Satpathy Bibhanwita, Saha Ivy, Halder Jitu, Rajwar Tushar Kanti, Rai Vineet Kumar, Pradhan Deepak, Mishra Ajit, Mahanty Ritu, Dash Priyanka, Das Chandan, Kar Biswakanth, Ghosh Goutam, Rath Goutam
Department of Pharmacology, School of Pharmaceutical Sciences, Siksha 'O' Anusandhan (Deemed to be University), Bhubaneswar, Odisha, India.
Department of Pharmaceutics, School of Pharmaceutical Sciences, Siksha 'O' Anusandhan (Deemed to be University), Bhubaneswar, Odisha, India.
Tissue Cell. 2025 Aug;95:102869. doi: 10.1016/j.tice.2025.102869. Epub 2025 Mar 26.
Nanotechnology-based herbal drug formulations that target multiple aspects of the disease are one of the possible approaches to address the pathological intricacies of Alzheimer's disease (AD). The present study includes the development of rutin embedded with zinc chloride-loaded bovine serum albumin nanoparticles (R-BSA-ZnCl NPs) to counter AD pathogenesis. In this work, the anti-AD potential of selected Phyto active (Rutin) was investigated using a high throughput in silico screening technique. Characterisation and optimization of the formulation were performed by different analytical methods such as FT-IR, zeta sizer and zeta potential, SEM analysis, thermal analysis, x-ray diffraction technique, etc. In vitro, free radical scavenging assay of the formulation was performed using a DPPH assay, and the ROS quantification was done by taking the RAW cell line. The amyloid β disaggregation study was confirmed by the thioflavin T assay, and the blood-brain barrier permeability assay was performed by taking brain endothelial cells. An anticholinesterase study was conducted to ascertain the formulation's potential for treating Alzheimer's disease. The NPs was prepared by ion gelation method and characterized for size (164.8 ± 5.6 nm), zeta potential (-29.6 mV), encapsulation efficiency (91 ± 1.1 %) and loading capacity (10 ± 0.2 %). The FTIR analysis indicated that there was no chemical interaction between the functional groups of rutin and other excipients. DSC, XRD studies suggested unchanged physical state of rutin in the prepared nanoparticle. Surface characterization analysed the irregular morphology of the nanoparticle. The antioxidant activity by DPPH and FRAP assay demonstrated a significant increase in free radical scavenging for R-BSA-ZnCl NPs in compared to rutin (p < 0.01). Anti-aggregation studies indicated that the nanoparticle inhibited the Aβ fibrils by over 70-80 %, as confirmed by Thioflavin T assay. Moreover, the blood brain barrier (BBB) permeability assay indicated permeation of nanoparticle via BBB. Thus, the present study highlighted that bovine serum albumin-zinc chloride nanoparticle may be used as a multifactorial therapeutic platform to address neurodegeneration associated with cognition.
基于纳米技术的草药制剂可针对疾病的多个方面,是解决阿尔茨海默病(AD)病理复杂性的可能途径之一。本研究包括开发负载氯化锌的牛血清白蛋白纳米颗粒包裹的芦丁(R-BSA-ZnCl NPs)以对抗AD发病机制。在这项工作中,使用高通量计算机模拟筛选技术研究了选定的植物活性成分(芦丁)的抗AD潜力。通过傅里叶变换红外光谱(FT-IR)、zeta粒度分析仪和zeta电位仪、扫描电子显微镜(SEM)分析、热分析、X射线衍射技术等不同分析方法对制剂进行表征和优化。在体外,使用二苯基苦味酰基自由基(DPPH)测定法对制剂进行自由基清除测定,并通过RAW细胞系进行活性氧(ROS)定量。通过硫黄素T测定法确认淀粉样β蛋白解聚研究,并通过脑内皮细胞进行血脑屏障通透性测定。进行抗胆碱酯酶研究以确定该制剂治疗阿尔茨海默病的潜力。通过离子凝胶法制备纳米颗粒,并对其尺寸(164.8±5.6 nm)、zeta电位(-29.6 mV)、包封率(91±1.1%)和载药量(10±0.2%)进行表征。FTIR分析表明芦丁的官能团与其他辅料之间没有化学相互作用。差示扫描量热法(DSC)、X射线衍射(XRD)研究表明制备的纳米颗粒中芦丁的物理状态未改变。表面表征分析了纳米颗粒的不规则形态。通过DPPH和铁还原抗氧化能力(FRAP)测定法的抗氧化活性表明,与芦丁相比,R-BSA-ZnCl NPs的自由基清除能力显著增加(p<0.01)。抗聚集研究表明,如硫黄素T测定法所证实,纳米颗粒抑制Aβ纤维形成的能力超过70-80%。此外,血脑屏障(BBB)通透性测定表明纳米颗粒可透过BBB。因此,本研究强调牛血清白蛋白-氯化锌纳米颗粒可作为一种多因素治疗平台来解决与认知相关的神经退行性变。