Self-assembled nanoparticle drug delivery systems from galactosylated polysaccharide-doxorubicin conjugate loaded doxorubicin
Self-assembled nanoparticle drug delivery systems from galactosylated polysaccharide-doxorubicin conjugate loaded doxorubicin
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DOI：
10.1016/j.ijbiomac.2009.11.008
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发表时间：
2010-03-01
影响因子：
8.2
通讯作者：
He, Hongxuan
中科院分区：
文献类型：
--
作者：
Cao, Yu;Gu, Ying;He, Hongxuan
将木葡聚糖与多柔比星（DOX）和半乳糖胺接枝，半乳糖胺是可用于将聚合物缀合物靶向肝细胞的末端部分。缀合物中DOX的含量超过5%（wt）。当与过量的去质子化阿霉素在水相中组合时，聚合物药物辅助形成直径为142 μ m的平均尺寸的纳米颗粒药物递送系统（nanoDDS）。体外细胞毒性实验表明，新型纳米给药系统对HepG2细胞的毒性与游离阿霉素相似，而与HeLa细胞共孵育后，新型纳米给药系统的细胞毒性无明显变化。在人肿瘤异种移植裸鼠模型中，新型nanoDDS产生的治疗效果高于非靶向多柔比星纳米颗粒或游离多柔比星。总之，这些结果表明，具有改善的转染效率和肝细胞特异性的新型nanoDDS可能用于肿瘤治疗（C）2009 Elsevier B V保留所有权利
Xyloglucan was grafted with the doxorubicin (DOX) and galactosamine, a terminal moiety that can be used to target polymeric conjugates to liver hepatocytes The content of the DOX was over 5% (wt) in the conjugate. The polymeric drug assisted to form nanoparticle drug delivery systems (nanoDDSs) with an average size of 142 rim in diameter when combined with an excess amount of deprotonated doxorubicin in an aqueous phase. A loading content of doxorubicin is as high as 23 8% in the nanoDDS In an in vitro cytotoxicity experiment, the novel nanoDDS has similar cytotoxicity as free DOX against HepG2 cells In contrast, for the incubation with HeLa cells of the novel nanoDDS, there was no significant cytotoxicity change. In a human tumor xenograft nude mouse model, the novel nanoDDS generated higher therapeutic effect than non-targeted doxorubicin nanoparticles or free doxorubicin. Together, these results suggest that novel nanoDDS, which has improved transfection efficiency and hepatocyte specificity, may be useful for tumor therapy (C) 2009 Elsevier B V All rights reserved