以β-环糊精-聚丙烯酸-聚甲基丙烯酸甲酯-聚乙烯吡咯烷酮聚合物为载体制备胶束的可行性研究  

Feasibility Study on the Preparation of Micelles Using β-CD-PAA-PMMA-PVP Polymer as Carrier

作　　者：佃少娜[1] 李桃[1] 余彩萍 黄淑玲[2] 杨帆[2] 

机构地区：[1]广东省人民医院/广东省医学科学院,广州510080 [2]广东药学院,广州510006

出　　处：《中国药房》2014年第29期2737-2740,共4页China Pharmacy

基　　金：广东省科技计划项目(No.2010B030700019);广东省医学科研基金立项课题(No.A2012043)

摘　　要：目的:研究两亲性共聚物β-环糊精-聚丙烯酸-聚甲基丙烯酸甲酯-聚乙烯吡咯烷酮聚合物(β-CD-PPP)作为载体制备胶束的可行性。方法:以长春西汀为模型药物、β-CD-PPP为载体,采用溶剂挥发法制备长春西汀载药胶束,考察其粒径分布、临界胶束浓度、红外表征、形态特征和在不同pH释放介质中的体外释放度。结果:制得的载药胶束载药量为(21.41±0.43)%,包封率为(54.50±1.38)%,平均粒径为86.2 nm,单分散性分布,临界胶束浓度为2.66×10-8g/L,大部分药物被包裹在胶束中,胶束离子均表现出较良好的圆形,在pH 1.0、4.2、6.8、7的释放介质中累积释放度分别为99%(96 h)、96%(216 h)、81%(216 h)、76%(216 h)。结论:β-CD-PPP具有较低的临界胶束浓度和较高的载药量,且能缓慢释放药物,具有pH依赖性,可作为新型给药载体。OBJECTIVE： To study the feasibility of the preparation of micelles using amphiphilic polymer β-cyclodextrin PAA-PMMA-PVP （β-CD-PPP） as carrier. METHODS： The vinpocetine micelles were prepared by solvent evaporation method using vinpocetine （VP） as model material and β-CD-PPP as carrier. The distribution of particle size, the concentration of critical micelle, IR characterization, morphological character and release rate in vitro of micelles in medium with different pH were all investigated. RESULTS： Drug-loading amount of prepared micelles was （21.41 ± 0.43）% , and entrapment efficiency was （54.50 ±1.38） % ; average particle size was 86.2 nm, and the particle was distributed dispersively; the concentration of critical micelle was 2.66x 10^-8 g/L, and most of drugs were coated with micelle and micelle ion was round in shape; accumulative release rates of micelle were 99%（96 h）, 96%（216 h）, 81%（216 h） and 76%（216 h） in medium with pH 1.0, 4.2, 6.8 and 7, respectively. CONCLUSIONS： β-CD-PPP with low concentration of critical micelle and Dendant manner and can be considered as drug delivery carrier.

关 键 词：Β-环糊精 聚丙烯酸 聚甲基丙烯酸甲酯 聚乙烯吡咯烷酮 聚合物 长春西汀 药物载体 

分 类 号：R95[医药卫生—药学]