Formulation and characterization of polymeric nanoparticle of Rivastigmine for effective management of Alzheimer’s disease

IF 3 3区 医学 Q2 PHARMACOLOGY & PHARMACY
Faisal Imam , Sayantan Mukhopadhyay , Preeti Kothiyal , Samiyah Alshehri , Khalid Saad Alharbi , Muhammad Afzal , Muzaffar Iqbal , Mohammad Rashid Khan , Md. Khalid Anwer , Abdulrazaq Ahmed Hattab Alanazi , Ali Ghanem Alqahtani , Mohammed Abdullah Alhamamah
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Abstract

Memory loss or dementia is a progressive disorder, and one of its common forms is Alzheimer’s disease (AD), effecting mostly middle aged and older adults. In the present study, we developed Rivastigmine (RIV) nanoparticles using poly(lactic-co-glycolic acid) (RIV-loaded PLGA NPs) and polyvinyl alcohol (PVA). The prepared RIV-PLGA nanoparticles was evaluated for the management of Alzheimer's disease (AD). The nanoparticles were prepared by the slightly modified nano-precipitation technique. The developed formulations were evaluated for particle size, zeta potential (ZP), polydispersibility index (PDI) and surface morphology and drug content. The experimental result revealed that prepared RIV-loaded PLGA NPs (F1) was optimized having particle size (61.2 ± 4.6 nm), PDI (0.292), ZP (−11.2 ± 1.2). SEM study confirms the prepared nanoparticles depicted non-aggregated as well smooth surface particles without any fracture. This formulation (F1) was further assessed for in vivo studies on animal model. A pharmacological screening on an animal model of Alzheimer's disease revealed that RIV-loaded PLGA NPs formulations treat CNS disorders like Alzheimer's effectively. In addition to that, an in-vivo brain cholinesterase estimation study found that, animals treated with optimized formulation significantly (p < 0.01) reduced brain cholinesterase activity when compared to scopolamine-treated animals. According to the above results, it can be concluded that RIV-loaded PLGA NPs are ideal carriers for delivering the drug at a specific target site in the brain, thus may treat Alzheimer's disease efficiently and improve patient compliance.

用于有效治疗阿尔茨海默病的利伐斯的明聚合物纳米粒子的制备和表征
记忆力减退或痴呆症是一种渐进性疾病,其常见形式之一是阿尔茨海默病(AD),主要影响中老年人。在本研究中,我们利用聚乳酸-共聚乙醇酸(RIV-loaded PLGA NPs)和聚乙烯醇(PVA)开发了利伐斯的明(RIV)纳米颗粒。所制备的 RIV-PLGA 纳米粒子被评估用于治疗阿尔茨海默病(AD)。纳米颗粒是通过略微改良的纳米沉淀技术制备的。对所开发的制剂进行了粒度、ZP、多分散指数(PDI)、表面形态和药物含量的评估。实验结果表明,制备的负载 RIV 的 PLGA NPs(F1)的粒度(61.2 ± 4.6 nm)、PDI(0.292)和 ZP(-11.2 ± 1.2)均达到最佳。扫描电子显微镜研究证实,制备的纳米颗粒无聚集,表面光滑,无任何断裂。该制剂(F1)在动物模型上进行了进一步的体内研究评估。在阿尔茨海默病动物模型上进行的药理学筛选显示,负载 RIV 的 PLGA NPs 制剂能有效治疗阿尔茨海默病等中枢神经系统疾病。此外,一项体内脑胆碱酯酶估计研究发现,与东莨菪碱处理的动物相比,使用优化制剂处理的动物的脑胆碱酯酶活性显著降低(p < 0.01)。根据上述结果,可以得出结论:负载 RIV 的 PLGA NPs 是一种理想的载体,可将药物输送到大脑中的特定靶点,从而有效治疗阿尔茨海默病,并提高患者的依从性。
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来源期刊
Saudi Pharmaceutical Journal
Saudi Pharmaceutical Journal PHARMACOLOGY & PHARMACY-
CiteScore
6.10
自引率
2.40%
发文量
194
审稿时长
67 days
期刊介绍: The Saudi Pharmaceutical Journal (SPJ) is the official journal of the Saudi Pharmaceutical Society (SPS) publishing high quality clinically oriented submissions which encompass the various disciplines of pharmaceutical sciences and related subjects. SPJ publishes 8 issues per year by the Saudi Pharmaceutical Society, with the cooperation of the College of Pharmacy, King Saud University.
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