二氢槲皮素纳米颗粒鼻腔凝胶是一种有望改善阿尔茨海默病的配方。

IF 5.3 2区 医学 Q1 PHARMACOLOGY & PHARMACY
Basant A. Abou-Taleb , Wessam F. El-Hadidy , Inas M. Masoud , Noura A. Matar , Hoda S. Hussein
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引用次数: 0

摘要

二氢槲皮素是一种天然类黄酮,具有抗炎、抗氧化和神经保护活性。二氢槲皮素通过阻止淀粉样β肽-Aβ(1-42)的聚集,对阿尔茨海默氏症有很好的神经保护作用。这项研究的目的是创造出载入壳聚糖的双氢槲皮素纳米粒子(DHQ-CS NPs),并将其载入具有粘附性、热敏性的原位凝胶中,直接经鼻给药治疗阿尔茨海默氏症。在壳聚糖纳米颗粒中添加药物并将其加入热敏凝胶后,药物在鼻腔中的停留时间延长,粘膜通透性降低。采用凝胶和纳米颗粒的不同体外物理化学特征对配方进行了评估。与鼻内 DHQ 凝胶相比,DHQ-CS NPs 凝胶在阿尔茨海默氏症大鼠模型中的治疗效果得到了行为学、生物化学和组织病理学方面的评估。结果表明,DHQ-CS NPs 凝胶的粒径为 235.3 nm。与未加工的 DHQ 凝胶相比,DHQ-CS NPs 凝胶的释放率更高。此外,与 DHQ 凝胶相比,鼻腔给药 DHQ-CS NPs 凝胶通过改善链脲佐菌素诱导的阿尔茨海默大鼠的记忆和学习障碍,以及探索行为和新物体记忆,显示出更好的体内效果。生化方面,与 DHQ 凝胶相比,鼻内 DHQ-CS NPs 凝胶减少了 Aβ 蛋白的形成和 tau 蛋白的过度磷酸化,抑制了乙酰胆碱酯酶的活性和大脑中的氧化应激,增加了大脑和血清中的总抗氧化剂。从组织病理学角度看,DHQ-CS NPs 鼻用凝胶改善了海马和大脑皮层结构,与正常组相当。因此,鼻内 DHQ-CS NPs 负载原位凝胶似乎是一种很有前景的阿尔茨海默病治疗配方。
本文章由计算机程序翻译,如有差异,请以英文原文为准。

Dihydroquercetin nanoparticles nasal gel is a promising formulation for amelioration of Alzheimer’s disease

Dihydroquercetin nanoparticles nasal gel is a promising formulation for amelioration of Alzheimer’s disease
Dihydroquercetin is a natural flavonoid with anti-inflammatory, antioxidant, and neuroprotective activities. Dihydroquercetin exhibits a great neuroprotector promise in Alzheimer’s disorder via preventing the aggregation of amyloid-beta-peptide-Aβ(1–42). The goal of the study was to create dihydroquercetin-loaded-chitosan nanoparticles (DHQ-CS NPs) loaded to a mucoadhesive, thermosensitive in-situ gel for direct nasal administration to cure Alzheimer’s disorder. Loading drug in chitosan nanoparticles and incorporation into thermosensitive gel enhanced residence time and reduced mucociliary-clearance. Different in-vitro-physicochemical-characteristics of gels and nanoparticles-characterization were used to evaluate the formulations. The therapeutic effectiveness of DHQ-CS NPs gel was evaluated behaviorally, biochemically and histopathologically in Alzheimer’s-rat-model compared to intranasal DHQ gel. The small particles-size was obtained = 235.3 nm of DHQ-CS NPs. The DHQ-CS NPs gel demonstrated a greater release rate compared to the raw DHQ gel. Additionally, the nasal-administration of the DHQ-CS NPs gel showed better In-vivo results compared to DHQ gel, through improvement of memory and learning deficits and also the exploratory behavior and new object memory in streptozotocin induced-Alzheimer rats. Biochemically, the intranasal DHQ-CS NPs gel, showed reduced both Aβ-protein formation and tau protein hyperphosphorylation, inhibition of acetylcholine esterase activity and oxidative stress in the brain with increase of total antioxidants in the brain and serum, compared to DHQ gel. Histopathologically, the DHQ-CS NPs nasal gel produced improvement in the hippocampal and cerebral cortex structures, being comparable to the normal group. Consequently, the intranasal DHQ-CS NPs loaded in-situ gel seems to be a promising therapeutic formulation for Alzheimer’s disease medication.
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来源期刊
CiteScore
10.70
自引率
8.60%
发文量
951
审稿时长
72 days
期刊介绍: The International Journal of Pharmaceutics is the third most cited journal in the "Pharmacy & Pharmacology" category out of 366 journals, being the true home for pharmaceutical scientists concerned with the physical, chemical and biological properties of devices and delivery systems for drugs, vaccines and biologicals, including their design, manufacture and evaluation. This includes evaluation of the properties of drugs, excipients such as surfactants and polymers and novel materials. The journal has special sections on pharmaceutical nanotechnology and personalized medicines, and publishes research papers, reviews, commentaries and letters to the editor as well as special issues.
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