载氟尿嘧啶纳米粒的制备及SGC-7901胃癌细胞株的摄取实验

Preparation of targeting nanoparticles loaded with fluorouracil and its uptake test by SGC-7901 gastric carcinoma cells

目的:制备载氟尿嘧啶的纳米粒,并考察其体外释放性能和胃癌细胞株对其的摄取能力。方法:以聚乙二醇单甲醚-聚乳酸乙醇酸-聚赖氨酸-(缬氨酸-精氨酸-甘氨酸-天冬氨酸-谷氨酸)环肽(PEAL-cRGD)为载体,用乳化-溶剂蒸发法制备氟尿嘧啶纳米粒,以粒径和包封率为评价指标,通过正交试验设计筛选最优制备工艺,并测定SGC-7901胃癌细胞株对该纳米粒的摄取能力。结果:以最优工艺制备的纳米粒为大小均匀的球形,粒径(172.9±2.3)nm,包封率(75.31±1.91)%,在pH7.4磷酸盐缓冲液中192h累积释放率为(58.63±2.47)%。SGC-7901胃癌细胞株能有效摄取该纳米粒。结论:本研究制备的氟尿嘧啶纳米粒包封率较高,粒径较小,能促进胃癌细胞对氟尿嘧啶的摄取。

Objective： To prepare fluorouracil nanoparticles and evaluate its drug release properties in vitro and its uptake effect by SGC-7901 gastric carcinoma cells. Methods： The {luorouracil nanoparticles were prepared by emulsification-solvent evaporation method,by using polyethylene glycol monomethyl ether-polylactic glycolic acid-polylysine-（valine-arginine-glycine- aspartic acid-glutamic acid） cyclic peptides as a carrier. The preparation was optimized by orthogonal design with particle diame- ter and encapsulation efficiency as evaluation indexes. The uptake efficiency of the nanoparticles by SGC-7901 gastric carcinoma cells was investigated. Results： The nanoparticles prepared by optimal technology were spherical with a diameter of （172.9±2.3） nm and encapsulation efficiency of （75.31±1.91） %. The in vitro cumulative drug release rate in pH 7.4 phosphate buffer during 192 h was （58. 63±2. 47）%. The nanoparticles could effectively be taken by SGC 7901 gastric carcinoma cells. Conclusion： The targeting nanoparticles loaded with fluorouracil possess the properties of high encapsulation efficiency and par- ticles of small diameter. They could enhance the uptake of fluorouracil by SGC-7901 gastric carcinoma cells.