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首页> 外文期刊>RSC Advances >Fabrication and characterization of a novel self-assembling micelle based on chitosan cross-linked pectin-doxorubicin conjugates macromolecular pro-drug for targeted cancer therapy
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Fabrication and characterization of a novel self-assembling micelle based on chitosan cross-linked pectin-doxorubicin conjugates macromolecular pro-drug for targeted cancer therapy

机译：基于壳聚糖交联果胶蛋白缀合物的新型自组装胶束的制造与表征靶癌治疗的大分子药物

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摘要

Cancer is one of the leading causes of morbidity and mortality worldwide. Doxorubicin is one of the most effective anticancer drugs approved by FDA. However, like all the other anticancer drugs, the efficacy of DOX is associated with high systemic toxicity to healthy tissues. In this study, chitosan cross-linked pectin-doxorubicin conjugates macromolecular pro-drug (CS-PDC-M) was prepared to enhance the therapeutic effects on liver cancer. CS-PDC-M was characterized in terms of size, size distribution, zeta potential, scanning electron microscope (SEM) and drug loading content. The CS-PDC-M achieved prolonged releasing ability was demonstrated by the in vitro drug release and in vitro cellular uptake assay. Biocompatibility of CS-PDC-M was screened by hemolysis activity examination, BSA adsorption test and cell viability evaluation in endothelial cells and LO2 cells. The CS-PDC-M achieved significantly high antitumor efficiency and targeting efficiency, which was demonstrated by the in vitro MTT assay and cellular targeting assay toward HepG2 cells, MCF-7 cells and A549 cells. The in vivo antitumor efficacy of CS-PDC-M was studied in athymic BALB/c nude mice bearing HepG2 cell xenografts. The organ damage assays of CS-PDC-M was studied in SD rats. Compared with that of free DOX and PDC-M, the CS-PDC-M exhibited higher antitumor efficacy and lower toxicity, implying that CS-PDC-M is a highly promising drug delivery system for hepatocellular carcinoma treatment.
机译：癌症是全世界发病率和死亡率的主要原因之一。 Doxorubicin是FDA批准的最有效的抗癌药物之一。然而，与所有其他抗癌药物一样，DOX的疗效与对健康组织的高系统毒性有关。在该研究中，制备壳聚糖交联果胶蛋白缀合物大分子促药（CS-PDC-M）以增强对肝癌的治疗作用。 CS-PDC-M以尺寸，尺寸分布，Zeta电位，扫描电子显微镜（SEM）和药物负载含量为特征。通过体外药物释放和体外蜂窝摄取测定，证明了CS-PDC-M实现的长时间释放能力。通过溶血活性检查，BSA吸附试验和内皮细胞和LO2细胞的细胞活力评估筛选CS-PDC-M的生物相容性。 CS-PDC-M通过体外MTT测定和朝向HepG2细胞，MCF-7细胞和A549细胞进行了显着高的抗肿瘤效率和靶向效率，并通过体外MTT测定和细胞靶向测定来证明。 CS-PDC-M的体内抗肿瘤效果在轴承HepG2细胞异种移植物中的含硼Balb / C裸鼠中研究。在SD大鼠中研究了CS-PDC-M的器官损伤测定。与游离DOX和PDC-M相比，CS-PDC-M表现出更高的抗肿瘤功效和较低的毒性，这意味着CS-PDC-M是用于肝细胞癌治疗的高度有前景的药物递送系统。

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  • 来源
    《RSC Advances》 |2018年第22期|共13页
  • 作者

    Li Zhi-Ping; Jiang Ming-Chao; Chen Bo; Gao Pei; Yang Sa; Liu Yu-Feng; Ye Peng-Ju; He Dong-Xiu; Huang Hong-Lin; Yu Cui-Yun;

  • 作者单位

    Univ South China Hunan Prov Cooperat Innovat Ctr Mol Target New Dr Hengyang 421001 Peoples R China;

    Univ South China Hunan Prov Cooperat Innovat Ctr Mol Target New Dr Hengyang 421001 Peoples R China;

    Univ South China Hunan Prov Cooperat Innovat Ctr Mol Target New Dr Hengyang 421001 Peoples R China;

    Eastern Kentucky Univ Chem Dept Richmond KY 40475 USA;

    Univ South China Hunan Prov Cooperat Innovat Ctr Mol Target New Dr Hengyang 421001 Peoples R China;

    Univ South China Hunan Prov Cooperat Innovat Ctr Mol Target New Dr Hengyang 421001 Peoples R China;

    Univ South China Hunan Prov Cooperat Innovat Ctr Mol Target New Dr Hengyang 421001 Peoples R China;

    Univ South China Hunan Prov Cooperat Innovat Ctr Mol Target New Dr Hengyang 421001 Peoples R China;

    Univ South China Hunan Prov Cooperat Innovat Ctr Mol Target New Dr Hengyang 421001 Peoples R China;

    Univ South China Hunan Prov Cooperat Innovat Ctr Mol Target New Dr Hengyang 421001 Peoples R China;

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  • 正文语种 eng
  • 中图分类 化学;
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