基础医学与临床 ›› 2009, Vol. 29 ›› Issue (9): 979-983.

• 技术与方法 • 上一篇    下一篇

表柔比星壳聚糖隐形纳米粒的制备及其抗肿瘤活性的检测

郭立文 汪森明 胡喜钢 曹漫明 张积仁   

  1. 南方医科大学附属珠江医院肿瘤中心 南方医科大学附属珠江医院肿瘤中心
  • 收稿日期:2008-09-11 修回日期:2009-02-28 出版日期:2009-09-20 发布日期:2009-09-20
  • 通讯作者: 汪森明

Study for preparation and anticancer activity of the stealth epirubicin chitosan nanoparticles

Li-wen GUO, Sen-ming WANG, Xi-gang HU, Man-ming CAO, Ji-ren ZHANG   

  1. Department of Oncology, Zhujiang Hospital, Southern Medical University Department of Oncology, Zhujiang Hospital, Southern Medical University
  • Received:2008-09-11 Revised:2009-02-28 Online:2009-09-20 Published:2009-09-20
  • Contact: Sen-ming WANG,

摘要: 目的 制备包裹抗癌药物表柔比星(EPI)的"隐形"壳聚糖纳米粒,并检测其抗肿瘤活性。方法 应用阴离子凝聚法制备负载EPI的PEG化壳聚糖纳米粒(PEG/CS-EPI NPs)和普通壳聚糖纳米粒(CS-EPI NPs),通过透射电镜和动态光散射方法表征粒子的形貌和尺寸分布,用MTT法测定鼻咽癌细胞的增殖抑制率;并通过尾静脉注射给药法对荷小鼠肉瘤细胞S-180小鼠进行体内抑瘤试验。结果 PEG/CS-EPI NPs呈圆形或椭圆形,平均粒径322nm,载药量为13%,包封率74%,抑制细胞增殖具有浓度和时间依赖性,与普通壳聚糖纳米粒相比,隐形纳米粒的体内抗肿瘤作用更明显。结论 隐形壳聚糖纳米粒较普通壳聚糖纳米粒更适合用于制备化疗药物载体。

关键词: 壳聚糖, 表柔比星, 隐形纳米粒

Abstract: Objective This study is to prepare a new type of chitosan nanoparticles (PEG/CS-EPI NPs), which contain epirubicin and modified by PEG, Furthermore, to investigate the anticancer activity of the NPs in vitro and in vivo. Methods The ionic gelation technique was employed to prepare the PEG/CS-EPI NPs and CS-EPI NPs. The particle size and morphology were determined respectively by laser scattering and transmission electron microscopy. The proliferation of nasopharyngeal carcinoma cells were detected by MTT assay in vitro; The mouse model of implantation murine sarcoma cells(S-180) were applied to evaluate the anticancer effectiveness of PEG/CS-EPI NPs and CS-EPI NPs in vivo. Results The PEG modified CS NPs prepared were discrete and uniform spheres with an average diameter of 322.1nm and the rates of drug loading and encapsulation is 13% and 74%, respectively. The results of the anticancer tests showed a sustained cytotoxicity of loading drug NPs on nasopharyngeal carcinoma cells in vitro and the stealth nanoparticles was more powerful than ordinary nanoparticles on the inhibitory potency in vivo. Conclution Stealth chitosan nanoparticles as compared with ordinary chitosan nanoparticles could be more suitable for the preparation of chemotherapy drug carriers.

Key words: Chitosan, epirubicin, stealth nanoparticles