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  

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

作　　者：郭立文[1] 汪森明[1] 胡喜钢[1] 曹漫明[1] 张积仁[1] 

机构地区：[1]南方医科大学珠江医院肿瘤中心,广东广州510282

出　　处：《基础医学与临床》2009年第9期979-983,共5页Basic and Clinical Medicine

基　　金：广东省医学科研基金立项课题(A2007680)

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322 nm,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。Objective To prepare a new type of chitosans nanoparticles （PEG/CS-EPI NPs）, which contains 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 shape were illustrated respectively by laser scattering and transmission electron microscopy. The proliferation of nasopharyngeal carcinoma cells was detected by MTT assay ; The mouse model of implantation murine sarcoma cells（S-180） was applied to evaluate the anticancer effectiveness of PEG/CS-EPI NPs and CS-EPI NPs in vivo. Results The PEG modified CS NPs were discrete and uniform spheres with average diameter of 322. 1 nm. The rate 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. Conclusion Stealth chitosan nanoparticles as compared with ordinary chitosan nanoparticles seems to be a potential candidate of chemotherapy drug carriers.

关 键 词：壳聚糖 表柔比星 隐形纳米粒 

分 类 号：R94[医药卫生—药剂学] R730.5[医药卫生—药学]