School of Pharmaceutical Sciences, Lovely Professional University, Phagwara, Punjab, India.
School of Pharmacy, International Medical University, Bukit Jalil, Kuala Lumpur, Malaysia.
Curr Top Med Chem. 2024;24(19):1683-1698. doi: 10.2174/0115680266296001240327090111.
Alzheimer's disease (AD) is the most prevalent form of neurodegenerative disorder (ND), affecting more than 44 million individuals globally as of 2023. It is characterized by cognitive dysfunction and an inability to perform daily activities. The progression of AD is associated with the accumulation of amyloid beta (Aβ), the formation of neurofibrillary tangles (NFT), increased oxidative stress, neuroinflammation, mitochondrial dysfunction, and endoplasmic reticulum stress. Presently, various phytomedicines and their bioactive compounds have been identified for their neuroprotective effects in reducing oxidative stress, alleviating neuroinflammation, and mitigating the accumulation of Aβ and acetylcholinesterase enzymes in the hippocampus and cerebral cortex regions of the brain. However, despite demonstrating promising anti-Alzheimer's effects, the clinical utilization of phytoconstituents remains limited in scope. The key factor contributing to this limitation is the challenges inherent in traditional drug delivery systems, which impede their effectiveness and efficiency. These difficulties encompass insufficient drug targeting, restricted drug solubility and stability, brief duration of action, and a lack of control over drug release. Consequently, these constraints result in diminished bioavailability and insufficient permeability across the blood-brain barrier (BBB). In response to these challenges, novel drug delivery systems (NDDS) founded on nanoformulations have emerged as a hopeful strategy to augment the bioavailability and BBB permeability of bioactive compounds with poor solubility. Among these systems, nanoemulsion (NE) have been extensively investigated for their potential in targeting AD. NE offers several advantages, such as ease of preparation, high drug loading, and high stability. Due to their nanosize droplets, NE also improves gut and BBB permeability leading to enhanced permeability of the drug in systemic circulation and the brain. Various studies have reported the testing of NE-based phytoconstituents and their bioactives in different animal species, including transgenic, Wistar, and Sprague-Dawley (SD) rats, as well as mice. However, transgenic mice are commonly employed in AD research to analyze the effects of Aβ. In this review, various aspects such as the neuroprotective role of various phytoconstituents, the challenges associated with conventional drug delivery, and the need for NDDS, particularly NE, are discussed. Various studies involving phytoconstituent-based NE for the treatment of AD are also discussed.
阿尔茨海默病(AD)是最常见的神经退行性疾病(ND),截至 2023 年,全球有超过 4400 万人受其影响。它的特征是认知功能障碍和无法进行日常活动。AD 的进展与淀粉样β(Aβ)的积累、神经原纤维缠结(NFT)的形成、氧化应激增加、神经炎症、线粒体功能障碍和内质网应激有关。目前,已经确定了各种植物药及其生物活性化合物具有神经保护作用,可以减少氧化应激、缓解神经炎症,并减轻海马体和大脑皮层区域 Aβ和乙酰胆碱酯酶的积累。然而,尽管这些植物药表现出有希望的抗 AD 作用,但它们在临床中的应用仍然有限。造成这种限制的关键因素是传统药物输送系统固有的挑战,这些挑战阻碍了它们的有效性和效率。这些困难包括药物靶向不足、药物溶解度和稳定性受限、作用持续时间短以及对药物释放缺乏控制。因此,这些限制导致生物利用度降低和血脑屏障(BBB)通透性不足。为了应对这些挑战,基于纳米制剂的新型药物输送系统(NDDS)已经成为提高生物利用度和提高生物活性化合物的 BBB 通透性的有希望的策略,这些化合物的溶解度较差。在这些系统中,纳米乳剂(NE)已被广泛研究用于治疗 AD。NE 具有易于制备、高药物载量和高稳定性等优点。由于其纳米尺寸的液滴,NE 还提高了肠道和 BBB 的通透性,从而增强了药物在全身循环和大脑中的通透性。各种研究已经报告了基于 NE 的植物药及其生物活性物质在不同动物物种中的测试,包括转基因、Wistar 和 Sprague-Dawley(SD)大鼠以及小鼠。然而,转基因小鼠通常用于 AD 研究中以分析 Aβ的影响。在本综述中,讨论了各种方面,例如各种植物药成分的神经保护作用、与传统药物输送相关的挑战以及对 NDDS 的需求,特别是 NE。还讨论了涉及基于植物药的 NE 治疗 AD 的各种研究。