摘要
目的:制备转铁蛋白(TF)修饰紫杉醇(PTX)脂质体(TF-PTX-LP),并研究其抑瘤作用。方法:采用薄膜分散法制备TF-PTX-LP并观察其形态;定性和定量考察肝癌Hep G2细胞对TF-LP和LP的摄取情况;检测PTX、PTX-LP和TF-PTX-LP分别处理Hep G2细胞24、48、72 h后细胞的增殖抑制率;以Hep G2细胞制备肿瘤球,考察生理盐水、PTX、PTX-LP和TF-PTX-LP分别处理0、1、2、4、5、6、7 d对肿瘤球体积的影响;复制Hep G2荷瘤裸鼠模型,考察生理盐水、PTX、PTX-LP和TF-PTX-LP(以PTX计8.5mg/kg)对荷瘤裸鼠移植瘤的抑制作用。结果:TF-PTX-LP均呈均一球形,粒径在100~120 nm。TF-LP处理后细胞的荧光强度强于LP(P〈0.01)。与PTX、PTX-LP比较,TF-PTX-LP处理后细胞的增殖抑制率更高(P〈0.01)。与生理盐水、PTX、PTX-LP比较,TF-PTX-LP处理后肿瘤球体积更小,对荷瘤裸鼠的抑瘤率更高,且6、7 d后抑瘤率差异有统计学意义(P〈0.01)。增殖抑制率和肿瘤球体积变化呈时间依赖性。结论:成功制得具有良好抑瘤作用的TF-PTX-LP。
OBJECTIVE:To prepare transferrin modified paclitaxel-loaded liposome(TF-PTX-LP),and to study the tumor inhibition effect. METHODS:TF-PTX-LP was prepared by thin-film method,and morphology of TF-PTX-LP was observed. Qualitative and quantitative investigation were used to value the uptake efficiency of TF-LP and LP by Hep G2 cells. The proliferation inhibition rate of Hep G2 cells was investigated after treated with PTX,PTX-LP and TF-PTX-LP for 24,48 and 72 h. Tumor spheres were prepared by using Hep G2 cells. Effects of normal saline,PTX,PTX-LP and TF-PTX-LP on the volume of tumor spheres were investigated after 0,1,2,4,5,6 and 7 d treatment. Hep G2 tumor-bearing nude mice model was induced. Inhibitory effects of normal saline,PTX,PTX-LP and TF-PTX-LP(8.5 mg/kg by PTX)on transplantable tumor of tumor-bearing nude mice were investigated. RESULTS:TF-PTX-LP showed uniform spherical shape,with particle size of 100-120 nm. The fluorescence intensity of Hep G2 cells treated with TF-LP was stronger than that treated with LP(P〈0.01). Compared with PTX and PTX-LP,TF-PTX-LP showed higher proliferation inhibition rate(P〈0.01). Compared with normal saline,PTX and PTX-LP,tumor spheres were smaller in volume after treated with TF-PTX-LP,and inhibition rate of tumor was higher in tumor-bearing nude mice;there were statistical significance after treated for 6,7 d(P〈0.01). The proliferation inhibition rate and tumor spheres volume changed in time-dependent manner. CONCLUSIONS:TF-PTX-LP which owns good tumor inhibition effect is prepared successfully.
出处
《中国药房》
CAS
北大核心
2016年第1期44-47,共4页
China Pharmacy
基金
河南省医学科技攻关计划项目(No.2011020091)
关键词
转铁蛋白
紫杉醇
脂质体
肝癌Hep
G2细胞
裸鼠
增殖抑制率
抑瘤率
Transferrin
Paclitaxel
Liposome
Lung cancer Hep G2 cell
Nude mice
Proliferation inhibition rate
Tumor inhibition rate