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乳酸-羟基乙酸共聚物包载匹伐他汀纳米粒的制备及其对内皮祖细胞的增殖作用

Preparation of pitavastatin-loaded poly lactic-co-glycolic acid nanoparticles and their effects on proliferation of endothelial progenitor cells

  • 摘要: 制备乳酸-羟基乙酸共聚物(PLGA)包载匹伐他汀纳米粒,检测其形貌、粒径、载药量、包封率及体外释药特点,研究其对内皮祖细胞的增殖作用。采用溶剂扩散法制备PLGA包载的匹伐他汀纳米粒,扫描电镜观察纳米粒形貌,激光粒度仪测定粒径,高效液相色谱法检测并计算载药量、包封率,体外药物释放实验检测纳米粒的缓释效能,CCK8法检测空白PLGA纳米粒及匹伐他汀纳米粒对内皮祖细胞的活性影响。扫描电镜下匹伐他汀纳米粒呈圆球形,平均粒径在(230.1±45)nm,载药量与包封率分别为(10.00±1.83)%、(35.54±5.40)%,具备缓释性能,不同浓度空白PLGA纳米粒对内皮祖细胞活性均无影响,匹伐他汀纳米粒组(0.01、0.1 μmol/L)可显著改善内皮祖细胞的增殖活性,与同浓度匹伐他汀原药组相比差异显著。结果表明,溶剂扩散法可制备形态较好的匹伐他汀纳米粒,具备缓释性能,载体材料具有较好的细胞生物相容性,匹伐他汀纳米粒显著改善内皮祖细胞增殖活性。

     

    Abstract: The objectives of this study were to prepare pitavastatin-loaded poly lactic-co-glycolic acid nanoparticles(PLGA), to characterize their pharmaceutical properties, to conduct in vitro drug-release from the nanoparticles, and to observe the effects on the proliferation of endothelial progenitor cells. Both pitavastatin-loaded PLGA and blank PLGA nanoparticles were prepared using emulsion-solvent diffusion method with PLGA being carrier materials. Morphology of the nanoparticles was observed by scanning electron microscopy(SEM), and particle size was analyzed by laser nanometer particle size analyzer. The drug loading and encapsulation efficiency were assayed using high-performance liquid phase. Impact of blank and pitavastatin-loaded nanoparticles on the viability of endothelial progenitor cells was investigated by CCK8 method. Pitavastatin-loaded PLGA nanoparticles exhibited the structure with spherical shape, smooth surface and average diameter of(230. 1±45)nm. The drug loading capacity and encapsulation efficiency were(10. 00±1. 83)% and(35. 54±5. 40)%, respectively. In vitro sustained-release of pitavastatin from the nanoparticles was found. The blank PLGA nanoparticles had no effect on the viability of the endothelial progenitor cells in different concentrations. Compared with pitavastatin group, pitavastatin-loaded nanoparticles(0. 01 μmol/L, 0. 1 μmol/L)had more effects on the proliferation of endothelial progenitor cells. In conclusion, emulsion-solvent diffusion method is applicable in preparation of pitavastatin-loaded PLGA nanoparticles with good shape and sustained-release of interest. Pitavastatin-loaded nanoparticles could significantly improve proliferation of the endothelial progenitor cells.

     

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