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​ DSPE-PEG-PEI共轭物的合成
发布时间:2025-07-02     作者:zyl   分享到:

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

作者:Guixiang Tian&#x;Guixiang Tian1†Ruiyan Pan&#x;Ruiyan Pan2†Bo Zhang&#x;Bo Zhang2†Meihua QuMeihua Qu2Bo LianBo Lian1Hong JiangHong Jiang1Zhiqin Gao*Zhiqin Gao1*Jingliang Wu*Jingliang Wu1*

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


Synthesis of DSPE-PEG-PEI Conjugates

Bi-functional DSPE-PEG-NHS was used to conjugate with PEI via the primary amine reactive NHS ester moiety at weakly basic pH, thus avoiding the conjugation and crosslinking of the maleimide groups to the amine functions of PEI, which occurs at higher pH (pH > 8). The structure of DSPE-PEG-NHS, PEI and resulting DSPE-PEG-PEI copolymer were verified by 1H NMR. The peaks of PEG (3.6 ppm, -CH2O-), DSPE (1.0–1.5 ppm, -CH2-) and PEI (2.5–3.0 ppm, CH2-N) were confirmed. The1H-NMR spectrum of DSPE-PEG-PEI in D2O exhibited characteristic peaks at 2.5–3.0 ppm (peaks of PEI), 3.6 ppm (peaks of PEG) and 1.0–1.5 ppm (peaks of DSPE), indicating that PEI was successfully introduced to the DSPE-PEG-NHS molecular.

  DSPE-PEG-PEI

DSPE-PEG-PEI共轭物的合成

双官能DSPE-PEG-NHS用于在弱碱性pH下通过伯胺反应性NHS酯部分与PEI偶联,从而避免了马来酰亚胺基团与PEI胺官能团的偶联和交联,这在较高pH值(pH>8)下发生。

通过1H NMR验证了DSPE-PEG-NHS、PEI和所得DSPE-PEG-PEI共聚物的结构。PEG(3.6ppm,-CH2O-)、DSPE(1.0-1.5ppm,-CH2-)和PEI(2.5-3.0ppm,CH2-N)的峰已被确认。

D2O中DSPE-PEG-PEI的1H NMR光谱在2.5-3.0 ppm(PEI峰)、3.6 ppm(PEG峰)和1.0-1.5 ppm(DSPE峰)处显示出特征峰,表明PEI已成功引入DSPE-PEG-NHS分子。

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