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@ARTICLE{Khalin:278048,
author = {Khalin, Igor and Adarsh, Nagappanpillai and Schifferer,
Martina and Wehn, Antonia and Boide-Trujillo, Valeria J and
Mamrak, Uta and Shrouder, Joshua and Misgeld, Thomas and
Filser, Severin and Klymchenko, Andrey S and Plesnila,
Nikolaus},
title = {{N}anocarrier {D}rug {R}elease and {B}lood-{B}rain
{B}arrier {P}enetration at {P}ost-{S}troke {M}icrothrombi
{M}onitored by {R}eal-{T}ime {F}örster {R}esonance {E}nergy
{T}ransfer.},
journal = {ACS nano},
volume = {19},
number = {15},
issn = {1936-0851},
address = {Washington, DC},
publisher = {Soc.},
reportid = {DZNE-2025-00554},
pages = {14780 - 14794},
year = {2025},
abstract = {Nanotechnology holds great promise for improving the
delivery of therapeutics to the brain. However, current
approaches often operate at the organ or tissue level and
are limited by the lack of tools to dynamically monitor
cargo delivery in vivo. We have developed highly fluorescent
lipid nanodroplets (LNDs) that enable tracking of
nanocarrier behavior at the subcellular level while also
carrying a Förster resonance energy transfer (FRET)-based
drug delivery detection system (FedEcs) capable of
monitoring cargo release in vivo. Using two-photon
microscopy, we demonstrate that circulating LNDs in naïve
mouse brain vasculature exhibit 3D real-time FRET changes,
showing size-dependent stability over 2 h in blood
circulation. Further, in the Nanostroke model, dynamic
intravital two-photon imaging revealed that LNDs accumulated
within cerebral postischemic microthrombi, where they
released their cargo significantly faster than in normal
blood circulation. Furthermore, the blood-brain barrier
(BBB) became permeable at the microclot sites thereby
allowing accumulated FedEcs-LNDs to cross the BBB and
deliver their cargo to the brain parenchyma. This
microthrombi-associated translocation was confirmed at the
ultrastructural level via volume-correlative light-electron
microscopy. Consequently, FedEcs represents an advanced tool
to quantitatively study the biodistribution and cargo
release of nanocarriers at high resolution in real-time. By
enabling us to resolve passive targeting mechanisms
poststroke, specifically, accumulation, degradation, and
extravasation via poststroke microthrombi, this system could
significantly enhance the translational validation of
nanocarriers for future treatments of brain diseases.},
keywords = {Blood-Brain Barrier: metabolism / Blood-Brain Barrier: drug
effects / Animals / Fluorescence Resonance Energy Transfer /
Mice / Drug Carriers: chemistry / Stroke: drug therapy /
Stroke: metabolism / Drug Liberation / Nanoparticles:
chemistry / Lipids: chemistry / Thrombosis: drug therapy /
Thrombosis: metabolism / Mice, Inbred C57BL / blood-brain
barrier (Other) / correlative light-electron microscopy
(Other) / microthrombosis (Other) / nanocarriers (Other) /
stroke (Other) / Drug Carriers (NLM Chemicals) / Lipids (NLM
Chemicals)},
cin = {AG Misgeld / LMF},
ddc = {540},
cid = {I:(DE-2719)1110000-4 / I:(DE-2719)1040180},
pnm = {351 - Brain Function (POF4-351) / 899 - ohne Topic
(POF4-899)},
pid = {G:(DE-HGF)POF4-351 / G:(DE-HGF)POF4-899},
experiment = {EXP:(DE-2719)LMF-20190308},
typ = {PUB:(DE-HGF)16},
pubmed = {pmid:40180319},
doi = {10.1021/acsnano.4c17011},
url = {https://pub.dzne.de/record/278048},
}