文献：基于甘草酸修饰的DSPE-PEG-PEI纳米粒联合递送阿霉素和Bcl-2 siRNA的肝靶向联合*

链接：https://www.frontiersin.org/journals/pharmacology/articles/10.3389/fphar.2019.00004/full

作者：Guixiang Tian，Ruiyan Pan&，Bo Zhang，Meihua Qu，LianBo Lian，Hong Jiang，Zhiqin Gao，Jingliang Wu

节选：

基于纳米药物递送系统的联合疗法已发展成为一种有前景的策略，它结合了两种或多种**机制。本研究制备了由1,2-二硬脂酰-sn-甘油-3-磷酸乙醇胺-聚乙二醇-聚醚酰亚胺（DSPE-PEG-PEI）和甘草次酸修饰透明质酸（GA-HA）组成的肝靶向纳米粒（GH-DPP），用于联合递送阿霉素（DOX）和Bcl-2 siRNA。

测定了载药GH-DPP纳米粒（siRNA/DOX/GH-DPP）的粒径、zeta电位和形态。分析了其对HepG2细胞的细胞摄取和体外细胞毒性。在荷瘤小鼠中评估了siRNA/DOX/GH-DPP的体内生物分布和***效果。结果表明，siRNA/DOX/GH-DPP纳米粒呈近球形，对HepG2细胞表现出剂量依赖性的细胞毒性。

与单独递送DOX或Bcl-2 siRNA的无甘草次酸共递送系统（siRNA/DOX/DPP）和GH-DPP纳米粒相比，siRNA/DOX/GH-DPP纳米粒能够诱导更多细胞凋亡，并表现出更高的**效果。GH-DPP纳米粒能够同时将化疗药物和siRNA递送至*区域，在***中展现出巨大的潜力。

译文：

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. Compared to Glycyrrhetinic acid-free co-delivery system (siRNA/DOX/DPP) and GH-DPP nanoparticles for delivery of DOX or Bcl-2 siRNA alone, siRNA/DOX/GH-DPP nanoparticles could induce more cellular apoptosis, and showed higher anti-tumor effect. Herein GH-DPP nanoparticles could simultaneously deliver both chemotherapy drugs and siRNA into the tumor region, exhibiting great potential in anti-tumor therapy.

西安齐岳生物提供相关产品：

Cy5-PEG-DPPE

Peptides PEG PLA

DSPE-PEG-SP94

iRGD-PEG-DSPE

PTP-PEG-COOH

Angiopep-2-PEG-N3

DMPE-PEG-CY3

cRGD-PEG-PLGA

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