model. GC/5-FU treatment can significantly lower the tumor weight and increase the survival time of mice when compared with 5-FU treatment alone. Flow cytometry and the TUNEL assay revealed that compared with 5-FU, GC/5-FU caused higher rates of G0-G1 arrest and apoptosis in hepatic cancer cells.
机译：可生物降解的聚合物纳米颗粒药物递送系统的特点是靶向药物递送，改善的药代动力学和生物分布，增强的药物稳定性和降低的副作用;这些药物递送系统被广泛用于细胞毒性剂的递送。半乳糖基化壳聚糖（GC）/ 5-氟尿嘧啶（5-FU）纳米颗粒是通过将GC，已知具有上述优点的聚合物和5-FU偶联而制得的纳米材料。 GC / 5-FU纳米颗粒是一种持续释放系统，表明GC / 5-FU的峰时间，半衰期，平均停留时间（MRT）和曲线下面积（AUC）更长或更长时间与5-FU组相比，最大浓度（Cmax）较低。 GC / 5-FU在体内的分布显示出在肝癌组织中的最大积累，并且肝细胞是纳米颗粒的靶标。毒理学研究表明，GC-5-FU的毒性低于5-FU。体内实验表明，GC / 5-FU可以显着抑制正交各向异性肝癌小鼠模型中的肿瘤生长。与单独的5-FU治疗相比，GC / 5-FU治疗可显着降低小鼠的肿瘤重量并延长其存活时间。流式细胞仪和TUNEL分析表明，与5-FU相比，GC / 5-FU在肝癌细胞中引起更高的G0-G1阻滞和凋亡率。

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