Department of Pharmaceutics, National Institute of Pharmaceutical Education and Research-Raebareli, Lucknow, India.
Department of Pharmaceutics, School of Pharmaceutical Education and Research, Jamia Hamdard, New Delhi, India.
J Biomater Sci Polym Ed. 2022 Oct;33(15):1901-1923. doi: 10.1080/09205063.2022.2088527. Epub 2022 Jun 23.
Acetylcholine imbalance in the human brain causes dementia-related symptoms of Alzheimer's disease. Acetylcholinesterase (AChE) inhibitors prevent the lysis of acetylcholine in the brain and prevent dementia. Therefore, the present study aims to investigate the and AChE potential of rosemary oil and then formulate it into nanoemulsion as an adjuvant with co-administration of Donepezil (Dz) with a thought for futuristic target for Alzheimer's diseases via the intranasal route. The aim for preparing this formulation was to add the AChE inhibition effect of the rosemary oil to the effect that acts as an additive effect along with Dz. The docking score of rosemary oil components on human cholinesterase 1GQR protein was found to be >-5 kcal/mol. AChE activity of rosemary oil confirms the prominent IC50 of oil at 0.001 µL/min. Nanoemulsion was prepared by low energy emulsification technique using Tween 80 as surfactant and ethanol or diethylene glycol monoethyl ether as cosurfactant. Droplet size, polydisperity index, and zeta potential of stable nanoemulsion was ∼16 nm, 0.1, and -6.05 mV for stable batch. High-resolution transmission electron microscopy microscopic studies depicted the spherical shape of the droplet. Micro rheology investigation of nanoemulsion clearly attributes to gel-sol-gel behaviour of formulated nanoemulsion. Thermal evaluation of nanoemulsion depicts the phase transition behaviour of ethanol-based nanoemulsion at 60 °C. nasal ciliotoxicity and permeation studies of formulation establish the safety of ethanol-based rosemary oil-loaded nanoemulsion and permeation mechanism of Dz from the nanoemulsion. permeation studies showed more drug penetration from the nanoemulsion as compared to the plain drug. The prepared nanoemulsion was found to be stable for 3 months at 4, 25, and 45 °C of storage. This low energy preparation method can be advantageous for the preparation of scalable nanoemulsion and can be a futuristic therapeutic for Alzheimer's disease.
人类大脑中的乙酰胆碱失衡会导致与阿尔茨海默病相关的痴呆症状。乙酰胆碱酯酶 (AChE) 抑制剂可防止大脑中乙酰胆碱的裂解，从而预防痴呆。因此，本研究旨在研究迷迭香油的 和 AChE 潜力，然后将其制成纳米乳液，作为与多奈哌齐 (Dz) 联合给药的佐剂，通过鼻腔途径为未来的阿尔茨海默病治疗提供一种新的思路。 该制剂的目的是将迷迭香油的 AChE 抑制作用添加到作为 Dz 添加剂的作用中。发现迷迭香油成分对人胆碱酯酶 1GQR 蛋白的对接评分> -5 kcal/mol。迷迭香油的 AChE 活性证实油的突出 IC50 为 0.001 μL/min。纳米乳液通过低能量乳化技术制备，使用吐温 80 作为表面活性剂，乙醇或二乙二醇单乙基醚作为助表面活性剂。稳定纳米乳液的粒径、多分散指数和 zeta 电位分别为约 16nm、0.1 和-6.05mV。高分辨率透射电子显微镜研究显示了液滴的球形形状。纳米乳液的微观流变学研究清楚地表明了配方纳米乳液的凝胶-溶胶-凝胶行为。纳米乳液的热评估描述了基于乙醇的纳米乳液在 60°C 时的相转变行为。 制剂的鼻纤毛毒性和渗透研究建立了基于乙醇的迷迭香油载纳米乳液的安全性以及 Dz 从纳米乳液中的渗透机制。 渗透研究表明，与普通药物相比，纳米乳液中的药物渗透更多。所制备的纳米乳液在 4、25 和 45°C 的储存条件下可稳定 3 个月。这种低能量制备方法有利于制备可扩展的纳米乳液，可为阿尔茨海默病提供未来的治疗方法。
