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目的制备载吉西他滨(gemcitabine,GemC)的介孔二氧化硅纳米粒(mesoporous silica nanoparticles,MSN),并对其体内外抗肿瘤活性进行评价。方法采用聚合法制备Gem C-MSN,采用激光粒度仪测定纳米粒的粒度分布和电位,并通过透射电镜对纳米粒的形态进行表征。应用UV评价纳米粒的载药量、包封率及体外释放特性。采用MTT染色法考察GemC-MSN对A549细胞的体外细胞毒性。建立体内肿瘤动物模型,评价纳米粒的体内抗肿瘤活性。结果纳米粒分布均一,平均粒径为107.29 nm,PDI为0.167,Zeta电位为0.107 m V;药物的载药量和包封率分别为(37.31±1.25)%和(87.37±2.12)%;体外释放结果显示,纳米粒具有一定的缓释作用,96 h时释放达到平衡;体内外抗肿瘤试验结果表明,GemC-MSN较游离GemC具有更强的抗肿瘤活性。结论 MSN作为药物的新型载体,具有良好的生物相容性,并能显著提高GemC的载药量,控制药物的缓慢释放,能显著提高GemC的体内外抗肿瘤活性,将为GemC新型给药系统的深入研究提供参考。
Objective To prepare mesoporous silica nanoparticles (MSN) for gemcitabine (GemC) and evaluate the antitumor activity in vitro and in vivo. Methods Gem C-MSN was prepared by polymerization. The particle size distribution and potential of the nanoparticles were measured by laser particle sizer. The morphology of the nanoparticles was characterized by transmission electron microscopy. The drug loading, entrapment efficiency and in vitro release characteristics of nanoparticles were evaluated by UV. In vitro cytotoxicity of GemC-MSN on A549 cells was examined by MTT staining. Animal models of tumor in vivo were established to evaluate the antitumor activity of the nanoparticles in vivo. Results The average particle size was 107.29 nm, the PDI was 0.167 and the Zeta potential was 0.107 mV. The drug loading and entrapment efficiency of the drug were (37.31 ± 1.25)% and (87.37 ± 2.12)%, respectively. In vitro Release results showed that the nanoparticles have a sustained release effect, 96 h release to achieve balance; anti-tumor in vitro and in vivo results show that, GemC-MSN GemC than free GemC has more anti-tumor activity. Conclusion MSN as a new drug carrier has good biocompatibility, and can significantly improve the drug loading of GemC, control the slow release of drugs, can significantly increase the anti-tumor activity of GemC in vitro and in vivo, will be the new GemC drug delivery system Provide a reference for further research.