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葛亮, 钱海, 高昊, 陈跃坚, 朱家壁. N-酰化壳聚糖的合成及其修饰多西他赛脂质体的体外性质研究[J]. 中国药科大学学报, 2009, 40(6): 519-523.
引用本文: 葛亮, 钱海, 高昊, 陈跃坚, 朱家壁. N-酰化壳聚糖的合成及其修饰多西他赛脂质体的体外性质研究[J]. 中国药科大学学报, 2009, 40(6): 519-523.
GE Liang, QIAN Ha, GAO hao, CHENG Yao-jian, ZHU Jiabi. Synthesis of N-acyl chitosan derivatives and investigation of chitosan-modified docetaxel liposomes in vitro[J]. Journal of China Pharmaceutical University, 2009, 40(6): 519-523.
Citation: GE Liang, QIAN Ha, GAO hao, CHENG Yao-jian, ZHU Jiabi. Synthesis of N-acyl chitosan derivatives and investigation of chitosan-modified docetaxel liposomes in vitro[J]. Journal of China Pharmaceutical University, 2009, 40(6): 519-523.

N-酰化壳聚糖的合成及其修饰多西他赛脂质体的体外性质研究

Synthesis of N-acyl chitosan derivatives and investigation of chitosan-modified docetaxel liposomes in vitro

  • 摘要: 目的 : 合成N-酰化壳聚糖并用其修饰多西他赛脂质体以期延缓药物的释放。 方法 : 用合成的长链脂肪酸酰化的壳聚糖修饰脂质体,体外血浆释放实验比较脂质体修饰前后的释放性质。 结果 : 合成了正己酰(C6)、月桂酰(C12)和棕榈酰(C16)3种N-酰化壳聚糖。普通脂质体于24 h内释药70%,而N-酰化壳聚糖修饰的脂质体24 h仅释药39%。 结论 : 用N-酰化壳聚糖修饰脂质体可以减缓释药,具有缓释作用。

     

    Abstract: Aim :Synthesized N-acylated chitosan(NAC) was used to anchor on the surface of plain docetaxel liposomes(PDL) in order to to sustain drug release. Methods ;NAC of low substitution degrees were prepared using hexanoic(C6),lauric(C12),and palmitic(C16) anhydrides.N-palmitoyl chitosan was chosen to anchor the docetaxel liposomes.In vitro release profiles of conventional liposmes and the anchored liposomes was compared. Results :Hexanoic(C6),lauric(C12),and palmitic(C16)-branched chitosans were synthesized.It was found that N-acylated chitosan-anchored DXL liposomes(NDL) increase stabilities of docetaxel liposomes.70% of docetaxel was released from PDL in 24 hours but 39% from NDL. Conclusion :Liposomes anchored by the low substituted N/-acylated chitosan could decrease the drug release.

     

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