摘要
目的探讨聚乙二醇(PEG)修饰的5-氟尿嘧啶磁性白蛋白微球(PEG-5-Fu-MAMS)和5-氟尿嘧啶磁性白蛋白微球(5-Fu-MAMS)对大肠癌组织的被动靶向性。方法 20只人大肠癌裸鼠随机数字表法分为PEG-5-Fu-MAMS组、5-Fu-MAMS组,每组10只,分别将2种不同的制剂(按8 mg/kg5-Fu)经尾静脉给药,在磁场下30 min后,经眼眶采血,处死大鼠,用高效液相色谱法测定肿瘤组织、血清和肾脏组织中5-Fu的水平。采用SPSS 13.0软件对资料进行统计分析,两组不同组织中5-Fu水平以x±s记录,显著性检验采用t检验。结果注射PEG-5-Fu-MAMS组大肠癌组织中的5-Fu水平为(51.21±2.12)μg/m L,明显高于5-Fu-MAMS组的(33.07±8.21)μg/m L(t=78.69,P<0.05);而在注射PEG-5-Fu-MAMS组的血清中5-Fu的水平为(1.69±0.53)μg/m L,则明显低于5-Fu-MAMS组的(6.78±0.23)μg/m L(t=18.76,P<0.05);在肾脏中PEG-5-Fu-MAMS组药5-Fu水平为(21.1±2.3)μg/m L,明显低于5-Fu-MAMS组的(38.2±4.9)μg/m L(t=39.23,P<0.05)。结论PEG-5-Fu-MAMS比5-Fu-MAMS的亲大肠癌作用强,PEG-5-Fu-MAMS有望成为一种新的靶向治疗大肠癌的药物。
Objective To explore passive targeting property of Polyethylene glycol (PEG)modification of 5-fluorouracil magnetic albumin microspheres (PEG 5-Fu-MAMS)and 5-fluorouracil magnetic albumin microspheres (Fu-MAMS)for colorectal cancer tissus.Methods Twenty mice were randomly divided into Group 5-Fu-MAMS(n =1 0)and Group PEG-5-Fu-MAMS(n =1 0).They were injected through the vena caudalis at the dose of 8 mg/kg of free drug respectively.After a magnetic field for 30 minutes,the mice were killed,the orbital cavity blood was sampled immediately.The concentrations of 5-fluorouracil in colorectal carcinoma and renal tissue and serum were determined by the high performance liquid chromatography (HPLC).The difference of the level of 5-Fu was compared with t -test.Results The 5-Fu concentration of colorectal carcinoma in PEG-5-Fu-MS (51 .21 ±2.1 2)μg/mL group was significantly higher than that of 5-Fu-MS group[(33.07 ±8.21 )μg/mL,t =78.69,P <0.05].But the 5-Fu concentration of serum in PEG-5-Fu-MAMS [(1 .69 ±0.53)μg/mL]was significantly lower than that of 5-Fu-MAMS group[(6.78 ±0.23)μg/mL,t =1 8.76,P<0.05].The 5-Fu concentration of kidney tissue in PEG-5-Fu-MAMS group (21 .1 ±2.3)μg/mL was significantly lower than that of the 5-Fu-MAMS group [(38.2 ±4.9)μg/mL,t =39.23,P <0.05)].Conclusions The study suggests that the affinity with colorectal cancer of PEG-5-FU-MASA to colorectal cancer is stronger than that of the 5-FU-MAMS .PEG-5-FU-MAMS are expected to become a new targeted therapy of colorectal cancer.
出处
《中华诊断学电子杂志》
2014年第3期198-201,共4页
Chinese Journal of Diagnostics(Electronic Edition)
基金
山东省医药卫生科技发展计划项目(2013WSB33012)
