文献：Liver-Targeted Combination Therapy Basing on Glycyrrhizic Acid-Modified DSPE-PEG-PEI Nanoparticles for Co-delivery of Doxorubicin and Bcl-2 siRNA

文献链接：https://xueshu.baidu.com/usercenter/paper/show?paperid=13620650816s00y0k60q02j0k0742988&site=xueshu_se

作者：G Tian，R Pan，B Zhang，M Qu，J Wu

摘要：

Combination therapy based on nano-sized drug delivery system has been developed as a promising strategy by combining two or more anti-tumor mechanisms. Here, we prepared liver-targeted nanoparticles (GH-DPP) composed of 1,2-distearoyl-sn-glycero-3-phosphoethanolamine-polyethylene glycol-polyetherimide (DSPE-PEG-PEI) with Glycyrrhetinic acid-modified hyaluronic acid (GA-HA) for co-delivery of doxorubicin (DOX) and Bcl-2 siRNA. Particles size, zeta potential and morphology were determined for the drug-loaded GH-DPP nanoparticles (siRNA/DOX/GH-DPP). Cellular uptake and in vitro cytotoxicity were analyzed against HepG2 cells. In vivo bio-distribution and anti-tumor therapeutic effects of siRNA/DOX/GH-DPP were evaluated in H22-bearing mice. The results showed that siRNA/DOX/GH-DPP nanoparticles were nearly spherical and showed dose-dependent cytotoxicity against HepG2 cells. 

基于纳米级药物递送系统的联合治疗已被开发为一种有前景的策略，通过结合两种或多种抗肿瘤机制。在这里，我们制备了由1,2-二硬脂酰基-sn-甘油-3-磷酸乙醇胺-聚乙二醇聚醚酰亚胺（DSPE-PEG-PEI）和甘草次酸修饰的透明质酸（GA-HA）组成的肝靶向纳米颗粒（GH-DPP），用于阿霉素（DOX）和Bcl-2 siRNA的共递送。测定了载药GH-DPP纳米颗粒（siRNA/DOX/GH-DPP）的粒径、ζ电位和形态。对HepG2细胞的细胞摄取和体外细胞毒性进行了分析。在携带H22的小鼠体内评估siRNA/DOX/GH-DCP的体内生物分布和抗肿瘤治疗效果。结果表明，siRNA/DOX/GH-DCP纳米颗粒呈近球形，对HepG2细胞具有剂量依赖性细胞毒性。

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DSPE-PEG-Cy7

DSPE-PEG-cRGD

DPPE-PEG-cRGD

DMPE-PEG-cRGD

DOPE-PEG-cRGD

DPPE-PEG-RGD

DMPE-PEG-RGD

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