顺铂立方液晶纳米粒的处方筛选及制备工艺优化

    Prescription screening and preparation process optimization of cisplatin cubic liquid crystal nanoparticles

    • 摘要:
      目的: 制备顺铂立方液晶纳米粒(Cis–LCNP),通过正交实验确定处方比例及工艺条件,并考察Cis–LCNP的体外药物释放及细胞毒性特性。
      方法: 通过注入法制备Cis–LCNP,以包封率为指标,采用4因素3水平设计正交试验,筛选最优处方工艺;采用偏光显微镜和粒度分析仪考察纳米粒的形态及粒子大小。利用CCK–8毒性检测顺铂和Cis–LCNP对MCF–7细胞的细胞毒性。
      结果: Cis–LCNP最佳处方为甘油单油酸酯900 mg,泊洛沙姆407为100 mg,顺铂90 mg,去离子水30 mL,Cis–LCNP的平均包封率为72.6%,24 h体外累计释放度为79.8%。CCK–8实验显示在一定浓度范围内与顺铂相比,顺铂立方液晶纳米粒的细胞毒性显著高于顺铂,具有更强的细胞毒药物特性。
      结论: 采用注入法制备的Cis–LCNP制备方法简单工艺稳定,具有较好的缓释特性和细胞毒性作用。

       

      Abstract:
      Objective To prepare cisplatin cubic liquid crystal nanoparticles (Cis-LCNP), determine the prescription ratio and process conditions through orthogonal experiments, and investigate the in vitro drug release and cytotoxicity characteristics of Cis-LCNP.
      Methods The Cis-LCNP was prepared by injection method. Taking the encapsulation rate as the index, a 4-factor 3-level orthogonal design experiment was adopted to screen the optimal prescription process. The morphology and particle size of nanoparticles were investigated using a polarizing microscope and particle size analyzer. The cytotoxicity of cisplatin and Cis-LCNP on MCF-7 cells was detected using CCK-8 toxicity.
      Results The optimal prescription of Cis-LCNP was 900 mg of glycerol monooleate, 100 mg of poloxamide 407, 90 mg of cisplatin and 30 mL of deionized water. The average encapsulation rate of Cis-LCNP was 72.6%, and the cumulative release rate in vitro within 24 hours was 79.8%. The CCK-8 experiment showed that within a certain concentration range, compared with cisplatin, the cytotoxicity of cisplatin cubic liquid crystal nanoparticles was significantly higher, and they had stronger cytotoxic drug characteristics.
      Conclusions The Cis-LCNP prepared by injection method is simple in preparation, stable in process, and has good sustained-release characteristics and cytotoxic effects.

       

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