Repurposing linagliptin-loaded novasomes as a neuroprotectant for Alzheimer's disease: in-vitro characterisation, statistical optimisation and ex-vivo permeation study.

IF 3 4区医学 Q2 CHEMISTRY, APPLIED

Journal of microencapsulation Pub Date : 2025-05-07 DOI:10.1080/02652048.2025.2500542

Michael M Farag, Nevine S Abdelmalak, Shahira F El Menshawe, Asmaa S Omara, Doaa S Hamad

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引用次数: 0

Abstract

Aim: Linagliptin (LGP) has poor oral bioavailability due to P-gp efflux and first-pass metabolism. This study aimed to develop LGP-loaded novasomes (LGP-NVS) for intranasal brain delivery.

Methods: LGP-NVS were prepared via thin film hydration and optimised using a Box-Behnken design, varying cholesterol, stearic acid, and span-80 levels. Fifteen formulations were evaluated for particle size, entrapment efficiency, zeta potential, and drug release. The optimised formula underwent further surface, compatibility, permeability, and stability studies.

Results: The optimised formula showed high entrapment (84.22% ± 1.68%), small particle size (239.35 ± 15.20 nm), plausible zeta potential (-30.25 ± 1.23 mV), polydispersity index (0.32 ± 0.058), and controlled release (66.85 ± 2.25% after 8 h). Transmission electron microscopy demonstrated uniform size. Stability was maintained over three months. Ex-vivo permeation studies showed 1.39-fold higher permeation through camel nasal mucosa compared to drug solution.

Conclusion: Intranasal LGP-NVS might be an auspicious therapeutic avenue for the combat of Alzheimer's disease.

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重新利用利格列汀负载的novassomes作为阿尔茨海默病的神经保护剂：体外表征，统计优化和离体渗透研究

目的：利格列汀（LGP）由于P-gp外排和首过代谢而具有较差的口服生物利用度。本研究旨在开发用于经鼻给药的LGP-NVS。方法：通过薄膜水合法制备LGP-NVS，并采用Box-Behnken设计优化，改变胆固醇、硬脂酸和span-80水平。评估了15种制剂的粒径、包封效率、zeta电位和药物释放。优化后的配方进行了进一步的表面、相容性、渗透性和稳定性研究。结果：优化后的配方包封度高（84.22%±1.68%），粒径小（239.35±15.20 nm）， zeta电位合理（-30.25±1.23 mV），多分散指数（0.32±0.058），8 h后控释率为66.85±2.25%。透射电镜显示尺寸均匀。稳定维持了三个多月。离体渗透研究表明，与药物溶液相比，通过骆驼鼻黏膜的渗透性高1.39倍。结论：鼻用LGP-NVS可能是治疗阿尔茨海默病的一种有利途径。

本文章由计算机程序翻译，如有差异，请以英文原文为准。

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来源期刊

Journal of microencapsulation 工程技术-工程：化工

CiteScore

6.30

自引率

2.60%

发文量

审稿时长

3 months

期刊介绍： The Journal of Microencapsulation is a well-established, peer-reviewed journal dedicated to the publication of original research findings related to the preparation, properties and uses of individually encapsulated novel small particles, as well as significant improvements to tried-and-tested techniques relevant to micro and nano particles and their use in a wide variety of industrial, engineering, pharmaceutical, biotechnology and research applications. Its scope extends beyond conventional microcapsules to all other small particulate systems such as self assembling structures that involve preparative manipulation. The journal covers: Chemistry of encapsulation materials Physics of release through the capsule wall and/or desorption from carrier Techniques of preparation, content and storage Many uses to which microcapsules are put.