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Preparation and in vitro investigation of antigastric cancer activities of carvacrol-loaded human serum albumin nanoparticles

机译:香芹酚负载人血清白蛋白纳米粒子的制备及其体外抗癌活性研究。

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In this study, carvacrol-loaded human serum albumin (HSA) nanoparticles were developed and characterised. Nanoparticles were prepared by desolvation and emulsion/desolvation methods. Encapsulation efficiency (EE%) and loading capacity (LC%) of nanoparticles prepared by desolvation method were 48.4 and 45.1%, respectively. Carvacrol-loaded nanoparticles had 132 ± 42 nm in diameter with monomodal distribution. Carvacrol-loaded nanoparticles which is prepared by emulsion/desolvation method had EE% and LC% of 32 and 32.3%, respectively, and 230 ± 38 nm in size. The release of carvacrol from nanoparticles was monitored in phosphate-buffered saline (pH = 7.4), 100 rpm at 37°C for 10 days. About 21.4% of carvacrol was released after 3 h from nanoparticles that were prepared by desolvation method. In emulsion/desolvation method, 26.8% of total carvacrol was released during 3 h of incubation. Cytotoxicity effect of loaded carvacrol was assessed by 3-[4, 5 dimethylthiazol-2-yl]-2,5-diphenyltetrazolium bromide (MTT) test on gastric cancer cells line (AGS). Cell line was exposed to the free carvacrol, unloaded and carvacrol-loaded nanoparticles for 48 h. The half maximal inhibitory concentration (IC) for free carvacrol, unloaded and carvacrol-loaded HSA nanoparticles were 30, 1070 and 120 μg/ml, respectively. In conclusion, the results of this study showed applications of HSA nanoparticles for entrapment of carvacrol and antigastric cancer activity. Moreover, loading of carvacrol in combination with chemotherapy agents into the HSA nanoparticles may treat cancer cells better than single drug loaded nanoparticles.
机译:在这项研究中,载有香芹酚的人血清白蛋白(HSA)纳米颗粒已得到开发和表征。纳米颗粒通过去溶剂化和乳液/去溶剂化方法制备。用去溶剂化法制备的纳米颗粒的包封率(EE%)和负载量(LC%)分别为48.4%和45.1%。载有香芹酚的纳米颗粒的直径为132±42 nm,具有单峰分布。通过乳液/去溶剂化方法制备的负载香芹酚的纳米粒子的EE%和LC%分别为32和32.3%,尺寸为230±38 nm。在磷酸盐缓冲盐水(pH = 7.4)中,于37°C,100 rpm的条件下监测香芹酚从纳米颗粒的释放,持续10天。 3小时后,通过去溶剂化方法制备的纳米颗粒释放了约21.4%的香芹酚。在乳液/去溶剂化方法中,孵育3小时释放了总香芹酚的26.8%。通过3- [4,5二甲基噻唑-2-基] -2,5-二苯基溴化四溴化铵(MTT)对胃癌细胞系(AGS)的测试评估了香芹酚的细胞毒性作用。将细胞系暴露于游离香芹酚,未装载和装载香芹酚的纳米颗粒48小时。游离香芹酚,未装载和装载香芹酚的HSA纳米颗粒的半数最大抑制浓度(IC)分别为30、1070和120μg/ ml。总之,这项研究的结果表明,HSA纳米颗粒可用于香芹酚的捕获和抗胃癌活性。而且,将香芹酚与化学治疗剂组合装载到HSA纳米颗粒中可能比装载单一药物的纳米颗粒更好地治疗癌细胞。

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