Al-Samydai Ali, Al Qaraleh Moath, Al Azzam Khaldun M, Mayyas Amal, Nsairat Hamdi, Abu Hajleh Maha N, Al-Halaseh Lidia K, Al-Karablieh Nehaya, Akour Amal, Alshaik Fatima, Alshaer Walhan
Pharmacological and Diagnostic Research Centre (PDRC), Faculty of Pharmacy, Al-Ahliyya Amman University, Amman, 19328, Jordan.
Faculty of Health Sciences, Department of Pharmacy, American University of Madaba, 11821, Madaba, Jordan.
Heliyon. 2023 Jun 18;9(6):e17267. doi: 10.1016/j.heliyon.2023.e17267. eCollection 2023 Jun.
Cancer is considered one of the top global causes of death. Natural products have been used in oncology medicine either in crude form or by utilizing isolated secondary metabolites. Biologically active phytomolecules such as gallic acid and quercetin have confirmed antioxidant, anti-bacterial, and neoplastic properties. There is an agreement that microorganisms could mediate oncogenesis or alter the immune system. This research project aims to develop a novel formulation of co-loaded gallic acid and quercetin into nanoliposomes and investigate the efficacy of the free and combined agents against multiple cancerous cell lines and bacterial strains. Thin-film hydration technique was adopted to synthesize the nanocarriers. Particle characteristics were measured using a Zetasizer. The morphology of nanoliposomes was examined by scanning electron microscopy, Encapsulation efficiency and drug loading were evaluated using High-Performance Liquid Chromatography. Cytotoxicity was determined against Breast Cancer Cells MCF-7, Human Carcinoma Cells HT-29, and A549 Lung Cancer Cells. The antibacterial activities were evaluated against , , , , and . Therapeutic formulas were categorized into groups: free gallic acid, free quercetin, free-mix, and their nano-counterparts. Findings revealed that drug loading capacity was 0.204 for the mix formula compared to 0.092 and 0.68 for free gallic acid and quercetin, respectively. Regarding the Zeta potential, the mix formula showed more amphiphilic charge than the free quercetin and free gallic acid formulas (-values 0.003 and 0.002 receptively). On the contrary, no significant difference in polydispersity indices was reported. Lung cancerous cells were the most affected by the treatments. The best estimated IC50 values were observed in breast and lung cancer lines for the nano-gallic acid and co-loaded particles. The nano-quercetin formula exhibited the least cytotoxicity with an IC50 value of ≥200 μg/mL in both breast (MCF-7) and colorectal adenocarcinoma cell lines (HT-29) with no activity against the lung. A remarkable improvement in the efficacy of quercetin was measured after mixing it with gallic acid against the breast and lungs. The tested therapeutic agents exhibited antimicrobial activity against gram-positive bacteria. Nano-liposomes can either enhance or reduce the cytotoxicity activity of active compounds depending on the physical and chemical properties of drug-loaded and type of cancer cells.
癌症被认为是全球主要死因之一。天然产物已以粗提物形式或通过利用分离出的次生代谢产物应用于肿瘤医学。生物活性植物分子如没食子酸和槲皮素已被证实具有抗氧化、抗菌和抗肿瘤特性。人们一致认为微生物可介导肿瘤发生或改变免疫系统。本研究项目旨在开发一种将没食子酸和槲皮素共负载于纳米脂质体中的新型制剂,并研究游离药物及其组合制剂对多种癌细胞系和细菌菌株的疗效。采用薄膜水化技术合成纳米载体。使用Zetasizer测量颗粒特性。通过扫描电子显微镜检查纳米脂质体的形态,使用高效液相色谱评估包封率和载药量。测定对乳腺癌细胞MCF-7、人癌细胞HT-29和A549肺癌细胞的细胞毒性。评估对[此处原文缺失具体细菌名称]、[此处原文缺失具体细菌名称]、[此处原文缺失具体细菌名称]、[此处原文缺失具体细菌名称]和[此处原文缺失具体细菌名称]的抗菌活性。治疗配方分为几组:游离没食子酸、游离槲皮素、游离混合配方及其纳米对应物。研究结果显示,混合配方的载药量为0.204,而游离没食子酸和游离槲皮素的载药量分别为0.092和0.68。关于Zeta电位,混合配方比游离槲皮素和游离没食子酸配方表现出更多的两亲性电荷(Zeta电位值分别为0.003和0.002)。相反,多分散指数未报告显著差异。肺癌细胞受治疗影响最大。在乳腺癌和肺癌细胞系中,纳米没食子酸和共负载颗粒的IC50值估计最佳。纳米槲皮素配方在乳腺癌(MCF-7)和结肠腺癌细胞系(HT-29)中的细胞毒性最小,IC50值≥200μg/mL,对肺癌细胞无活性。将槲皮素与没食子酸混合后,对乳腺癌和肺癌的疗效有显著提高。所测试的治疗剂对革兰氏阳性菌具有抗菌活性。纳米脂质体可根据载药的物理化学性质和癌细胞类型增强或降低活性化合物的细胞毒性活性。