灯盏乙素-PEG-PLGA载药纳米粒的制备及质量评价.PDFVIP

灯盏乙素-PEG-PLGA载药纳米粒的制备及质量评价 祖洪碧＊，李小华（重庆市长寿区人民医院药学部，重庆 401220） 中图分类号 R943 文献标志码 A 文章编号 1001-0408（2015）19-2705-04 DOI 10.6039/j.issn.1001-0408.2015.19.35 摘 要 目的：制备灯盏乙素-聚乙二醇-聚乳酸/羟基乙酸共聚物（PEG-PLGA）载药纳米粒，优化其处方，并进行质量评价。方法： 采用复乳-溶剂蒸发法制备灯盏乙素-PEG-PLGA 载药纳米粒。以包封率为评价指标，以初乳与外水相的比例、灯盏乙素和 PEG-PLGA 质量浓度为因素，通过单因素试验和正交试验优化处方；测定最优处方所制纳米粒的表观形态、粒径、Zeta 电位、载药 ∶ 量、包封率和稳定性。结果：最优处方为初乳与外水相的比例 1 15，灯盏乙素质量浓度 10 mg/ml，PEG-PLGA 质量浓度 15 mg/ml。 所制得纳米粒为圆形或椭圆形，平均粒径为（78.54±2.21）nm，Zeta 电位为（－23.07±1.39）mV，载药量为（1.67±0.12）％，包封率 为（45.32±1.29）％；纳米粒在 4 ℃下保存 3 个月内粒径和包封率无明显变化。结论：成功制得具有较好理化性质和稳定性的灯盏 乙素-PEG-PLGA纳米粒。 关键词 灯盏乙素；聚乙二醇-聚乳酸/羟基乙酸共聚物；纳米粒；包封率；粒径 Preparation and Quality Evaluation of Scutellarin-PEG-PLGA Drug-loaded Nanoparticles ZU Hong-bi，LI Xiao-hua（Dept. of Pharmacy，People’s Hospital of Chongqing Changshou District，Chongqing 401220，China） ABSTRACT OBJECTIVE：To prepare the scutellarin-PEG-PLGA drug-laded nanoparticles，optimize the formulation with ratio of colostrum and external aqueous phase，mass concentration of scutellarin and PEG-PLGA as factors and conduct quality evalua- tion. METHODS：A double emulsion-solvent evaporation method was adopted to prepare the scutellarin-PEG-PLGA nanoparticles. With the evaluation index of encapsulation efficiency，single factor and orthogonal test were used to determine the apparent shape， particle size，Zeta potential，drug loading amount，encapsulation efficiency and stability of prepared nanoparticles by optimized for- mulation with ratio of colostrum and external aqueous phase，mass concentration of scutellarin and PEG-PLGA as factors. RE- ∶ SULTS：The ratio of colostrum and external aqueous phase was 1 15 and the mass