苯甲酰亚胺动态化学键在构筑pH响应药物载体中的应用

SYNTHESIS OF pH RESPONSIBLE DRUG DELIVERY SYSTEMS BY THE INCLUSION OF A DYNAMIC COVALENT BOND,BENZOIC-IMINE

介绍了作者近期利用苯甲酰亚胺化学结构构筑对生理环境pH值响应的药物输送体系的工作进展.亚胺(Schiff碱)作为动态共价键早已为人们所熟知,但其在pH敏感药物输送载体领域的应用并不多.苯甲酰亚胺由于苯环与碳氮双键共轭作用使其在生理pH值下的稳定性更好,同时具有在弱酸环境下(如固态肿瘤细胞外环境、内涵体环境等)的水解特性,适合作为pH响应性单元构筑药物控制释放载体,如聚合物胶束、纳米颗粒等.此外,利用Schiff碱反应随pH值改变的可逆性还可制备可注射凝胶等药物输送体系.

The article highlights the recent approaches on the design and synthesis of drug delivery systems with a dynamic covalent bond,i.e.benzoic-imine,that renders the responsiveness of the vehicles to the pH changes under physiological conditions.Although the characteristics of Schiff base in chemical compounds and polymers have been well documented,recent reports demonstrate the advantages of the derivative benzoic-imine bond on the construction of pH sensitive polymeric micelles,nanoparticles and injectable hydrogels for pharmaceutical applications.In those systems,the benzoic-imine linkage is stable at physiological pH（7.4）,and hydrolyzes following a pH drop to mild acidic,which covers the extracellular pH of solid tumor（6.5）,endosome and lysosome environments（5~6.5）.Therefore the benzoic-imine containing delivery systems are promising in tumor-targeting and intracellular delivery.