Maryam Keshavarzi, Shakeri Shahryar, Kiani Keyhaneh
Department of Biotechnology, Institute of Science and High Technology and Environmental Sciences, Graduate University of Advanced Technology, Kerman, Iran.
IET Nanobiotechnol. 2015 Oct;9(5):294-9. doi: 10.1049/iet-nbt.2014.0040.
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 (IC50) 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.
在本研究中，制备并表征了负载香芹酚的人血清白蛋白（HSA）纳米颗粒。纳米颗粒通过去溶剂化法和乳化/去溶剂化法制备。通过去溶剂化法制备的纳米颗粒的包封率（EE%）和载药量（LC%）分别为48.4%和45.1%。负载香芹酚的纳米颗粒直径为132±42 nm，呈单峰分布。通过乳化/去溶剂化法制备的负载香芹酚的纳米颗粒的EE%和LC%分别为32%和32.3%，尺寸为230±38 nm。在37°C、100 rpm的条件下，于磷酸盐缓冲盐水（pH = 7.4）中监测香芹酚从纳米颗粒中的释放情况，持续10天。通过去溶剂化法制备的纳米颗粒在3小时后约有21.4%的香芹酚释放。在乳化/去溶剂化法中，孵育3小时期间共释放了26.8%的总香芹酚。通过3-[4,5-二甲基噻唑-2-基]-2,5-二苯基四氮唑溴盐（MTT）试验评估负载香芹酚对胃癌细胞系（AGS）的细胞毒性作用。将细胞系分别暴露于游离香芹酚、未负载和负载香芹酚的纳米颗粒中48小时。游离香芹酚、未负载和负载香芹酚的HSA纳米颗粒的半数最大抑制浓度（IC50）分别为30、1070和120 μg/ml。总之，本研究结果表明HSA纳米颗粒在包封香芹酚及抗胃癌活性方面具有应用价值。此外，将香芹酚与化疗药物联合负载到HSA纳米颗粒中可能比单一药物负载的纳米颗粒更有效地治疗癌细胞。
