肝靶向去甲斑蝥素修饰物的合成及其纳米粒的制备

胡展红;章良;周奕;张学农

中国药学杂志 ›› 2009, Vol. 44 ›› Issue (09) : 679-684.

中国药学杂志 ›› 2009, Vol. 44 ›› Issue (09) : 679-684.
论著

肝靶向去甲斑蝥素修饰物的合成及其纳米粒的制备

  • 胡展红;章良;周奕;张学农
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Synthesis of Hepatocyte-Targeting Norcantharidin Prodrug and Preparation of Its Nanoparticles

  • HU Zhan-hong,ZHANG Liang,ZHOU Yi,ZHANG Xue-nong
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摘要

目的合成乳糖化-去甲斑蝥素作为主动肝靶向性修饰物,并将其制成纳米粒。方法利用乙二胺为连接臂合成乳糖化-去甲斑蝥素修饰物,并考察其相关理化性质;采用离子诱导法制备乳糖化-去甲斑蝥素壳聚糖纳米粒,以粒径分布、包封率、载药量为综合指标,正交设计优化载药纳米粒的制备工艺,并考察其体外释放特性。结果乳糖化-去甲斑蝥素是一种具有良好水溶性的多羟基化合物,其合成产率为68.35%;经优化工艺制备的乳糖化-去甲斑蝥素的纳米粒的平均粒径(149.46±1.79)nm,包封率(80.29±0.56)%,载药量(9.58±0.09)%,其体外释药遵循Higuchi方程。结论乳糖化-去甲斑蝥素合成简单,产率高,其纳米粒体外释放具有良好的缓释特性。

Abstract

OBJECTIVE To synthesize lactosyl-norcantharidin(Lac-NCTD) as active liver-tageting modified drug and prepare its nanoparticles.METHODS Lac-NCTD was synthesized with ethanediamine as truss arm,and then its properties were studied.Chitosan nanoparticles(CS-NP) were achieved by ionic cross-linkage process with lactosyl-norcantharidin as a model drug.Orthogonal experiment design was applied to optimize the formulation and preparation procedure with particle distribution,entrapment rate and drug-loading rate as integrated indexes.The in vitro release was investigated.RESULTS Lac-NCTD was a kind of polyhydroxy compound and the yield was 68.35%.CS-NP were spherical,average particle size was(149.46±1.79)nm,entrapment rate was(80.29±0.56) %,drug-loading rate was(9.58±0.09)%,and in vitro release followed Higuchi equation.CONCLUSION The synthesis procedure of Lac-NCTD was simple and the yield was high.Sustained release of CS-NP was identified.

关键词

乳糖化-去甲斑蝥素 / 主动肝靶向 / 壳聚糖 / 纳米粒

Key words

lactosyl-norcantharidin / active liver-targeting / chitosan / nanoparticle

引用本文

导出引用
胡展红;章良;周奕;张学农. 肝靶向去甲斑蝥素修饰物的合成及其纳米粒的制备[J]. 中国药学杂志, 2009, 44(09): 679-684
HU Zhn-hong;ZHNG Ling;ZHOU Yi;ZHNG Xue-nong. Synthesis of Hepatocyte-Targeting Norcantharidin Prodrug and Preparation of Its Nanoparticles [J]. Chinese Pharmaceutical Journal, 2009, 44(09): 679-684

参考文献

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基金

国家科技支撑计划课题资助(2006BAI09B00);国家科技部科技型中小企业技术创新基金(07C26223201333);江苏省“六大人才高峰”资助项目;江苏省卫生厅招标项目(H200630)

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