C-Fe@CN-CN对人肝癌细胞增殖的抑制作用

The inhibitive effect of the carboplatin-Fe@C nanocage-loaded chitosan nanoparticles on the proliferation of human hepatoma cell line HepG2

目的制备卡铂碳包铁纳米笼壳聚糖微球(C-Fe@CN-CN),观察其对人肝癌细胞体外增殖的抑制作用。方法采用反相微乳法制备C-Fe@CN-CN,测定其表征,观察其体外释药行为。采用MTT法检测C-Fe@CN-CN对人肝癌细胞体外增殖的抑制效应;计算IC50,绘制生长曲线。结果C-Fe@CN-CN球形圆整,平均粒径(2 0 7±2 1)nm,载药量为(1 1.4 0±1.3 1)%。C-Fe@CN-CN的体外释药行为包括快速相和平稳相两阶段,可持续5 d。C-Fe@CN-CN对人肝癌细胞增殖有明显抑制作用,并呈剂量和时间依赖性,作用2 4 h时抑制效应低于原药,作用4 8 h和7 2 h时抑制效应等同于原药。C-Fe@CN-CN的2 4,4 8,7 2 h IC50分别为1 3 5,1 8.8 4,6.0 9μg/mL。空白微球对肝癌细胞增殖无影响。结论C-Fe@CN-CN具有长循环和肿瘤组织滞留潜能,磁靶向性强,可缓释药物。体外能有效地抑制肝癌细胞增殖,空白微球表现出良好的生物相容性。

Objective To prepare the carboplatin-Fe @ C nanocage-loaded chitosan nanoparticles （C-Fe @ CN-CN ） , and observe the inhibitive effect on the proliferation of human hepatoma cell line HepG2 in vitro. Methods The C-Fe @ CN-CN were prepared by the reverse microemulsion method and the character and drug release in vitro were observed. The inhibitive effect on the proliferation of the HepG2 cell was measured by MTT colorimetry, IC50 was calculated and the growth curve of HepG2 cell was drawn. Results C-Fe@ CN-CN were in good spherical shape. The average size was 207nm ± 21nm with narrow distribution. The drug content was 11 . 40 ± 1 . 31% . After a fast release during the first day, a more gradual drug release was sustained for another 4 days. C-Fe@ CN-CN could apparently inhibit the proliferation of HepG2 cell inthe dose-dependent and time-dependent manner. The inhibitive effect of C-Fe@ CN-CN at 24 hours was lower than that of original carboplatin, and was equal to original carboplatin at 48 hours and 72 hours. IC50 of C- Fe @ CN- CN at 24h, 48h and 72h was 135μg/ml, 18. 84μg/ml and 6.09μg/ml respectively. Bland nanoparticles had no cytotoxicity on HepG2 cell. Conclusions C-Fe @ CN-CN possess strong magnetic responsivity, drug controlled releasing performance and the potential abilities of long circulation and permeation in tumor tissue. C- Fe @ CN- CN can effectively inhibit the proliferation of HepG2 cell, and the blank nanoparticles express favourable biocompatibility in vitro.