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分别采用酰肼(HYD)、酰肼氨基苯甲酸酯(ABZ)和甘氨酸酰肼(GLY)为连接剂,将模型药物多柔比星(DOX)与聚乙二醇-聚(门冬氨酸)共聚物通过腙键(该键在pH<7的环境中会降解而在生理环境中较稳定)连接,制备了3种pH敏感但释药速率不同(HYD胶束>ABZ胶束>GLY胶束)的聚合物胶束。研究显示,释药速率最慢的胶束在体外试验中杀伤肿瘤细胞的能力显著优于游离药物和释药速率较快的胶
The model drug, doxorubicin (DOX) and polyethylene glycol-poly (aspartame, respectively) were synthesized using hydrazide (HYD), hydrazide aminobenzoate (ABZ) and glycine hydrazide (GLY) Acid) copolymer was linked via a hydrazone bond, which degrades in the pH <7 environment and is more stable in the physiological environment, to prepare three pH sensitive but different drug delivery rates (HYD micelles> ABZ micelles> GLY Micelles) of polymeric micelles. Studies have shown that micelles with the slowest rate of release kill tumor cells significantly better in vitro than free drugs and faster release rates