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生物可降解Dex-APBA-IBU偶联物的合成和表征

Synthesis and Characterization of Biodegradable Dex-APBA-IBU Conjugate
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摘要 首先制备了布洛芬-3-氨基苯硼酸单体(IBU-APBA),之后,通过3-氨基苯硼酸的双羟基和葡聚糖(Dextran)的邻位二醇生成的硼酯缀合形成了Dex-APBA-IBU聚合物-药物偶联物,利用核磁共振波谱仪氢谱(1H-NMR)、傅立叶变换红外光谱仪(FT-IR)对单体和偶联物的结构进行表征,测试结果证明了单体和偶联物的成功合成。以质子泵抑制剂奥美拉唑(OME)为模型药物,使用滴加法技术将Dex-APBA-IBU偶联物组装制备了包载OME的Dex-APBA-IBU纳米粒子,利用紫外分光光度计测得Dex-APBA-IBU纳米粒子的载药量为15%±2. 0%。 Phenylboronic acid-modified Ibuprofen(IBU-APBA)monomer was first synthesized by amidation reaction.Then,Dex-APBA-IBU polymer-drug conjugate was formed by conjugation of the dihydroxy group of 3-aminophenylboronic acid with the ortho-diol of dextran.The structures of monomer and polymer were detenmined by 1H-NMR and FT-IR.Using the proton pump inhibitor omeprazole(OME)as a model drug,Dex-APBA-IBU conjugate was assembled to prepare Dex-APBA-IBU nanoparticles by dropwise addition technique.The drug loading of Dex-APBA-IBU nanoparticles measured by UV spectrophotometer was 15%±2.0%.
作者 高亚钗 Gao Yachai(School of Materials Science and Engineering,Tiangong University,Tianjin 300387,China)
出处 《山东化工》 CAS 2020年第9期13-14,17,共3页 Shandong Chemical Industry
关键词 布洛芬 聚合物-药物偶联物 葡聚糖 硼酯键 ibuprofen polymer-drug conjugate dextran boron ester bond
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