Abstract：
Alzheimer\'s disease (AD) is a very common disorder that affects the elderly. There are relatively few medications that can be used orally or as a suspension to treat AD. A mucoadhesive (o/w) nano emulsion of mefenamic acid was made by adding Carbopol 940P to the optimised drug nanoemulsion using distilled water as the aqueous phase (6%); Solutol HS: tween 20 (3.6%) as the surfactant and co-surfactant; and clove oil: TPGS (0.4%) as the oil phase and mefenamic acid as the drug (2.8 mg/ml). The mucoadhesive nanoemulsion (S40.5%w/v) had a particle size of 91.20 nm, polydispersity index of 0.270, and surface charge of - 12.4 mV. Significantly higher (p < 0.001) drug release (89.37%) was observed for mucoadhesive drug formulation in comparison to mucoadhesive drug suspension (25.64%) at 8 h. The ex vivo nasal permeation of 83.03% in simulated nasal fluid and 85.71% in artificial cerebrospinal fluid was observed. The percent inhibition and inhibitory concentration (IC50) of mucoadhesive drug nanoemulsion were found to be 91.57 ± 2.69 and 6.76 respectively. Higher cell viability on glioblastoma cells (85-80%) was researched for mucoadhesive nanoemulsion as compared to drug suspension (80-70%). Significantly higher (p < 0.001) drug absorption and Cmax (491.94 ± 24.13 ng/ml) of mucoadhesive drug nanoemulsion were observed than mucoadhesive drug suspension (107.46 ± 11.46 ng/ml) at 8 h. The stability studies confirmed that the formulation was stable at 40°C ± 2°C and 75 ± 5% RH. The authors concluded that the mucoadhesive mefenamic acid-loaded nanoemulsion may be an effective technique for treating Alzheimer\'s disease by intranasal route.
摘要：
阿尔茨海默病（AD）是一种非常常见的影响老年人的疾病。相对较少的药物可以口服或作为混悬液来治疗AD。通过将Carbopol940P添加到优化的药物纳米乳液中来制备甲芬那酸的粘膜粘附(o/w)纳米乳液,使用蒸馏水作为水相(6%);SolutolHS:吐温20(3.6%)作为表面活性剂和助表面活性剂;和丁香油:TPGS(0.4%)作为油相和甲芬那酸作为药物(2.8mg/ml)。粘膜粘附纳米乳液(S40.5%w/v)的粒径为91.20nm,多分散指数为0.270，表面电荷为-12.4mV。在8小时时,与粘膜粘附药物悬浮液(25.64%)相比,粘膜粘附药物制剂的药物释放(89.37%)显著更高(p<0.001)。观察到在模拟鼻液中83.03%的离体鼻渗透和在人工脑脊液中85.71%的离体鼻渗透。发现粘膜粘附药物纳米乳剂的抑制百分比和抑制浓度(IC50)分别为91.57±2.69和6.76。与药物悬浮液(80-70%)相比,对于粘膜粘附纳米乳液,研究了胶质母细胞瘤细胞上更高的细胞活力(85-80%)。在8h时观察到粘膜粘附药物纳米乳剂的药物吸收和Cmax(491.94±24.13ng/ml)显著高于粘膜粘附药物悬浮液(107.46±11.46ng/ml)。稳定性研究证实制剂在40°C±2°C和75±5%RH下是稳定的。作者得出结论，粘膜粘附性甲芬那酸纳米乳剂可能是通过鼻内途径治疗阿尔茨海默病的有效技术。
