Yadha Harika, Kolure Rajini, Thakur Sneha, Mandava Kiranmai, Boddu Suhasini
Incozen Pharma, Hyderabad, India.
Department of Pharmacology, St. Pauls College of Pharmacy, Turkayamjal, Telangana, 501510, India.
Heliyon. 2024 Sep 24;10(20):e38391. doi: 10.1016/j.heliyon.2024.e38391. eCollection 2024 Oct 30.
Rutin is a flavonoid glycoside abundant in many plants exhibiting pharmacological activities like antioxidant, anticancer, anti-inflammatory and antimicrobial activities. Plant biomarkers suffer low bioavailability and solubility that lack clinical effectiveness. The smart nanoparticles conversion addresses this limitation with optimal particle size and targeted drug delivery. The present study involves QbD approach for formulation of Rutin silver nanoparticles and evaluation of antioxidant, anticancer and anticlastogenic potential. QbD experimentation involved particle size and drug release as dependent variables over the silver nitrate concentration, methanol and sonication time as independent variables devising 15 formulations (F1 -F15). F12 formulation was found to be optimized with 126.3 nm average size, stable and dispersible characterized by UV, FTIR, SEM and DLS studies. The calibration curve of Rutin was plotted at 352 nm with linearity (LOD = 0.061 μg/ml and LOQ = 0.187 μg/ml). The drug release studies by USP dissolution apparatus I (Basket type) proved the sustained release characteristics with 97.3 % drug release when compared to the Rutin. The pharmacological screening for potential antioxidant and anticancer activity on G361 and MCF 7 cell line of F12 formulation have shown promising results and also enhanced solubility in water compared to Rutin. Anticalstogenic potential as a function of induced micronuclei frequency was evaluated as a characteristic feature in bone marrow cells obtained from mice. Results indicate pre-treatment with the F12 reduced frequency of micronuclei in mouse bone marrow cells caused by Cyclophosphamide (CP) significantly. The protective effect of F12 in suppression was demonstrated at both dosages of 100 and 200 mg/kg. Thus the findings suggest the novel Rutin silver nanoparticles as lead drug serving as antioxidant, anticancer and anticlastogenic agent.
芦丁是一种黄酮苷,在许多植物中含量丰富,具有抗氧化、抗癌、抗炎和抗菌等药理活性。植物生物标志物的生物利用度和溶解度较低,缺乏临床疗效。智能纳米颗粒转化通过优化粒径和靶向药物递送解决了这一局限性。本研究采用质量源于设计(QbD)方法制备芦丁银纳米颗粒,并评估其抗氧化、抗癌和抗致突变潜力。QbD实验将粒径和药物释放作为因变量,硝酸银浓度、甲醇和超声处理时间作为自变量,设计了15种配方(F1 - F15)。通过紫外、傅里叶变换红外光谱、扫描电子显微镜和动态光散射研究发现,F12配方优化良好,平均粒径为126.3nm,稳定且可分散。芦丁的校准曲线在352nm处绘制,具有线性关系(检测限=0.061μg/ml,定量限=0.187μg/ml)。美国药典溶出度仪I(篮式)进行的药物释放研究证明,与芦丁相比,该配方具有缓释特性,药物释放率为97.3%。对F12配方在G361和MCF 7细胞系上的潜在抗氧化和抗癌活性进行的药理筛选显示出有前景的结果,并且与芦丁相比,其在水中的溶解度也有所提高。作为诱导微核频率函数的抗致突变潜力被评估为从小鼠获得的骨髓细胞中的一个特征。结果表明,用F12预处理可显著降低环磷酰胺(CP)引起的小鼠骨髓细胞微核频率。在100和200mg/kg两种剂量下均证明了F12在抑制方面的保护作用。因此,研究结果表明新型芦丁银纳米颗粒作为先导药物,可作为抗氧化、抗癌和抗致突变剂。