Novel Repurposing of Empagliflozin-Loaded Buccal Composite (Chitosan/Silk Fibroin/Poly(lactic acid)) Nanofibers for Alzheimer’s Disease Management via Modulation of Aβ–AGER–p-tau Pathway

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Authors: Walaa A. El‐Dakroury, Samar A. Salim, Abdelrahman R. Said, Gihan F. Asaad, Mohamed F. Abdelhameed, Mohamed A. Shabana, Mohamed Ibrahim, Sara G. Abualmajd, Haidy H. Mosaad, Aliaa Salama, Shrouk E. Asran, Mayar L. Amer
+2 more Ahmed S. Doghish, Fatma Sa’eed El-Tokhy
Cited by: 6
References: 124

Abstract

Background/Objectives: Empagliflozin (EMPA) was repurposed for Alzheimer’s disease (AD) treatment via buccal delivery, exploiting novel nanofibers (NFs) integrating chitosan (Cs), silk fibroin (Fb), and poly(lactic acid) (PLA). Methods: EMPA-loaded Cs/Fb/PLA NFs were electrospun in different formulations to optimize the formulation parameters. The optimized formulation was then investigated for its enhanced in vivo effect. Results: Optimized nanofiber diameters ranged from 459 ± 173 to 668 ± 148 nm, possessing bead-free morphology confirmed by SEM and satisfactory mechanical properties. EMPA was successfully well-dispersed in the polymer matrix as evidenced by FTIR, XRD, and drug content. The optimized NFs displayed a hydrophilic surface (contact angle < 90°), and biphasic drug release with sustained EMPA liberation (84.98% over 24 h). In vivo, buccal EMPA-Cs/Fb/PLA NFs in an AlCl3-induced AD rat model significantly reduced brain-amyloid-β, phosphorylated tau, IL-1β, and AGER expression by 2.88-, 2.64-, 2.87-, and 2.50-fold, respectively, compared to positive controls, and improved locomotor activity (1.86-fold) and cognitive performance (T-maze) (4.17-fold). Compared to pure EMPA, the nanofiber formulation achieved further reductions in amyloid-β (1.78-fold), p-tau (1.42-fold), IL-1β (1.89-fold), and AGER (1.38-fold), with efficacy comparable to memantine. Histopathological examination revealed preservation of the hippocampal neuronal structure. Conclusions: The findings suggest EMPA-loaded Cs/Fb/PLA NFs as a promising non-invasive, sustained-release buccal delivery platform for AD therapy, offering multimodal neuroprotection through modulation of the Aβ–AGER–p-tau axis.

Fields of Study & Subjects

Advanced Drug Delivery Systems Electrospun Nanofibers in Biomedical Applications Graphene and Nanomaterials Applications

Publication details

Journal / source
Pharmaceutics
Publisher
MDPI AG
Volume
18
Issue
1
Pages
83–83
Publication date
8 January 2026
Language
EN