摘要
目的:研究去甲基斑蝥素N-乳糖酰壳聚糖纳米粒(NCTD-GC-NPs)的吸收机制和小鼠抑瘤作用。方法:以表观透过系数为指标,考察NCTD-GC-NPs(80μg·mL-1)及其分别与环孢素A(50μmol·L-1)、去氧胆酸钠(100mmol·L-1)、叠氮化钠(25mmol·L-1)、氧化苯胂(25mmol·L-1)联用后对结肠癌Caco-2细胞转运的影响;将接种肝癌细胞H22后的小鼠随机分为空白组、对照组(NCTD原料药2mg·kg-1)和NCTD-GC-NPs低、中、高剂量组(0.5、2、4mg·kg-1),每组10只,每日灌胃给药1次,连续给药8d,考察各组小鼠体重和抑瘤率。结果:环孢素A、去氧胆酸钠和叠氮化钠均能明显促进NCTD-GC-NPs在Caco-2细胞的转运(P<0.05或P<0.01),氧化苯胂对转运无明显影响;各组小鼠体重无明显变化;与对照组比较,NCTD-GC-NPs中、高剂量组的抑瘤率明显增强(P<0.05或P<0.01)。结论:NCTD-GC-NPs主要通过主动转运穿过小肠上皮细胞,能明显抑制肝癌肿瘤细胞H22的生长。
OBJECTIVE： To study absorption mechanism and anti-tumor effect in mice of Norcantharidin loaded N-galactosylated chitosan nanoparticles （NCTD-GC-NPs）. METHODS： Using apparent coefficient as index, effects of NCTD-GC-NPs （80 μg.mL-1） combined with cyclosporin A （CyA, 50 μmol.L -1）, sodium deoxycholate （SDCh, 100 mmol·L-1）, NaN3 （25 mmol-L-1） or oxo- phenylarsine （25 mmol. L--1） on Caco-2 cell transport were investigated; after the vaccination of H22, mice were randomly divided into blank group, control group （NCTD raw material 2 mg. kg-1）, NCTD-GC-NPs high-dose, medium-dose and low-dose groups （0.5, 2, 4 mg.kg-1） with each group of 10 mice. Those groups were given medicine via i.g. once a day for consecutive 8 days. The body weight and anti-tumor rate were investigated during this experiment. RESULTS： CyA, SDCh and NaN3 could improved the transportation of NCTD-GC-NPs in Caco-2 cells significantly （P〈0.05 or P〈0.01）, while oxophenylarsine showed no obvious effect. The body weight of mice had no significant change. Compared with control group, the anti-tumor rate of NCTD-GC-NPs of medium-dose and high-dose groups were enhanced significantly （P〈 0.05 or P〈 0.01）. CONCLUSION： NCTD-GC-NPs may pass through intestinal epithelial cells primarily by active transport, which could inhibit the growth of hepatic carcinoma cell H22.
作者
贝永燕
管敏
周奕
许静玉
薛成文
胡展红
张学农
BEI Yong-yan;GUAN Min;ZHOU Yi;XU Jing-yu;XUE Cheng-wen;HU Zhan-hong;ZHANG Xue-nong(College of Pharmacy,Soochow University,Jiangsu Suzhou 215123,China;Suzhou Liyuan Medical Technology Co.,Ltd.,Jiangsu Suzhou 215002,China)
出处
《中国药房》
CAS
CSCD
2012年第1期26-28,共3页
China Pharmacy
