替莫唑胺聚合物前药及纳米组装体的性质研究

Study on the Properties of Temozolomide Polymer Prodrug and Nanometer Assembly

指出了替莫唑胺(TMZ)是治疗胶质母细胞瘤的一线化疗药物,它是一种疏水性抗癌药,在pH值为7.4的生理环境中容易发生降解,可大大降低药效。将亲水性的葡聚糖与疏水性药物TMZ通过酯化反应生成两亲性聚合物葡聚糖-替莫唑胺结合物(Dex-TMZ),这种聚合物前药可以在水中通过自组装得到纳米粒子(152nm),通过激光动态光散射(DLS)和荧光光谱探讨了该纳米粒子的粒径、电位、临界聚集浓度等性质,通过紫外分光光度计研究了纳米粒子的降解行为。

Temozolomide(TMZ),a first-line chemotherapy drug for glioblastoma,is a hydrophobic anticancer drug that tends to degrade in physiological environments with a pH of 7.4,greatly reducing its potency.In this paper,the hydrophilic dextran and hydrophobic drug TMZ were esterified to produce amphiphilic polymer dextran-temozolomide conjugate(Dex-TMZ).This polymer prodrug can be self-assembled in water to nanoparticles with size of 152 nm.The particle size,potential,critical concentration and other properties of the nanoparticles were studied by laser dynamic light scattering(DLS)and fluorescence spectra,and the degradation behavior of the nanoparticles was studied by ultraviolet spectrophotometer.