中国中药杂志

2011, v.36(11) 1431-1435

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硫酸长春新碱聚氰基丙烯酸正丁酯纳米粒制备及药剂学性质研究
Preparation and in vitro release characteristics of vincristine sulphate loaded poly(butylcyanoacrylate) nanoparticles

谭蓉;刘颖;冯年平;赵继会;
TAN Rong,LIU Ying,FENG Nianping,ZHAO Jihui(Department of Pharmaceutics,Shanghai University of Traditional Chinese Medicine,Shanghai 201203,China)

摘要(Abstract):

目的:制备硫酸长春新碱聚氰基丙烯酸正丁酯纳米粒(VCR-PBCA-NPs)并进行释药动力学研究。方法:采用乳化聚合法制备VCR-PBCA-NPs,考察纳米粒形态和粒径分布,测定包封率和载药量,采用星点设计效应面法优化处方;采用透析法进行体外释放研究,并利用药物释放模型方程拟合释放曲线。结果:制得的纳米粒形态圆整,平均粒径(98.9±3.05)nm,包封率(55.23±0.96)%,载药量(7.87±0.11)%,体外释放曲线符合W e ibu ll方程。结论:本研究制备了VCR-PBCA-NPs,其体外释放速度较慢,具有一定的缓释特征。
Objective:To prepare vincristine sulphate loaded poly(butylcyanoacrylate) nanoparticles(VCR-PBCA-NPs) and to investigate the in vitro release charactersitics.Method:VCR-PBCA-NPs were prepared by emulsion polymerization method,and characterized for morphology,particle size,drug encapsulation efficiency and loading efficiency.The formulation was optimized using central composite design and response surface methodology.In vitro release study of VCR-PBCA-NPs was performed by dialysis technique.Model fitting was used to determine the kinetics and to discuss the mechanism.Result:The nanoparticles were spherical and uniform with a mean diameter of(98.9±3.05) nm.The drug encapsulation efficiency and loading efficiency were(55.23±0.96)% and(7.87±0.11)%,respectively.In vitro release results showed that 63.66% of VCR was released from VCR-PBCA-NPs in 4 h,and the Weibull model fitted VCR release pattern best.Conclusion:The VCR-PBCA-NPs prepared in this study showed sustained release compared with VCR solution.

关键词(KeyWords): 硫酸长春新碱;聚氰基丙烯酸正丁酯纳米粒;体外释放动力学
vincristine sulphate;poly(butylcyanoacrylate) nanoparticles;in vitro release kinetics

Abstract:

Keywords:

基金项目(Foundation): 上海市教委重点学科项目(J50302);; 上海市优秀学科带头人项目(10XD1403900);; 教育部新世纪优秀人才支持计划项目(NECT08-0898)

作者(Author): 谭蓉;刘颖;冯年平;赵继会;
TAN Rong,LIU Ying,FENG Nianping,ZHAO Jihui(Department of Pharmaceutics,Shanghai University of Traditional Chinese Medicine,Shanghai 201203,China)

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