载5-FU纳米微粒抗肿瘤的实验研究  

Experimental study of 5-fluorouracil loaded polylactic acid nanoparticles control-releasing preparation on tumor

作　　者：黄开红[1] 刘建化[1] 王凌云[1] 朱兆华[1] 陈其奎[1] 闵军[2] 陈汝福[2] 

机构地区：[1]中山大学附属第二医院消化内科,广东广州510120 [2]中山大学附属第二医院普通外科,广东广州510120

出　　处：《中国病理生理杂志》2007年第9期1706-1709,共4页Chinese Journal of Pathophysiology

基　　金：广州市科技攻关资助项目(No.2003Z3-E03851);国家自然科学基金资助项目(No.30670951);广东省自然科学基金资助项目(No.06021322);广东省科技攻关项目(No.2005B31211002)

摘　　要：目的:研究抗癌药5-FU纳米控释静脉注射微粒的制备工艺及其体内外抗肿瘤作用。方法:以聚乳酸(PLA)作为基质材料,采用超声乳化-溶剂挥发法制备PLA包载5-FU的纳米微粒(5-FU-NPs)。扫描电镜观察5-FU-NPs形态,通过激光光散射实验测定5-FU-NPs的粒径分布。利用高效液相色谱(HPLC)测定5-FU-NPs的载药率,以MTT方法检测5-FU-NPs体外杀伤癌细胞效应,用5-FU-NPs不同剂量、给药频度条件下体内抑瘤实验。结果:电镜观察5-FU-NPs为表面光滑的球形微粒,粒径分布平均值是191.1nm,呈正态分布。5-FU-NPs载药率为15.2%。体外MTT实验提示5-FU-NPs作用明显优于5-FU(P<0.05)。体内抑瘤实验表明:5-FU-NPs间隔给药疗效优于未包载药物每日给药的疗效,量-效关系明显,且毒性减低。结论:5-FU-NPs可以作为5-FU的有效载体,实现药物控制释放并减低毒性,发挥药物更佳的抗肿瘤作用。AIM： To investigate the preparation techniques and anti -tumor effects both in vitro and in vivo of a novel nanoparticles control - releasing preparation of 5 - fluorouracil （5 - FU） by intravenous injection. METHODS ： With polylactic acid （PLA） as marix materials, we adopted ultrasound emulsification method to prepare PLA enveloped 5 - FU nanoparticles （5 - FU - NPs）. Scanning electricity microscopy was used to observe the morphology of 5 - FU - NPs and laser optical scattering experiment was conducted to determine its diameter distribution. The drug - carrying capacity （ratio） of the nanoparticles was determined by means of high -power liquid chromatography（HPLC） and MTT test was used to observe cytotoxicity in vitro, The anti - tumor effects were determined at different dosages, frequencies of taking drugs in vivo. RESULTS： Scanning electron microscopy showed that the 5 - FU - NPs were globular particles with smooth surface in an average particle diameter of 191.9 nm with a normal distribution, and the drug - carrying capacity of 5 - FU - NPs was 15.2%. 5 - FU - NPs had the same anti - cancer effect as unenveloped drug in vitro and showed typical dose - effect relationship. Compared to naked 5 - FU, 5 - FU - NPs presented significant difference （ P 〈 0, 05 ） in anti - cancer effect. CONCLUSION： Nanoparticles may serve as effective carrier for controlled release of 5 - FU, which lead to reasonable administration of 5 -FU with less toxicity.

关 键 词：纳米微粒 氟尿嘧啶 肿瘤 缓释作用 

分 类 号：R733[医药卫生—肿瘤]