摘要
目的制备白藜芦醇(RES)聚合物胶束并对其进行质量评价。方法采用薄膜分散法,以聚乙烯己内酰胺-聚乙酸乙烯酯-聚乙二醇接枝共聚物(SPS)和D-α生育酚聚乙二醇1000琥珀酸酯(TPGS)为载体材料,制备白藜芦醇聚合物胶束(RES-SPS-TPGS-PMs);采用纳米粒度分析仪、差示扫描量热法(DSC)及傅立叶变换红外光谱法(FTIR)对其进行表征;采用高效液相色谱法测定聚合物胶束的包封率和载药量;采用动态膜透析法考察载药胶束的体外释放特性。结果制备的胶束平均粒径为(52.4±0.66)nm,多分散指数为0.06±0.01,包封率为(97.12±9.08)%,载药量为(2.37±0.22)%。白藜芦醇在聚合物胶束中可能以无定型或分子的形式存在,且白藜芦醇与载体材料之间形成了氢键。体外释放结果表明白藜芦醇聚合物胶束具有明显的缓释效果。结论该胶束制备工艺简单,其粒径、包封率、载药量可控,具有缓释作用。
Objective To prepare resveratrol-soluplus-TPGS-polymeric micelles(RES-SPS-TPGS-PMs)and evaluate its quality.Methods The RES-SPS-TPGS-PMs were prepared by the thin film hydration method,and the micelles were characterized by the nanoparticle analyzer,differential scanning calorimeter(DSC)and Fourier transform infrared spectroscopy(FTIR).The HPLC method was established for determining the encapsulation efficiency and drug loading capability.The in vitro release of resveratrol from polymeric micelles was evaluated by dialysis method.Results The particle size and polymer dispersity index(PDI)of RES-SPS-TPGS-PMs were(52.4±0.66)nm and(0.06±0.01),respectively.Encapsulation efficiency and drug loading were(97.12±9.08)%and(2.37±0.22)%,respectively.Resveratrol possibly existed in an amorphous or molecular form in the polymer micelles and the hydrogen bonds were formed between resveratrol and polymer.The release profile showed that resveratrol-loaded polymeric micelles were sustained-release formulations.Conclusions The preparation process of RES-SPS-TPGS-PMs was simple,its particle size,entrapment efficiency and drug loading capacity could be controllable,and it possesses a slow drug-release effect.
作者
周韵秋
冀素平
刘聪
颜雄
典灵辉
ZHOU Yun-qiu;JI Su-ping;LIU Cong;YAN Xiong;DIAN Ling-hui(College of Pharmaceutical Sciences,Guangdong Medical University,Dongguan 523808,China)
出处
《中国医药生物技术》
2020年第1期25-31,共7页
Chinese Medicinal Biotechnology
基金
广东省东莞市社会科技发展（重点）项目（2017507152463）
广东医科大学重点培育项目（Z2017002）
广东省教育厅青年创新人才类项目（2018KQNCX093）
广东省科技计划项目（2014A020212296）
广东省大学生创新创业训练计划项目（201610571016、201710571055、201810571084）
