文獻(xiàn)：基于甘草酸修飾的DSPE-PEG-PEI納米粒聯(lián)合遞送阿霉素和Bcl-2 siRNA的肝靶向聯(lián)合*

鏈接：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

節(jié)選：

基于納米藥物遞送系統(tǒng)的聯(lián)合療法已發(fā)展成為一種有前景的策略，它結(jié)合了兩種或多種**機(jī)制。本研究制備了由1,2-二硬脂酰-sn-甘油-3-磷酸乙醇胺-聚乙二醇-聚醚酰亞胺（DSPE-PEG-PEI）和甘草次酸修飾透明質(zhì)酸（GA-HA）組成的肝靶向納米粒（GH-DPP），用于聯(lián)合遞送阿霉素（DOX）和Bcl-2 siRNA。

測(cè)定了載藥GH-DPP納米粒（siRNA/DOX/GH-DPP）的粒徑、zeta電位和形態(tài)。分析了其對(duì)HepG2細(xì)胞的細(xì)胞攝取和體外細(xì)胞毒性。在荷瘤小鼠中評(píng)估了siRNA/DOX/GH-DPP的體內(nèi)生物分布和***效果。結(jié)果表明，siRNA/DOX/GH-DPP納米粒呈近球形，對(duì)HepG2細(xì)胞表現(xiàn)出劑量依賴(lài)性的細(xì)胞毒性。

與單獨(dú)遞送DOX或Bcl-2 siRNA的無(wú)甘草次酸共遞送系統(tǒng)（siRNA/DOX/DPP）和GH-DPP納米粒相比，siRNA/DOX/GH-DPP納米粒能夠誘導(dǎo)更多細(xì)胞凋亡，并表現(xiàn)出更高的**效果。GH-DPP納米粒能夠同時(shí)將化療藥物和siRNA遞送至*區(qū)域，在***中展現(xiàn)出巨大的潛力。

譯文：

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pg電子官方生物提供相關(guān)產(chǎn)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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