生物可降解哑铃状高分子共聚物替莫唑胺载药微球的制备与表征  

Preparation and Characterization of Temozolomide-Loaded Microcapsules by Biodegradable Dumbbell-Shaped Triblock Compolymers

作　　者：郭睿[1] 陈明宇[2] 范霄宇[3] 徐建[2] 钟平[2] 戎宗明[1] 

机构地区：[1]华东理工大学化学与分子工程学院,上海200237 [2]复旦大学附属华山医院,上海200040 [3]上海市食品药品检验所,上海201203

出　　处：《华东理工大学学报（自然科学版）》2014年第5期555-561,共7页Journal of East China University of Science and Technology

摘　　要：以生物可降解的哑铃状高分子共聚物材料作为药物载体,饱和替莫唑胺水溶液为选择性溶剂,采用透析法制备了替莫唑胺载药微球。通过动态光散射仪、扫描电镜、紫外分光光度计对替莫唑胺载药微球的粒径分布、表面形貌、载药量及释放行为进行了研究。结果表明:微球载药后其平均粒径不超过800nm,载药量可以达到39.9%;体外释放时间可达900h以上,且可用n级动力学速度方程较为真实地反映其释放行为。细胞实验证明了替莫唑胺载药微球对人源性SHG-44细胞的抑制效果优于替莫唑胺纯药粉末。Self-assembled spherical microparticles and Temozolomide （TMZ）-loaded microcapsules were successfully prepared based on biodegradable dendrimers by dialysis method using Temozolomide saturated solution as selective solvents. The drug-loaded microspheres were characterized by dynamic light scattering （DLS）, scanning electronic microscope （SEM） and UV spectrophotometer to determine their sizes, morphology, drug loading and in vitro release behavior. The results showed that the mean diameter of the drug-loaded microcapsules was under 800 nm, and the drug loading reached 39.9%. Preliminary in vitro release studies revealed a prolonged release, which could last about 900 h. Meanwhile, the release behavior could be better predicted via n-level dynamics velocity equation. MTT assay demonstrated that TMZ-loaded microcapsules offered a greater tumor inhibitory effect than TMZ to SHG-44 human glioblastoma cells growth.

关 键 词：替莫唑胺 哑铃状高分子 载药微球 体外释放 SHG-44细胞 

分 类 号：O631[理学—高分子化学] R318.08[理学—化学]