兰州大学机构库 >学院待认领
5-FU载药纳米微粒的制备、表征及体外实验
Alternative TitlePreparation、Characterization and experiment of 5-fluorouracil-loaded nanoparticles in vitro study
冯芳
Thesis Advisor吴静
2009-05-22
Degree Grantor兰州大学
Place of Conferral兰州
Degree Name硕士
Keyword载药纳米微粒 5—氟尿嘧啶 聚乳酸 O-羧甲基壳聚糖
Abstract具有生物相容性和生物可降解性的高分子材料为载体的抗肿瘤药物是目前药物释放领域研究的热点之一。纳米载药微粒其活性成分(药物或生物活性材料等)可包裹于粒子内部或吸附于粒子表面,该系统可增溶疏水性药物,保护药物活性,增加药物稳定性,改变药物在体内的分布,增加药物在靶器官中的累积,提高治疗指数,减少毒副作用。本研究采用复乳法制备5-氟尿嘧啶-聚乳酸-羧甲基壳聚糖(5-FU-PLA-O-CMC)载药纳米微粒,并对其表面形貌、粒径分布、体外释放等表征及对食管癌细胞的体外杀伤效应等微粒性能进行应用评估。 通过电子显微镜观察纳米载药微粒的外形结构,用紫外分光光度计测微粒的载药量和包封率,并测定体外释放量,且与纯5-Fu对比,观察其对人食管癌细胞株的体外杀伤效应。 5-FU-PLA-O-CMC载药纳米微粒呈规则球形,平均粒径100-200nm,载药量为9.87% 包封率为32.5%;体外释放实验表明微粒具有缓释特性,在模拟体液中,10天的累积释药达92.90%;5-Fu的杀伤效应在1-7d时呈时间依赖关系,7d后进入平台期;5-Fu-PLA-O-CMC载药纳米微粒则在1-11 d均呈时间依赖关系,5-Fu-PLA-O-CMC载药纳米微粒和5-FU均呈剂量依赖杀伤效应。 制备的载药纳米微粒可改变5-FU在体内的药代动力学行为,具有缓释作用,可制备为静脉用药,延长药物在体内的循环时间,发挥更好的抗肿瘤效应。5-FU-PLA-O-CMC载药纳米微粒可抑制Eca109细胞增殖,且5-FU- PLA -O-CMC载药纳米微粒的缓释功能可维持较长时间的抗癌作用。
Other AbstractAs a carrier, the polymers with biocompatibility and biodegradability as a type of anticancer drug, is one of the hot spots in the field of drug delivery. The active ingredient of nanoparticles (drug or biologically active materials, etc.) can be coated inside of particles or adsorbed on the surface of particles. This system can increase the solubility, protect activity, reinforce the stability and change the distribution of drug in the body, increase accumulation in target organs, improve the therapeutic index and diminish side effect. This study was to observe prepared nanoparticles’ morphology, diameter, and efficacy of esophageal cancer cells in vitro study. The morphology of nanoparticles was observed under scanning electron microscope,its drug loading (DL)and embedding ratio (ER)were assessed by ultraviolet spectroscopy, the pure 5-Fu as contrast, observe efficacy of nanoparticles on esophageal cancer cells in vitro study. The nanoparticles were uniformly spherical with average diameter of 100-200nm, DL of 9.87%, and ER of 32.5%. The experiment of release shows that the nanoparticles have a sustained release character. In the analog body fluid,the cumulative drug release rate of ten days is 92.9%. The cytotoxic effect of 5-Fu showed a time-dependent manner from the first day to 7th day, and then reached a plateau. But the cytotoxic effect of 5-Fu-PLA-O-CMC-NP sustained this manner until the 11th day. Using the PLA as a carrier of 5-FU, the act of pharmacokinetics in human body can be changed, which has an effect of releasing. Thus, it can be used to produce the drug for veins,which would prolong the circulation time of the drug and have a better antitumor effect. Efficacy of the nanoparticles on esophageal cancer cells showed time-dependent manner and dosage-dependent manner .the 5-Fu-PLA-NP can prolong the phase of the inhibitory effect of 5-Fu against Eca109 cells. The nanoparticles enhance the biological activity of 5-Fu.
URL查看原文
Language中文
Document Type学位论文
Identifierhttps://ir.lzu.edu.cn/handle/262010/224263
Collection学院待认领
Affiliation临床医学院
Recommended Citation
GB/T 7714
冯芳. 5-FU载药纳米微粒的制备、表征及体外实验[D]. 兰州. 兰州大学,2009.
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