School of Dentistry, Yasuj University of Medical Sciences, Yasuj, Iran.
Medicinal Plants Research Center, Yasuj University of Medical Sciences, Yasuj, Iran.
IET Nanobiotechnol. 2023 Oct 26;2023:1745877. doi: 10.1049/2023/1745877. eCollection 2023.
Curcumin is one of the natural anticancer drugs but its efficiency is limited by low stability, insufficient bioavailability, poor solubility, and poor permeability. (Bilhar) is a herb with precious pharmaceutical properties. This study aimed to develop a nanoliposome-based curcumin and Bilhar extract codelivery system. The nanocompounds were synthesized using the lipid thin-film hydration method and characterized by transmission electron microscopy, and dynamic light scattering techniques, and their cytotoxicity and apoptotic effect on the primary oral cancer cell line were evaluated via 2,5-diphenyl-2H-tetrazolium bromide assay and flow cytometry. Moreover, the expression of the epidermal growth factor receptor (EGFR) gene in the treated cells was assessed using the real-time polymerase chain reaction technique. Based on the results, nanoliposomes had a size of 91 ± 10 nm with a polydispersity index of 0.13. Free curcumin, the extract, and the curcumin-extract combination showed dose-dependent toxicity against cancer cells; yet, the extract (IC: 86 g/ml) and curcumin-extract (IC: 65 g/ml) activities were much more than curcumin (IC: 121 g/ml). Also, the curcumin and extract loaded on liposomes showed a dose and time-dependent cytotoxicity. After loading the curcumin-extract compound on nanoliposomes, their IC decreased from 180 g/ml (within 24 hr) to 43 g/ml (within 72 hr), indicating their sustainable release and activity. Likewise, this compound induced the highest apoptosis percentage (95%) in cancerous cells and inhibited the expression of the EGFR gene in the cells by 81% ± 3%. These findings demonstrated the effectiveness of the Bilhar extract against oral cancer cells. Also, in combination with curcumin, it showed an additive activity that considerably improved after loading on nanoliposomes.
姜黄素是一种天然抗癌药物，但由于其稳定性低、生物利用度低、溶解度差和渗透性差，其效率受到限制。（Bilhar）是一种具有珍贵药用特性的草药。本研究旨在开发基于纳米脂质体的姜黄素和 Bilhar 提取物共递送系统。纳米复合物是通过脂质薄膜水化法合成的，并通过透射电子显微镜和动态光散射技术进行了表征，通过 2,5-二苯基-2H-四唑溴盐测定法和流式细胞术评估了它们对原发性口腔癌细胞系的细胞毒性和凋亡作用。此外，还使用实时聚合酶链反应技术评估了处理细胞中表皮生长因子受体（EGFR）基因的表达。基于结果，纳米脂质体的粒径为 91±10nm，多分散指数为 0.13。游离姜黄素、提取物和姜黄素-提取物组合对癌细胞表现出剂量依赖性毒性；然而，提取物（IC：86g/ml）和姜黄素-提取物（IC：65g/ml）的活性远高于姜黄素（IC：121g/ml）。此外，负载在脂质体上的姜黄素和提取物表现出剂量和时间依赖性细胞毒性。将姜黄素-提取物化合物负载在纳米脂质体上后，其 IC 从 180g/ml（24 小时内）降低至 43g/ml（72 小时内），表明其具有可持续释放和活性。同样，该化合物在癌细胞中诱导了最高的凋亡百分比（95%），并抑制了细胞中 EGFR 基因的表达，抑制率为 81%±3%。这些发现表明 Bilhar 提取物对口腔癌细胞有效。此外，与姜黄素联合使用时，其表现出协同作用，负载在纳米脂质体上后协同作用显著增强。
