文獻(xiàn):Liver-Targeted Combination Therapy Basing on Glycyrrhizic Acid-Modified DSPE-PEG-PEI Nanoparticles for Co-delivery of Doxorubicin and Bcl-2 siRNA
文獻(xiàn)鏈接:https://www.frontiersin.org/journals/pharmacology/articles/10.3389/fphar.2019.00004/full
Synthesis of HA-GA and DSPE-PEG-PEI Conjugates
GA-HA conjugate (GH) was synthesized using HA as a hydrophilic segment and GA as a hydrophobic segment (Wu et al., 2016). In brief, GA–NH2 was obtained by adding ethylene diamine to the GA solution in the presence of DMT-MM. And the GA–HA conjugate was synthesized by the chemical modification of GA–NH2 to HA chain.
Syntheses of DSPE-PEG-PEI (DPP) were conducted in one steps as shown in Figure 2. Briefly, PEI was dissolved in DMSO (10 mL) in a 25 mL glass flask, and then functional DSPE-PEG-NHS was added into the reaction solution under stirring. The reaction solution was stirred for 24 h at room temperature. The product was purified by dialysis against distilled water (MWCO 8000-14000 Da), lyophilized, and the chemical structure was confirmed by 1H NMR (in D2O, 300 MHz).
HA-GA和DSPE-PEG-PEI共軛物的合成
使用HA作為親水性鏈段,GA作為疏水性鏈段合成GA-HA偶聯(lián)物(GH)(Wu等人,2016)。簡而言之,GA-NH2是在DMT-MM的存在下通過向GA溶液中加入乙二胺獲得的。GA-HA共軛物是通過將GA-NH2化學(xué)修飾為HA鏈合成的。
如圖2所示,DSPE-PEG-PEI(DPP)的合成是一步完成的。簡而言之,將PEI溶解在25mL玻璃燒瓶中的DMSO(10mL)中,然后在攪拌下將功能性DSPE-PEG-NHS加入反應(yīng)溶液中。反應(yīng)溶液在室溫下攪拌24小時(shí)。通過用蒸餾水(MWCO 8000-14000Da)透析純化產(chǎn)物,凍干,并通過1H NMR(在D2O中,300MHz)確認(rèn)化學(xué)結(jié)構(gòu)。
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