Optimization, Characterization and In-Vitro Cellular Uptake of Donepezil-Loaded NanoCrystVesicles

IF 2.7 4区化学 Q2 CHEMISTRY, INORGANIC & NUCLEAR

Journal of Cluster Science Pub Date : 2024-04-06 DOI:10.1007/s10876-024-02608-x

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Abstract

The prevalence of Alzheimer's disease (AD) in developed and developing nations is increasing day by day. The monotherapy doesn't fit best for AD due to chronic treatment. This work aimed to prepare the liposomes coloaded with Donepezil and pine oil intended for adjuvant effect. Pine oil was selected due to its amyloid disaggregation and AChE inhibition property. The thin film hydration method with sonication was selected to formulate ultra-small-sized unilamellar vesicles. Apart from this formulated vesicle were subject to particle size, morphological, release, nasal ciliotoxicity and cellular uptake studies. The PDI, particle size, and zeta potential of the final egg lecithin-based liposome were found to be 0.19, 129 nm, and -27.5 mV, respectively, stable at 4° and 25°C. SEM microscopy of oil-loaded liposomes exhibits a crystalline cubic shape and is compared with alone drug-loaded liposomes that are spherical. AChE inhibition activity was found to be higher in combination when compared with others. The prepared liposomes were safe when studied for nasal ciliotoxicity studies and rapid uptake by C6 cells with complete internalization. This study demonstrated the development and potential of the vesicular system that carries valuable characteristics and overcomes patient compliance concerns that prove to be novel therapeutics for managing AD.

Graphical Abstract

Abstract Image

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多奈哌齐负载型纳米晶体囊泡的优化、表征和体外细胞吸收

摘要阿尔茨海默病（AD）在发达国家和发展中国家的发病率与日俱增。由于需要长期治疗，单一疗法并不适合阿尔茨海默病。这项研究旨在制备含有多奈哌齐和松油的脂质体，以达到辅助治疗的效果。之所以选择松油，是因为它具有淀粉样蛋白分解和 AChE 抑制特性。采用超声薄膜水合法来配制超小型单酰胺基囊泡。此外，还对配制的囊泡进行了粒度、形态、释放、鼻腔纤毛毒性和细胞摄取研究。结果发现，最终卵磷脂脂质体的 PDI、粒度和 zeta 电位分别为 0.19、129 nm 和 -27.5 mV，并在 4° 和 25°C 温度下保持稳定。油载脂质体的扫描电镜显微镜观察显示其呈结晶立方体状，而单独的药物载脂体则呈球形。与其他脂质体相比，组合脂质体的 AChE 抑制活性更高。在鼻腔纤毛虫毒性研究中，制备的脂质体是安全的，而且能被 C6 细胞快速吸收并完全内化。这项研究证明了囊泡系统的发展和潜力，它具有宝贵的特性，克服了患者的依从性问题，被证明是治疗注意力缺失症的新型疗法。图表摘要

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来源期刊

Journal of Cluster Science 化学-无机化学与核化学

CiteScore

6.70

自引率

0.00%

发文量

166

审稿时长

3 months

期刊介绍： The journal publishes the following types of papers: (a) original and important research; (b) authoritative comprehensive reviews or short overviews of topics of current interest; (c) brief but urgent communications on new significant research; and (d) commentaries intended to foster the exchange of innovative or provocative ideas, and to encourage dialogue, amongst researchers working in different cluster disciplines.