去氧鬼臼毒素mPEG-PDLLA聚合物胶束的制备及其性质的研究  

Preparation and Physico-chemical Properties of Deoxypodophyllotoxin Polymeric Micelles Using mP EG-PDLLA as a Drug Carrier

作　　者：孙如宁[1] 熊晔蓉[2] 涂家生[3] 

机构地区：[1]中国药科大学高等职业技术学院,南京211198 [2]中国药科大学理学院,南京210009 [3]中国药科大学药学院,南京210009

出　　处：《海峡药学》2016年第4期26-30,共5页Strait Pharmaceutical Journal

基　　金：中央高校基本科研业务费青年项目(ZJ13154)

摘　　要：目的合成聚乙二醇单甲醚-聚乳酸(mPEG-PDLLA)嵌段共聚物,制备去氧鬼臼毒素mPEG-PDLLA嵌段共聚物(DPT-PM),提高去氧鬼臼毒素在水中的溶解度。方法以开环聚合反应合成mPEG-PDLLA,并通过IR、1H-HMR确证其结构,芘荧光探针法测定其临界胶束浓度(CMC);采用溶剂蒸发法制备DPT-PM溶液,并将其冷冻干燥;分别采用动态光散射法(DLS)、透射电子显微镜(TEM)、差示扫描量热法(DSC)、高效液相色谱法(HPLC)等手段对胶束形态、粒径与分布、载药量、包封率等进行表征,并采用透析法考察DPT-PM体外释放,并对释放机制进行探讨。结果制备了去氧鬼臼毒素共聚物胶束,透射电镜下观察为近球形,平均粒径为22.0±8.9nm,载药量为20.67%,包封率为99.63%。结论 m PEG-PDLLA聚合物胶束可作为疏水性药物去氧鬼臼毒素的载体,具有较高的载药性能,能一定程度提高去氧鬼臼毒素在水中的溶解度。OBJECTIVE To synthesis m PEG-PDLLA and prepare deoxypodophyllotoxin polymeric micelles using m PEG-PDLLA as a drug carrier,which can improve the poor solubility. METHODS m PEG-PDLLA was synthesized by ring opening and polymerization reaction. The molecular weight was determined by Infrared spectroscopy（ IR） and1H-HMR. The critical micelle concentration（ CMC） was determined by pyrene fluorescence probe spectrometry. DPT-PM was prepared by solvent evaporation-film dispersion method. The physico-chemical properties of DPT-PM were characterized by dynamic light scattering（ DLS）,transmission electron microscopy（ TEM） and differential scanning calorimeter（ DSC）,respectively. The drug-loading and entrapment efficiency were characterized by HPLC. The property of their release in vitro was investigated by the dialysis method. RESULTS DPT was found to be encapsulated in the micelles; the DPT-PMs were spherical with an average diameter of 22. 0 ± 8. 9nm,drug-loading content of 20. 67%,encapsulation efficiency of 99. 63%. CONCLUSION m PEG-PDLLA can obviously improve the solubility of deoxypodophyllotoxin.

关 键 词：去氧鬼臼毒素 mPEG-PDLLA 溶剂蒸发法 体外释放 

分 类 号：R44[医药卫生—诊断学]