5-氟尿苷棕榈酸酯脂质体的制备及其细胞毒性研究

吴镁春;朱莉;赵怡;潘黎军;王驰

中国药学杂志 ›› 2009, Vol. 44 ›› Issue (07) : 520-523.

中国药学杂志 ›› 2009, Vol. 44 ›› Issue (07) : 520-523.
论著

5-氟尿苷棕榈酸酯脂质体的制备及其细胞毒性研究

  • 吴镁春;朱莉;赵怡;潘黎军;王驰
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Study on Preparation of 5′-Palmitoyl-5-Fluorouridine Liposome and Its Cell Toxicity

  • WU Mei-chun,ZHU Li,ZHAO Yi,PAN Li-jun,WANG Chi
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文章历史 +

摘要

目的制备前药5-氟尿苷棕榈酸酯(5-FURP)脂质体,并进行体外细胞毒性实验。方法通过正交实验设计筛选5-FURP脂质体的最佳处方,采用逆向蒸发法制备5-FURP脂质体,测定其包封率及理化性质;以人乳腺癌细胞系MCF-7、人鼻咽癌细胞系CNE-1、人喉癌细胞系HEP-2为模型细胞,考察5-FUR前药脂质体的细胞毒性。结果制备的脂质体平均包封率为94.35%,将脂质体分别在4和25℃下密闭放置1个月,以包封率、脂质体中磷脂含量变化为指标考察其稳定性。结果显示,脂质体于4℃贮存时,上述指标无显著变化,脂质体比较稳定;细胞实验表明,5-FURP经脂质体包裹后,细胞毒性较游离药物增高,对人乳腺癌细胞系MCF-7、人鼻咽癌细胞系CNE-1、人喉癌细胞系HEP-2的IC50分别是游离药物的5.0,3.4,2.6倍。结论实验室制备的5-FURP经脂质体包裹后能增强细胞摄取,具有提高药物疗效的效果。

Abstract

OBJECTIVE To prepare prodrug 5′-palmitoyl-5- fluorouridine (5-FURP) liposome and to evalutate its toxicity in vitro. METHODS The orthogonal design was used to screen the optimal formation and preparation process.The 5-FURP liposome was prepared by the reverse-phase evaporation vesicles(REV),and its encapsulation efficiency and physicochemical property was determined. The cytotoxicity of 5-FURP liposome was investigated by human breast cancer of MCF-7cell line,human nasopharyngeal carcinoma of CNE-1 cell line,human nasopharyngeal carcinoma of HEP-2 cell line. RESULTS encapsulation efficiency of the 5-FURP liposome was 94.35%. The stability of 5-FURP liposome was valuated with the entrapment efficiency and the change of EPC value in 4,25 ℃ for 1 month. The results showed that the 5-FURP liposome stored in 4 ℃ would keep stable. The results of cell toxicity in vitro showed that the liposomes encapsulated with 5-FURP inhibited human breast cancer of MCF-7 cell line,human nasopharyngeal carcinoma of CNE-1 cell line,human nasopharyngeal carcinoma of HEP-2 cell line was higher than that of the free drug.The IC50 of 5-FURP liposome was higher(5.0,3.4,2.6 times) for the MCF-7,CNE-1,HEP-2 than for free 5-FUR. CONCLUSION 5-FURP was encapsulated in liposomes can inhance corpuscular uptake and promote therapeutic effect of medicine.

关键词

5-氟尿苷棕榈酸酯 / 脂质体 / 逆向蒸发法 / 细胞毒作用

Key words

5-FUR prodrug / liposome / reverse-phase evaporation vesicles / cytotoxic effect

引用本文

导出引用
吴镁春;朱莉;赵怡;潘黎军;王驰. 5-氟尿苷棕榈酸酯脂质体的制备及其细胞毒性研究[J]. 中国药学杂志, 2009, 44(07): 520-523
WU Mei-chun;ZHU Li;ZHO Yi;PN Li-jun;WNG Chi. Study on Preparation of 5′-Palmitoyl-5-Fluorouridine Liposome and Its Cell Toxicity [J]. Chinese Pharmaceutical Journal, 2009, 44(07): 520-523

参考文献

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