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@ARTICLE{Singh:901790,
author = {Singh, Smriti and Drude, Natascha and Blank, Lena and
Desai, Prachi Bharat and Königs, Hiltrud and Rütten,
Stephan and Langen, Karl-Josef and Möller, Martin and
Mottaghy, Felix M. and Morgenroth, Agnieszka},
title = {{P}rotease {R}esponsive {N}anogels for {T}ranscytosis
across the {B}lood−{B}rain {B}arrier and {I}ntracellular
{D}elivery of {R}adiopharmaceuticals to {B}rain {T}umor
{C}ells},
journal = {Advanced healthcare materials},
volume = {10},
number = {20},
issn = {2192-2659},
address = {Weinheim},
publisher = {Wiley-VCH},
reportid = {FZJ-2021-03823},
pages = {2100812 -},
year = {2021},
abstract = {Despite profound advances in treatment approaches, gliomas
remain associated with very poor prognoses. The residual
cells after incomplete resection often migrate and
proliferate giving a seed for highly resistant gliomas. The
efficacy of chemotherapeutic drugs is often strongly limited
by their poor selectivity and the blood brain barrier (BBB).
Therefore, the development of therapeutic carrier systems
for efficient transport across the BBB and selective
delivery to tumor cells remains one of the most complex
problems facing molecular medicine and nano-biotechnology.
To address this challenge, a stimuli sensitive nanogel is
synthesized using pre-polymer approach for the effective
delivery of nano-irradiation. The nanogels are cross-linked
via matrix metalloproteinase (MMP-2,9) substrate and armed
with Auger electron emitting drug
5-[125I]Iodo-4”-thio-2”-deoxyuridine ([125I]ITdU) which
after release can be incorporated into the DNA of tumor
cells. Functionalization with diphtheria toxin receptor
ligand allows nanogel transcytosis across the BBB at tumor
site. Functionalized nanogels efficiently and increasingly
explore transcytosis via BBB co-cultured with glioblastoma
cells. The subsequent nanogel degradation correlates with
up-regulated MMP2/9. Released [125I]ITdU follows the
thymidine salvage pathway ending in its incorporation into
the DNA of tumor cells. With this concept, a highly
efficient strategy for intracellular delivery of
radiopharmaceuticals across the challenging BBB is
presented.},
cin = {INM-4 / PTJ-NMT},
ddc = {610},
cid = {I:(DE-Juel1)INM-4-20090406 / I:(DE-Juel1)PTJ-NMT-20090406},
pnm = {5253 - Neuroimaging (POF4-525)},
pid = {G:(DE-HGF)POF4-5253},
typ = {PUB:(DE-HGF)16},
pubmed = {34490744},
UT = {WOS:000692944100001},
doi = {10.1002/adhm.202100812},
url = {https://juser.fz-juelich.de/record/901790},
}