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@ARTICLE{MartinezDominguez:285737,
author = {Martinez Dominguez, Maria Victoria and Falke, Lisa and
Beretta, Stefania and Dauer, Katharina and Wagner, Karl G.
and Boeckers, Tobias M.},
title = {{M}anufacturing and testing of a polymer formulation for
long-time release delivery of antisense oligonucleotides in
hi{PSC}-derived motoneurons},
journal = {Journal of drug delivery science and technology},
volume = {119},
issn = {1773-2247},
address = {Paris},
publisher = {Ed. de Santé},
reportid = {DZNE-2026-00294},
pages = {108171},
year = {2026},
abstract = {Antisense oligonucleotides (ASOs) are an emerging
therapeutic approach for genetically induced neurological
disorders such as spinal muscular atrophy (SMA). For SMA,
the Food and Drug administration (FDA)-approved ASO
Nusinersen (Spinraza®) restores exon 7 inclusion in
survival motor neuron (SMN) 2, leading to improved
motoneuron survival. However, current administration to
patients requires repeated intrathecal (IT) injections via
lumbar puncture, an invasive procedure with considerable
side effects. There is therefore an urgent need for more
efficient and sustained drug-delivery strategies capable of
overcoming these limitations. In this study, we developed
and tested a system for the controlled, long-term release of
Nusinersen ASO. Using motoneurons derived from human induced
pluripotent stem cells (hiPSCs) from SMA and control
patients, two formulations were evaluated: (I) pure ethylene
vinyl acetate (EVA, $40\%$ vinyl acetate) and (II) a
composite of EVA $(40\%$ vinyl acetate) and silica (50:50
w/w). Both formulations were found to be biocompatible in
the co-cultures in vitro. Moreover, the efficient uptake of
ASOs and the optimization of ASO dose and time-response in
motoneurons was achieved. Additionally, fluorescently
labeled ASOs confirmed sustained release from the implants.
Importantly, sustained polymer-released ASO significantly
increased exon 7 inclusion in SMN2 transcripts and
motoneuron viability over time, demonstrating therapeutic
efficacy and preserved biological activity. These findings
demonstrate the initial feasibility for a minimally
invasive, long-term ASO delivery system that could overcome
the limitation for repeated lumbar punctures in SMA patients
and potentially be adapted as ASO delivery systems for other
neurodegenerative diseases.},
cin = {AG Böckers},
ddc = {610},
cid = {I:(DE-2719)1910002},
pnm = {352 - Disease Mechanisms (POF4-352)},
pid = {G:(DE-HGF)POF4-352},
typ = {PUB:(DE-HGF)16},
doi = {10.1016/j.jddst.2026.108171},
url = {https://pub.dzne.de/record/285737},
}