5-氟尿嘧啶/明胶纳米载药微球的制备及体外性能研究

Preparation and in Vitro Properties of 5-fluorouracil/gelatin Nanocomposite

摘要:

目的：以5-氟尿嘧啶(5-FU)为模型药物，明胶为载体材料，制备5-氟尿嘧啶/明胶纳米载药微球，探究药物的缓释效果和抗肿瘤性能。方法：“单凝聚相法”制备明胶纳米载药微球；透射电镜（TEM）和粒径分析仪（DLS）分析纳米微球的形貌、粒径分布情况；计算其包封率和载药量，并对其体外缓释效果和抗肿瘤性能进行研究。结果：明胶纳米微球的表面形态良好，分散均一，平均粒径65.1?2.1 nm，明胶纳米微球的包封率为23.5?1.9 %，载药量为69.7?0.5 %；明胶微球具有良好的缓释性能，Higuchi方程对微球的体外药物释放情况拟合度较高。四甲基偶氮唑蓝实验结果表明，5-FU/明胶微球对胃癌细胞(SGC7901)具有明显的抑制作用。结论：5-FU/明胶微球缓释性好，抗肿瘤活性显著，可作为抗癌药物的缓释制剂。

Abstract:

Objective: In this study, 5-fluorouracil as the drug model molecules, and gelatin as the carrier of matrine. Methods: The gelatin nanoparticles were prepared by coacervation method, the surface morphology and particle size of the gelatin nanoparticles were observed by Transmission electron microscope (TEM) and Dynamic light scattering (DLS), it's envelopment rate and drug loadings were calculated and the sustained-release effect were detected in vitro. Results: The gelatin nanoparticles had a good surface morphology, the average particle size was 65.1?2.1 nm, dispersed uniformly. The envelopment rate and drug loadings of 5-fluorouracil/ gelatin were 23.5?1.9 % and 69.7?0.5 % respectively. In vitro release experiments displayed that the release of 5-fluorouracil/gelatin nanocomposite accorded with the Higuchi equation, indicating that the gelatin could sustain the release of 5-fluorouracil. MTT measurement showed that the 5-fluorouracil/gelatin nanocomposite has significant cytotoxicity on human gastric cancer cells (SGC7901). Conclusion: The prepared 5-fluorouracil/gelatin nanocomposite has good properties of sustainab release and cytotoxicity and could be used as a kind of drug-loading carrier in the pharmaceutical field.