ZnO基葡萄糖响应性药物载体的制备与性能

Preparation and properties of ZnO-based glucose-responsive drug carrier

采用溶剂热法制备氨基化的介孔ZnO纳米颗粒,通过酰胺化反应将经过EDC/NHS活化的4-羧基苯硼酸(CPBA)结合到氨基化ZnO纳米颗粒上,并负载降糖药二甲双胍;利用苯硼酸能与邻二醇结合的原理,进一步在纳米颗粒表面修饰海藻酸钠(SA),得到具有葡萄糖响应性的SA/CPBA/ZnO药物载体;通过SEM、XRD、FTIR、氮气吸脱附法、Zeta电位等方式对氨基化ZnO、CPBA/ZnO、SA/CPBA/ZnO进行表征。结果表明:CPBA和SA成功结合到氨基化ZnO的表面;SA/CPBA/ZnO具有葡萄糖响应性,当葡萄糖浓度为4 mg/mL时,12 h内药物累计释放率为71.8%,比在1 mg/mL葡萄糖溶液中增加了26.4%,累计释放率在一定范围内与葡萄糖浓度正相关;SA/CPBA/ZnO具有良好的生物相容性,具备作为葡萄糖响应性药物递送体系载体的潜力。

Aminated mesoporous ZnO nanoparticles were prepared by solvothermal method,and 4-carboxyphenylboronic acid(CPBA)activated by EDC/NHS was bound to ZnO nanoparticles by means of amidation reaction,and then the hypoglycemic drug metformin was loaded.Based on the principle that phenylboronic acid can be combined with vicinal diol,sodium alginate(SA)is further modified on the surface of nanoparticles to obtain a glucose-responsive SA/CPBA/ZnO drug carrier.The aminated ZnO,CPBA/ZnO and SA/CPBA/ZnO were characterized by SEM,XRD,FTIR,nitrogen adsorption and desorption method,and Zeta potential,etc.The results show that CPBA and SA are successfully bonded to the surface of aminated ZnO.SA/CPBA/ZnO has glucose responsiveness.When the glucose concentration is 4 mg/mL,the cumulative drug release rate within 12 h is 71.8%,which was 26.4%higher than that in 1 mg/mL glucose solution.The cumulative release rate is positively correlated with glucose concentration within a certain range.In addition,SA/CPBA/ZnO has good biocompatibility and the potential as a delivery carrier of glucose-responsive drug.