Fuster Marta G, Carissimi Guzmán, Montalbán Mercedes G, Víllora Gloria
Department of Chemical Engineering, Faculty of Chemistry, University of Murcia (UMU), Campus de Espinardo, 30100 Murcia, Spain.
Nanomaterials (Basel). 2020 Apr 10;10(4):718. doi: 10.3390/nano10040718.
Naringenin (NAR), a flavonoid present in a variety of fruits, vegetables and herbs, exhibits a wide range of pharmacological effects, including anticancer activity. Nevertheless, its application in cancer therapy is limited due to its low bioavailability at the tumour site because of its poor solubility in water and slow dissolution rate. To improve the therapeutic efficacy of NAR, emergent research is looking into using nanocarriers. Silk fibroin (SF), from the silkworm, is a biocompatible and biodegradable polymer with excellent mechanical properties and an amphiphilic chemistry that make it a promising candidate as a controlled release drug system. The aim of this work is to synthesize naringenin-loaded silk fibroin nanoparticles (NAR-SFNs) by dissolving the SF in the ionic liquid 1-ethyl-3-methylimidazolium acetate, using high-power ultrasounds and rapid desolvation in methanol followed by the adsorption of NAR. The NAR-SFNs were characterized by dynamic light scattering, Fourier transform infrared spectroscopy and thermogravimetric analysis. The drug loading content and encapsulation efficiency were calculated. The drug release profile best fitted a first order equation. The cytotoxicity effects of free NAR, bare silk fibroin nanoparticles (SFNs) and NAR-SFNs were assessed on HeLa and EA.hy926 cells via 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) assay. The results demonstrated the higher in vitro anticancer potential of synthesized NAR-SFNs than that of free NAR in HeLa cancer cells.
柚皮素（NAR）是一种存在于多种水果、蔬菜和草药中的黄酮类化合物，具有广泛的药理作用，包括抗癌活性。然而，由于其在水中溶解度差、溶解速度慢，导致其在肿瘤部位的生物利用度低，限制了其在癌症治疗中的应用。为了提高NAR的治疗效果，新兴研究正在探索使用纳米载体。家蚕的丝素蛋白（SF）是一种生物相容性和可生物降解的聚合物，具有优异的机械性能和两亲化学性质，使其成为一种有前途的控释药物系统候选物。这项工作的目的是通过将SF溶解在离子液体1-乙基-3-甲基咪唑醋酸盐中，利用高功率超声和在甲醇中快速去溶剂化，随后吸附NAR，来合成负载柚皮素的丝素蛋白纳米颗粒（NAR-SFNs）。通过动态光散射、傅里叶变换红外光谱和热重分析对NAR-SFNs进行了表征。计算了载药量和包封率。药物释放曲线最符合一级方程。通过3-(4,5-二甲基噻唑-2-基)-2,5-二苯基四氮唑溴盐（MTT）法评估了游离NAR、裸丝素蛋白纳米颗粒（SFNs）和NAR-SFNs对HeLa和EA.hy926细胞的细胞毒性作用。结果表明，合成的NAR-SFNs在HeLa癌细胞中的体外抗癌潜力高于游离NAR。
