摘要
目的:观察卡铂碳铁纳米球(C-C&Fe-N)经肝动脉注射,结合体外磁场引导下,在移植性肝癌大鼠体内的靶向分布情况。方法:移植性肝癌大鼠40只为A组,健康大鼠40只为B组。肝动脉插管,注入C-C&Fe-N,以肿瘤(A组)或肝左叶(B组)为靶区,施加磁场30min(5000Gs)。分别于相应时间点,采集肿瘤或靶区肝、非靶区肝、肾、脾、肺和心组织标本,测定卡铂浓度,显微镜观察C-C&Fe-N在各脏器沉积情况。结果:A组靶区肿瘤组织卡铂峰浓度(Cmax)65.21μg/g,为B组靶区肝组织38.47μg/g的1.7倍,为A组非靶区肝组织14.36μg/g的4.5倍。48h时A组靶区肿瘤组织卡铂浓度7.27μg/g,为B组靶区肝组织3.11μg/g的2.3倍,为A组非靶区肝组织0.32μg/g的22.7倍。各时间点,A组肿瘤组织药物浓度均成倍高于B组靶区肝组织和两组非靶区肝组织,差异有统计学意义,P<0.05。A组靶区肿瘤组织卡铂AUC是906(μg.h)/g,为B组靶区肝组织421.34(μg.h)/g的2.2倍,为A组非靶区肝组织86.47(μg.h)/g的10.5倍。结论:C-C&Fe-N在体内显示出良好的磁靶向性和药物缓释性,并且对肿瘤组织具有更强的靶向性,能成倍提高肿瘤组织中的药物浓度,延长维持时间。
OBJECTIVE：To observe the targeted biodistribution of Carboplatin-C ＆Fe Nanocage-loaded Chitosan Nanopartieles （C-C ＆ Fe-N） injected by hepatic artery under magnetic field in rats with transplanted liver cancer. METHODS： Forty rats with transplanted liver cancer were composed of Group A. Forty normal rats were composed of Group B. Abdominal exposure was carried out through a midline incision, and a cannula was inserted into the hepatic artery and fixed. C-C ＆ Fe-N was injected into hepatic artery. The tumors （Group A） and the left liver lobes （Group B） were under 5 000 Gs magnetic field as targeted region for 30 rain. At different injection time rats in each group were sacrificed respectively. The drug levels in tumor, targeted liver, non-targeted liver, kidney, spleen, lung and heart were measured by flameless atomic absorption spectrophotometry. The tissues were stained by HE to observe the aggregation of C-C ＆ Fe-N. RESULTS： The Cmax of eaboplatin of targeted tumor in Group A （65.21 μg/g） was 1. 7 times higher than that of targeted liver in Group B （38.47 /μg/g）, and 4.5 times higher than that of non-targeted liver in Group A（14.36 μg/g）. The concentration of carboplatin of targeted tumor at 48 h in Group A （7.27 μg/g） was 2.3 times higher than that of targeted liver in Group B（3.11 μg/g）, and 22. 7 times higher than that of non-targeted liver in Group A（0.32 μg/g）. The drug concentrations of tumor at every time were significantly higher than those of targeted liver in Group B and those of nontargeted-liver in both groups （P〈0. 05）. The area under curve of caboplatin of targeted tumor in Group A （906（ μg · h）/g] was 2.2 times higher than that of targeted liver in Group B （421.34 （μg · h）/g], and 10.5 times higher than that of non-targeted liver in Group A （86.47 （μg·h）/g]. CONCLUSIONS： C C ＆ Fe N shows remarkable magnetic target and delayed release in vivo, which are specially stronger to tumor than targeted liver. The level of drug in tumor is multiplied, and the active time is prolonged.
出处
《中华肿瘤防治杂志》
CAS
2009年第23期1828-1831,共4页
Chinese Journal of Cancer Prevention and Treatment
基金
深圳市科技计划重点项目(200601016)
广东省自然科学基金(04006966)
广东省名医工程研究项目
深圳市科技计划项目(2002-K3-121)
关键词
磁靶向
纳米球
卡铂
肝肿瘤
大鼠
magnetic target
nanoparticles
carboplatin
liver neoplasms
rats
