2.3. The synthesis of DSPE-PEG-LA

AL Aiyun Liu
HW Huaisong Wang
XH Xiaoshuang Hou
YM Yu Ma
GY Gongjun Yang
YH Yanglong Hou
YD Ya Ding
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To offer an active liver targeting function in liposomes, DSPE-PEG-LA was synthesized by acylation reaction of DSPE-PEG-NH2 and LA under the catalysis of EDC·HCl and NHS. White powders of DSPE-PEG-NH2 (50 mg, 0.018 mmol) and LA (64.5 mg, 0.18 mmol) were dissolved in 2 mL DMSO, respectively, and stirred at room temperature for 2 h. And then, EDC·HCl (34.5 mg, 0.18 mmol), NHS (20.7 mg, 0.18 mmol), and triethylamine (TEA, 3 μL) were added into the mixture to stirred overnight at room temperature. The reaction solution was dialyzed (MWCO 2000 Da) against deionized water for 24 h. The product was lyophilized to obtain white powder (47.5 mg, yield 84.7%). 1H NMR (DMSO-d6): δ 0.85 (s, 6H), 1.23 (s, 64H), 3.31–3.51 (m, 180H, broad), 3.74 (s, 4H), 3.86 (s, 2H), 4.72 (s, 1H), 7.90 (s, 2H). IR (KBr): υmax 3407, 2917, 2888, 1740, 1660, 1547, 1334, 1111, 721 cm−1.

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