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目的制备包裹5-氟尿嘧啶的二氧化硅(5-Fu/Si O_2)纳米颗粒,并对其药剂学参数及体外细胞毒性进行研究。方法利用反相微乳化法制备5-Fu/Si O_2纳米颗粒,对5-Fu投入量及反应时间等合成条件进行优化,考察纳米颗粒的稳定性及体外释药行为,并采用MTT法对其体外细胞毒性进行研究。结果当5-Fu投入量为1.33 mg及反应时间为24 h时,5-Fu/Si O_2纳米的载药率及包封率达到最高,分别为1.03%及24.77%,同时该纳米在48 h内释放率达到41.31%,7 d内粒径无明显变化。细胞毒性实验表明,5-Fu/Si O_2纳米对人肝癌细胞具有明显的抑制效果,而空白Si O_2纳米对细胞活性影响较小。结论成功制备了稳定性好、缓释时间长的5-Fu/Si O_2纳米颗粒,为开发5-Fu缓释剂型提供了新的思路。
Objective To prepare 5-fluorouracil-coated silica nanoparticles (5-Fu / Si O 2) and study its pharmacokinetics and in vitro cytotoxicity. Methods The 5-Fu / Si O 2 nanoparticles were prepared by reverse microemulsification. The synthesis conditions such as the amount of 5-Fu and the reaction time were optimized. The stability of nano-particles and the release behavior in vitro were investigated. In vitro cytotoxicity was studied. Results When the amount of 5-Fu was 1.33 mg and the reaction time was 24 h, the drug loading rate and entrapment efficiency of 5-Fu / Si O 2 nanoparticles were the highest (1.03% and 24.77%, respectively) The internal release rate reached 41.31%, within 7 d no significant change in particle size. Cytotoxicity experiments showed that 5-Fu / Si O 2 nano-particles had obvious inhibitory effect on human hepatocellular carcinoma cells, while blank Si O 2 nano-particles had little effect on cell activity. Conclusion 5-Fu / Si O 2 nanoparticles with good stability and long sustained release time were successfully prepared, which provided a new idea for the development of 5-Fu sustained release formulations.