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 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 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.

中文翻译：

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用于有效治疗阿尔茨海默病的卡巴拉汀聚合物纳米颗粒的配方和表征

记忆丧失或痴呆是一种进行性疾病，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，我们使用聚乳酸-乙醇酸共聚物（RIV 负载的 PLGA NP）和聚乙烯醇（PVA）开发了卡巴拉汀（RIV）纳米颗粒。评估制备的 RIV-PLGA 纳米颗粒对阿尔茨海默病 (AD) 的治疗作用。纳米颗粒是通过稍微改进的纳米沉淀技术制备的。对开发的制剂进行了粒径、zeta 电位 (ZP)、多分散性指数 (PDI) 以及表面形态和药物含量的评估。实验结果表明，制备的RIV负载PLGA NPs（F1）经过优化，粒径为（61.2±4.6 nm），PDI（0.292），ZP（-11.2±1.2）。 SEM 研究证实制备的纳米粒子呈现非聚集且表面光滑的粒子，没有任何断裂。该制剂 (F1) 进一步评估用于动物模型研究。对阿尔茨海默病动物模型的药理学筛选表明，负载 RIV 的 PLGA NP 制剂可以有效治疗阿尔茨海默病等中枢神经系统疾病。除此之外，一项脑胆碱酯酶估计研究发现，与东莨菪碱治疗的动物相比，用优化配方治疗的动物显着（p < 0.01）降低了脑胆碱酯酶活性。根据上述结果可以得出结论，负载RIV的PLGA NPs是将药物递送至大脑特定靶位点的理想载体，因此可以有效治疗阿尔茨海默病并提高患者的依从性。