Otaegui Léa, Urgin Théo, Zaiter Taghrid, Zussy Charleine, Vitalis Mathieu, Pellequer Yann, Acar Niyazi, Vigor Claire, Galano Jean-Marie, Durand Thierry, Givalois Laurent, Béduneau Arnaud, Desrumaux Catherine
MMDN, University of Montpellier, EPHE, INSERM, Montpellier, France.
MMDN, University of Montpellier, EPHE, INSERM, Montpellier, France; LipSTIC LabEx (ANR-11-LABX0021), Dijon, France.
Int J Pharm. 2025 Feb 10;670:125125. doi: 10.1016/j.ijpharm.2024.125125. Epub 2025 Jan 7.
Reduced docosahexaenoic acid (DHA) concentrations seem to be associated with an increased risk of Alzheimer's disease (AD), and DHA accretion to the brain across the blood-brain-barrier (BBB) can be modulated by various factors. Therefore, there is an urgent need to identify an efficient and non-invasive method to ensure brain DHA enrichment. In the present study, a safe and stable DHA-enriched nanoemulsion, designed to protect DHA against oxidation, was designed and administered intranasally in a transgenic mouse model of AD, the J20 mice. Intranasal treatment with nanoformulated DHA significantly improved well-being and working spatial memory in six-months-old J20 mice. These behavioral effects were associated with a reduction of amyloid deposition, oxidative stress, and neuroinflammation in brain tissues, which may be partially due to DHA-induced inactivation of the pleiotropic kinase GSK3β. In conclusion, intranasal DHA administration exhibited strong therapeutic effects and disease-modifying benefits in the J20 AD model. Given that DHA has already shown safety and tolerability in healthy human subjects, our results further support the need for clinical trials to assess the potential of this approach in Alzheimer's patients.
二十二碳六烯酸(DHA)浓度降低似乎与阿尔茨海默病(AD)风险增加有关,并且DHA通过血脑屏障(BBB)向大脑的积聚可受多种因素调节。因此,迫切需要确定一种有效且非侵入性的方法来确保大脑中DHA富集。在本研究中,设计了一种安全稳定的富含DHA的纳米乳剂,旨在保护DHA不被氧化,并将其经鼻给予AD转基因小鼠模型J20小鼠。用纳米制剂DHA经鼻治疗显著改善了6月龄J20小鼠的健康状况和工作空间记忆。这些行为效应与脑组织中淀粉样蛋白沉积、氧化应激和神经炎症的减少有关,这可能部分归因于DHA诱导的多效性激酶GSK3β失活。总之,经鼻给予DHA在J20 AD模型中表现出强大的治疗效果和疾病修饰益处。鉴于DHA已在健康人类受试者中显示出安全性和耐受性,我们的结果进一步支持进行临床试验以评估这种方法对阿尔茨海默病患者的潜在作用。