Department of Pharmacology, Poona College of Pharmacy, Bharati Vidyapeeth, (Deemed to be University), Pune, Maharashtra, 411038, India.
Cent Nerv Syst Agents Med Chem. 2024;24(3):281-293. doi: 10.2174/0118715249279534240214111155.
Alzheimer's disease (AD) is a form of brain degeneration that gradually impairs a person's memory and cognitive skills, eventually making it harder for them to perform everyday activities. Its pathophysiology has been attributed to the deposition of amyloid β (Aβ), neurofibrillary tangles (NFT), and α-synuclein (A-s) in some cases. Presently, 4 drugs have been approved for the treatment. They are Donepezil, Rivastigmine, Galantamine and Memantine. The first three are acetylcholinesterase inhibitors, while memantine is an NMDA receptor antagonist. Even though these medications are successful in treating mild to moderate Alzheimer's disease, they have not been able to reverse the disease or even slow its progression completely. Hence, natural products are gaining more popularity due to the advantage of the multitarget intervention effect. The most investigated spice, 's bioactive component, curcumin, has demonstrated anti-amyloid, anti-NFT, and anti-Lewy body properties and substantial antiinflammatory, antioxidant, and antiapoptotic properties. However, its proven neuroprotective activity is hampered by many factors, such as poor water solubility and bioavailability. Therefore, many novel formulations have been designed to improve its bioavailability with methods such as 1) Micellar Solubilization, 2) Cyclodextrin Complexation, 3) Crystal Modification, and 4) Particle Size Reduction, etc. The current chapter aims to summarize various novel formulations of curcumin and their effectiveness in treating AD.
阿尔茨海默病(AD)是一种脑部退化的疾病,它会逐渐损害人的记忆力和认知能力,最终使他们难以进行日常活动。其病理生理学归因于某些情况下淀粉样β(Aβ)、神经原纤维缠结(NFT)和α-突触核蛋白(A-s)的沉积。目前,已有 4 种药物被批准用于治疗。它们是多奈哌齐、利斯的明、加兰他敏和美金刚。前三种是乙酰胆碱酯酶抑制剂,而美金刚是 NMDA 受体拮抗剂。尽管这些药物在治疗轻度至中度阿尔茨海默病方面取得了成功,但它们未能完全逆转疾病,甚至无法减缓其进展。因此,由于具有多靶点干预作用的优势,天然产物越来越受到关注。研究最多的香料“姜黄素”的生物活性成分,已显示出抗淀粉样、抗 NFT 和抗 Lewy 体的特性,以及显著的抗炎、抗氧化和抗凋亡特性。然而,其已被证实的神经保护活性受到许多因素的限制,如较差的水溶性和生物利用度。因此,已经设计了许多新型制剂来通过以下方法提高其生物利用度:1)胶束增溶,2)环糊精包合,3)晶体修饰和 4)粒径减小等。本章旨在总结姜黄素的各种新型制剂及其在治疗 AD 中的有效性。