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载药聚氰基丙烯酸正丁酯纳米粒的制备
Preparation of Drug-loaded Polybutylcyanoacrylate Nanoparticles
【作者】 林锦超;
【导师】 张俊卿;
【作者基本信息】 福建医科大学 , 外科学, 2009, 硕士
【摘要】 目的:优化工艺制备吐温80和(或)PEG20000双重修饰的聚氰基丙烯酸正丁酯纳米载体,进一步制备包载福莫司汀、替莫唑胺的聚氰基丙烯酸正丁酯纳米粒。方法:(1)选择α-氰基丙烯酸正丁酯为载体材料,吐温80和(或)PEG20000为表面修饰材料,用乳液聚合法制备双重修饰的聚氰基丙烯酸正丁酯纳米载体。在单因素试验基础上,进行均匀设计,并优化制备工艺。(2)进一步制备包载福莫司汀、替莫唑胺的聚氰基丙烯酸正丁酯纳米粒,通过考察粒径大小和包封率两个指标,优化制备工艺。结果:(1)优化条件下制备的双重修饰的聚氰基丙烯酸正丁酯纳米载体(PBCA-NP)为乳白色胶体溶液,透射电镜观察纳米载体呈圆形,无粘连。粒度分析仪测定平均粒径约137.7nm,粒子分散度(PDI)为0.190。(2)优化条件下制备的包载福莫司汀的聚氰基丙烯酸正丁酯纳米粒(FCNU-PBCA-NP)为乳白色胶体溶液,透射电镜观察纳米粒呈圆形,无粘连。粒度分析仪测定平均粒径为(124.6±5.2)nm,粒子分散度(PDI)范围为0.07-0.16,平均包封率ER为(64.12±2.36)%。(3)优化条件下制备的包载替莫唑胺的聚氰基丙烯酸正丁酯纳米粒(TMZ-PBCA-NP)为乳白色胶体溶液,透射电镜观察纳米载体呈圆形,无粘连。粒度分析仪测定纳米粒平均粒径约125.1nm,粒子分散度(PDI)为0.098,替莫唑胺包封率(ER)约83.02%。结论:首次以α-氰基丙烯酸正丁酯为载体材料,吐温80和(或)PEG20000为表面修饰材料,用乳液聚合法制备双重修饰的聚氰基丙烯酸正丁酯纳米载体,并经优化筛选出最佳制备工艺,并进一步成功制备包载福莫司汀、替莫唑胺的聚氰基丙烯酸正丁酯纳米粒,对拓展福莫司汀、替莫唑胺临床给药新剂型提供一定的参考,并对进一步研究其缓释性和脑靶向性奠定基础。目前国内外未见报道。
【Abstract】 Objective:To prepare polybutylcyanoacrylate(PBCA) nanocarriers with optimized process,double-located with Tween80 and(or) polyethylene glycol(PEG)20000,to further prepare fotemustine polybutylcyanoacrylate nanoparticles(FCNU-PBCA-NP) and temozolomide polybutylcyanoacrylate nanoparticles(TMZ-PBCA-NP).Method:(1)Double-coated PBCA nanocarries was prepared by emulsion polymerization method with butylα-cyanoacrylate(BCA) as carrier materials, Tween80 and(or) PEG20000 as surfactants,and the procedure was optimized by both single factor test and uniform design test.(2) To further prepare fotemustine polybutylcyanoacrylate nanoparticles(FCNU-PBCA-NP) and temozolomide polybutylcyanoacrylate nanoparticles(TMZ-PBCA-NP),and optimize the preparing technology according to the particle size and the embedding ration(ER).Results:(1) The solution of double-coated PBAC-NP under optimum conditions was milk-white colloidal solution and the nanocarriers were circular and non-adhesion through transmission electronic microscopy.The average particle size was about 137.7nm and particle density index(PDI)was about 0.190.(2) The solution of fotemustine polybutylcyanoacrylate nanoparticles(FCNU-PBCA-NP) under optimum conditions was milk-white colloidal solution and the nanocarriers were circular and non-adhesion through transmission electronic microscopy.The average particle size was about(124.6±5.2)nm and particle density index(PDI) was about 0.07~0.16.the average embedding ration(ER) was about(64.12±2.36)%.(3)The solution of temozolomide polybutylcyanoacrylate nanoparticles(TMZ-PBCA-NP) under optimum conditions was milk-white colloidal solution and the nanocarriers were circular and non-adhesion through transmission electronic microscopy.The average particle size was about 125.1nm and particle density index(PDI) was about 0.098.the average embedding ration(ER) was about 83.02%.Conclusion:Double-coated PBCA nanocarries was prepared by emulsion polymerization method with butylα-cyanoacrylate(BCA) as carrier materials, Tween80 and(or) PEG20000 as surfactants for the first time,and the procedure was optimized by uniform design test.fotemustine polybutylcyanoacrylate nanoparticles (FCNU-PBCA-NP) and temozolomide polybutylcyanoacrylate nanoparticles (TMZ-PBCA-NP) were successfully prepared On this basis.They have provided a new direction for fotemutine and temozolomide dosage forms,and laid the foundation for Research for Sustained release and targeting of brain.They have not been reported at home and abroad at present.
【Key words】 polybutylcyanoacrylate; emulsion polymerization method; nanoparticles; fotemustine; temozolomide;
- 【网络出版投稿人】 福建医科大学 【网络出版年期】2009年 10期
- 【分类号】R318.08
- 【被引频次】1
- 【下载频次】232