目的 制备姜黄素纳米混悬剂以提高姜黄素的水溶性和生物利用度。方法 分别以聚乙烯吡咯烷酮、十二烷基磺酸钠和泊洛沙姆为稳定剂,采用溶剂沉淀法结合高剪切匀质法制备了姜黄素纳米混悬剂。以平均粒径、多分散系数及Zeta电位为指标进行处方筛选。结果 聚乙烯吡咯烷酮稳定的姜黄素纳米混悬剂在原料药与稳定剂的质量比为1∶2、剪切转速为25 000 rmin-1时为最佳处方。所得纳米混悬剂中姜黄素为100 nm以下的非晶态球形串珠体颗粒。体外释放实验结果表明,姜黄素纳米混悬剂的溶出度较原料药有显著提高,同时累积释放浓度的拟合结果表明,该纳米混悬剂中姜黄素的释放符合零级方程模型。结论 本实验制备的姜黄素纳米混悬剂均匀稳定,有效提高了姜黄素的水溶性和体外溶出度,并显示一定的缓控释特性,为解决姜黄素应用局限提供了实验基础。
Abstract
OBJECTIVE To improve the dissolution and bioavailability of curcumin. METHODS Polyvinylpyrrolidone, sodium dodecyl sulfonate, and poloxamer were used as stabilizing agent. Curcumin nanosuspension was prepared by solvent precipitation method combined with high shear homogenization. The prescription was optimized with average particle size, polydispersity index and Zeta potential as indexes. RESULTS The prescription using polyvinylpyrrolidone was the most stable when the mass ratio of curcumin to PVP was 1∶2 and the cutting speed was 250 000 rmin-1. The nanoparticles in curcumin nanosuspension were amorphous and spherical with diameter of about 100 nm. The in vitro release experimental showed that the dissolution of curcumin nanosuspension was significantly improved compared with crude curcumin. Characteristic curve fitting showed that the release of curcumin in the nanosuspension could be fitted to zero-order equation. CONCLUSION The prepared curcumin nanosuspension has good sustained release property.
关键词
姜黄素 /
纳米混悬剂 /
稳定剂 /
溶出度 /
聚乙烯吡咯烷酮
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Key words
curcumin /
nanosuspension /
stabilizer /
in vitro dissolution /
polyvinylpyrrolidone
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中图分类号：
R944
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参考文献
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脚注
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基金
国家自然科学基金资助项目(51303006);安徽省教育厅自然科学项目(KJ2012ZD09);安徽省科技厅面上项目(1408085MH196)
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