標(biāo)題：Liposomes Modified with Cyclic RGD Peptide for Tumor Targeting（環(huán)RGD肽修飾脂質(zhì)體的腫瘤靶向性研究）

文獻(xiàn)鏈接：https://xueshu.baidu.com/usercenter/paper/show?paperid=5ed88386737462844d7fe9a0bd7fc650&site=xueshu_se

作者：Praveen，K.，Dubey，Vivek，Mishra，Sanyog，Jain，Sunil，Mahor，S.P.

摘要：

Cyclic RGD peptide anchored sterically stabilized liposomes (RGD-SL) were investigated for selective and preferential presentation of carrier contents at angiogenic endothetial cells overexpressing &alphanuβ3 integrins on and around tumor tissue and thus for assessing their targetabilty. Liposomes were prepared using distearoylphosphatidylcholine (DSPC). cholesterol and distearoylphosphatldylethanolamine-polyethyleneglycol- RGD peptide conjugate (DSPE-PEG-RGD) in a molar ratio 56:39:5. The control RAD peptide anchored sterically stabilized liposoines (RAD-SL) and liposome with 5 mol% PEG (SL) without peptide conjugate which had similar lipid composition were used for comparison. The average size of all liposome preparations prepared was approximately 105 nm and maximum drug entrapment was 10.2 ± 1.1%. In vitro endothelial cell binding of liposomes exhibited 7-fold higher binding of RGD-SL to HUVEC in comparison to the SL and RAD-SL.

譯文：

研究了環(huán)RGD肽錨定的立體穩(wěn)定脂質(zhì)體（RGD-SL）對腫瘤組織及其周圍血管生成內(nèi)皮細(xì)胞中過表達(dá)α-NUβ3整合素的載體含量的選擇性和選擇性呈現(xiàn)，從而評估其靶向性。用二硬脂酰磷酰膽堿（DSPC）制備脂質(zhì)體。膽固醇和二硬脂酰磷酸二乙醇胺聚乙二醇-RGD肽偶聯(lián)物（DSPE-PEG-RGD），摩爾比56:39:5。對照RAD-肽錨定的立體穩(wěn)定脂質(zhì)體（RAD-SL）和含有5 mol%PEG（SL）的脂質(zhì)體（不含多肽偶聯(lián)物，具有相似的脂質(zhì)組成）用于比較。制備的脂質(zhì)體平均粒徑約為105 nm，*大包封率為10.2±1.1%。在體外，脂質(zhì)體與內(nèi)皮細(xì)胞的結(jié)合顯示RGD-SL與HUVEC的結(jié)合比SL和RAD-SL高7倍。

DOI:10.1080/10611860410001728040

主要應(yīng)用方向

1. 靶向脂質(zhì)體與納米載體構(gòu)建

• DSPE部分可嵌入脂質(zhì)雙層，PEG鏈延伸至表面，RGD實(shí)現(xiàn)與細(xì)胞整合素結(jié)合；

• 廣泛用于遞送系統(tǒng)，如核酸載體、藥物包載納米粒、固體脂質(zhì)納米粒等。

2. 表面功能化與細(xì)胞黏附調(diào)控

• 將該分子插入聚合物材料、納米顆�；騻鞲衅鞅砻�；

• 提高特定細(xì)胞（如血管內(nèi)皮細(xì)胞、腫瘤來源細(xì)胞）對材料的識別與附著。

3. 細(xì)胞成像與示蹤系統(tǒng)

• 可與熒光染料/探針共用，提升探針對細(xì)胞的靶向攝取效率；

• 支持構(gòu)建可視化追蹤工具。

4. 體內(nèi)靶向轉(zhuǎn)運(yùn)研究

• 在動物模型中實(shí)現(xiàn)對RGD整合素陽性組織（如某些病變血管）的主動聚集；

• 可配合診斷或治療載體進(jìn)行深入機(jī)制探究。

西安pg電子官方生物提供相關(guān)產(chǎn)品：

DSPE-PEG-RGD

DSPE-PEG-cRGD  

DSPE-PEG-iRGD 

DSPE-PEG-SP94

DSPE-PEG-RVG29 

DSPE-PEG-GPC3  

DSPE-PEG-ANG-2  

DMG-PEG-cRGD 

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