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Evaluation of the toxicity and efficacy of a multi-target polymer-drug nano-polyplex in SH-SY5Y cells and Drosophila model of tauopathy

Abstract:
Hyperphosphorylated tau contributes to synaptic damage and neuronal dysfunction in neurodegenerative diseases such as Alzheimer's disease (AD), making it a key therapeutic target. This study evaluated the toxicity and therapeutic potential of a novel polymer-drug nano-polyplex, N5NM15, and polyacrylic acid (PAA) in Drosophila tauopathy models and undifferentiated human SH-SY5Y cells. Cellular uptake was demonstrated by N5NM15, and SH-SY5Y cell viability was significantly enhanced (45%, p ≤ 0.0001) under okadaic acid-induced stress, and total tau levels were reduced (1.43-fold, p ≤ 0.01). In comparison, PAA had a modest effect on decreasing tau phosphorylation (1.3-fold) at the pSer202/pThr205 site. Toxicity studies in Drosophila revealed that N5NM15 (3.5:1 and 44:12.5 µg/mL) and PAA (44 µg/mL) were toxic to adult flies expressing the eye-specific driver (GMR-GAL4) but were well-tolerated in flies overexpressing the pan-neuronal driver ELAV-GAL4. Furthermore, treatment with N5NM15 and PAA did not improve the ommatidial arrangement, eye bristle count, or eye length in tauopathy models. Climbing and survival assays indicated a potential mild protective effect at a lower concentration (3.5:1 µg/mL) at the early stage of the disease, but at a higher dose (44:12.5 µg/mL) was significantly toxic, in both wild-type (p ≤ 0.0001) and tauopathy models (p < 0.05). These findings highlight the need for N5NM15 and PAA dose optimisation and reformulation with non-toxic buffers to enhance therapeutic potential while minimising adverse effects in normal and Drosophila tauopathy models for AD treatment.
Publication status:
Published
Peer review status:
Peer reviewed

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Publisher copy:
10.1038/s41598-025-22924-0

Authors

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Role:
Author
ORCID:
0009-0004-3298-2587
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Institution:
University of Oxford
Division:
MSD
Department:
Oncology
Role:
Author
ORCID:
0000-0002-5005-1864
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Role:
Author
ORCID:
0000-0003-2217-0900


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Funder identifier:
https://ror.org/037866t57
Grant:
G22.06 BG
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Funder identifier:
https://ror.org/025sbr097
Grant:
C23-1720928079


Publisher:
Springer Nature
Journal:
Scientific Reports More from this journal
Volume:
15
Issue:
1
Article number:
39454
Place of publication:
England
Publication date:
2025-11-11
Acceptance date:
2025-10-03
DOI:
EISSN:
2045-2322
Pmid:
41219231


Language:
English
Keywords:
Pubs id:
2409673
Local pid:
pubs:2409673
Source identifiers:
W4416113290
Deposit date:
2026-04-21
ARK identifier:

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