偶氮聚合物类结肠靶向药物载体的合成与降解  

Synthesis and biodegradation of azopolymer as carriers for colon-site specific drug delivery

作　　者：陈建海[1] 陈清元[1] 沈家瑞[2] 

机构地区：[1]广州第一军医大学南方医院药学部,广东广州510515 [2]华南理工大学高分子材料系,广东广州510640

出　　处：《中国药学杂志》2004年第6期471-474,共4页Chinese Pharmaceutical Journal

基　　金：国家自然科学基金课题 (3 9970 876)

摘　　要：目的　设计与合成新型偶氮聚合物类结肠靶向给药载体 ,探讨在模拟结肠环境下材料降解性能与化学结构关系。方法　以对甲基丙烯酰胺偶氮苯 (BMAAB)为偶联剂 ,偶氮二异丁腈 (AIBN)为引发剂 ,甲基丙烯酸羟乙酯 (HEMA)、甲基丙烯酸甲酯(MMA)、甲基丙烯酸 (MAA)为共单体 ,合成聚甲基丙烯酸羟乙酯 甲基丙烯酸 甲基丙烯酸甲酯 [P(HEMA MAA MMA) ]无规偶氮聚合物。用紫外、红外、核磁共振手段进行化学结构测定。测定该材料溶胀性能 ,建立体外厌氧条件下模拟结肠环境模型 ,用凝胶色谱法、差热分析法与扫描电镜法比较聚合物降解前后分子量、热性能与形态变化。结果　材料溶胀指数Q随材料中HEMA MAA含量增加而增大。材料在模拟结构内容液环境中 ,降解程度与材料中亲水组分含量直接相关。结论　该偶氮聚合物可望作为结肠靶向给药系统载体。OBJECTIVE: To design and synthesize a novel vector for colon-site specific drug delivery and investigate the relationship between the biodegradation properties and composition of the materials in simulated colon fluid. METHODS: The azopolymer P (MEMA-MAA-MMA) was synthesized using azobisisobutyronitrilel (AIBN) as initiator, 2-hydroxyethylmethacrylate (HEMA), methacrylic acid (MAA) and methyl methacrylate (MMA) as comonomer, cross-linked with Bis (mathacryloylamino)-azobenzene (BMAAB). The chemical structure of azocopolymer was elucidated with UV and FTIR spectroscopy and nuclear magnetic resonance data. The swelling behavior was evaluated by the swelling equilibrium parameter Q. The biodegradation tests of the materials were carried out in physiologically relevant buffer designed to mimic the colon environment. The biodegradation properties were assessed using Differential Scanning Calorimeters (DSC) and Gel Permeation Chromatography (GPC) and the surface morphology of the material before and after degradation was observed by Scanning Electron Microscopy (SEM). RESULTS: The swelling equilibrium parameter Q increased with the increasing of HEMA and MAA contents in the material. The degradation behavior was relevant to the ratios of the three components in the copolymer. CONCLUSION: This material could become a good carrier for the colon-site specific drug delivery system if the contents of comonmer HEMA, MMA and MAA are adjusted appropriately.

关 键 词：结肠靶向系统 偶氮聚合物 生物降解 

分 类 号：R943.42[医药卫生—药剂学] R945.2[医药卫生—药学]