5-氟尿嘧啶聚乙二醇-聚十六烷基氰丙烯酸酯纳米粒的制备  

Preparation of 5-fluorouracil polymer nanoparticles

作　　者：陈婷[1] 贾军[2] 王东凯[1] 叶林茂[1] 张晓君[1] 崔文奇[1] 冷迪[1] 李翔[1] 

机构地区：[1]沈阳药科大学药学院,沈阳110016 [2]沈阳沃森药物研究所,沈阳110179

出　　处：《中国新药杂志》2008年第23期2039-2043,2047,共6页Chinese Journal of New Drugs

摘　　要：目的:以聚乙二醇-聚十六烷基氰丙烯酸酯(PEG-PHDCA)聚合物制备5-氟尿嘧啶(5-Fu)纳米粒,并对其进行体外释药研究。方法:采用溶剂扩散法制备5-Fu PEG-PHDCA纳米粒,在单因素基础上采用正交设计法优化得到最佳处方,并对5-Fu聚合物纳米粒的粒径、Zeta电位、载药量、包封率和体外释放进行了研究。结果:制得的5-Fu聚合物纳米粒的平均粒径为132 nm,Zeta电位为-(12±2)V,载药量为12.3%,包封率为48.8%。体外释放研究发现,5-Fu PEG-PHDCA纳米粒释药近似符合H iguchi释药模型:Q=0.5644+8.386t1/2(r=0.9960)。结论:采用溶剂扩散法制备5-Fu聚合物纳米粒方法简单,重现性好,其体外释放显示出明显缓释作用。Objectives：To prepare 5-fluorouracil （5-Fu） loaded nanoparticles using the biodegradable poly （methoxypolyethyleneglycol eyanoaerylate-co-n-hexadecyl eyanoacrylate） （PEG-PHDCA） ,and to study the characteristics and in vitro release behaviors of the nanoparticles. Methods：5-Fu loaded nanoparticles（NPs） were made by the solvent exchange （nanoprecipitation） method with PEG-PHDCA as carrier materials. The influence of formulation and manufacture was studied with drug loading and encapsulation efficiency as evaluation indexes. Based on the results of single factor experiments,the optimal formulations were verified by orthogonal design. The mean diameter and the size distribution of nanoparticles were determined by photon correlation spectrometry. The zeta potential was determined. The drug loading,incorporation efficiency and release behavior of 5-Fu NPs in vitro were examined by ultraviolet spectrophotometry. Results：The mean size of 5-Fu PEG-PHDCA nanopartieles was 132 nm. The zeta potential, drug loading and encapsulation efficiency were estimated to be -（ 12 ± 2） V, 12.3% and 48.8% , respectively. In vitro release behavior was described by Higuchi equation ： Q = 0. 564 4 ＋ 8. 386t^1/2 （ r = 0. 996 0）. Conclusion：5-Fu can be encapsuled in PEG-PHDCA by solvent exchange method. The method is simple and re, producible. The significant sustained release of 5-Fu PEG-PHDCA nanopaticles is observed in the in vitro study.

关 键 词：5-氟尿嘧啶 聚乙二醇.聚十六烷基氰丙烯酸酯 纳米粒 溶剂扩散法 体外释放 

分 类 号：R943.42[医药卫生—药剂学] R979.12[医药卫生—药学]