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目的制备氟尿嘧啶聚丙交酯乙交酯-聚乙二醇单甲基醚(PLGA-mPEG)纳米粒,并对其体外释放特性进行研究。方法采用纳米沉淀法制备氟尿嘧啶PLGA-mPEG纳米粒,采用高效液相色谱法进行包封率的测定。在单因素实验的基础上,通过正交实验优化处方和制备工艺。采用动态膜透析法对纳米粒子的体外释药特性进行研究。结果制备的纳米粒为较均匀的类球形粒子,平均粒径约124.3 nm,Zeta电位-20.6 mV,平均包封率为(44.72±0.38)%。体外释药实验研究表明,粒子在2 h的突释量小于30%,在突释后的48 h内药物缓慢释放。结论纳米沉淀法操作简单,制备的氟尿嘧啶PLGA-mPEG纳米粒粒径小,体外药物释放具有良好的缓释效果。
Objective To prepare poly (L-lactide-co-glycolide monomethyl ether) (PLGA-mPEG) nanoparticles with fluorouracil and investigate its in vitro release characteristics. Methods Fluorouracil PLGA-mPEG nanoparticles were prepared by nano-precipitation method, and the entrapment efficiency was determined by high performance liquid chromatography. Based on the single factor experiment, the prescription and preparation technology were optimized by orthogonal experiment. Dynamic membrane dialysis was used to study the in vitro release characteristics of nanoparticles. Results The prepared nanoparticles were relatively uniform spherical particles with an average diameter of 124.3 nm and a Zeta potential of -20.6 mV with an average entrapment efficiency of (44.72 ± 0.38)%. In vitro release experiments showed that the burst release of the particles at 2 h was less than 30%, and the drug release slowly within 48 h after the burst release. Conclusions Nanoprecipitation method is simple and easy to prepare. The prepared fluorouracil PLGA-mPEG nanoparticles have small particle size and good drug release in vitro.