Targeted delivery of a phosphoinositide 3‐kinase γ inhibitor to restore organ function in sepsis

Abstract Jaundice, the clinical hallmark of infection‐associated liver dysfunction, reflects altered membrane organization of the canalicular pole of hepatocytes and portends poor outcomes. Mice lacking phosphoinositide 3‐kinase‐γ (PI3Kγ) are protected against membrane disintegration and hepatic exc...

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Main Authors: Adrian T Press, Petra Babic, Bianca Hoffmann, Tina Müller, Wanling Foo, Walter Hauswald, Jovana Benecke, Martina Beretta, Zoltán Cseresnyés, Stephanie Hoeppener, Ivo Nischang, Sina M Coldewey, Markus H Gräler, Reinhard Bauer, Falk Gonnert, Nikolaus Gaßler, Reinhard Wetzker, Marc Thilo Figge, Ulrich S Schubert, Michael Bauer
Format: Article
Language:English
Published: Springer Nature 2021-09-01
Series:EMBO Molecular Medicine
Subjects:
Online Access:https://doi.org/10.15252/emmm.202114436
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author Adrian T Press
Petra Babic
Bianca Hoffmann
Tina Müller
Wanling Foo
Walter Hauswald
Jovana Benecke
Martina Beretta
Zoltán Cseresnyés
Stephanie Hoeppener
Ivo Nischang
Sina M Coldewey
Markus H Gräler
Reinhard Bauer
Falk Gonnert
Nikolaus Gaßler
Reinhard Wetzker
Marc Thilo Figge
Ulrich S Schubert
Michael Bauer
author_facet Adrian T Press
Petra Babic
Bianca Hoffmann
Tina Müller
Wanling Foo
Walter Hauswald
Jovana Benecke
Martina Beretta
Zoltán Cseresnyés
Stephanie Hoeppener
Ivo Nischang
Sina M Coldewey
Markus H Gräler
Reinhard Bauer
Falk Gonnert
Nikolaus Gaßler
Reinhard Wetzker
Marc Thilo Figge
Ulrich S Schubert
Michael Bauer
author_sort Adrian T Press
collection DOAJ
description Abstract Jaundice, the clinical hallmark of infection‐associated liver dysfunction, reflects altered membrane organization of the canalicular pole of hepatocytes and portends poor outcomes. Mice lacking phosphoinositide 3‐kinase‐γ (PI3Kγ) are protected against membrane disintegration and hepatic excretory dysfunction. However, they exhibit a severe immune defect that hinders neutrophil recruitment to sites of infection. To exploit the therapeutic potential of PI3Kγ inhibition in sepsis, a targeted approach to deliver drugs to hepatic parenchymal cells without compromising other cells, in particular immune cells, seems warranted. Here, we demonstrate that nanocarriers functionalized through DY‐635, a fluorescent polymethine dye, and a ligand of organic anion transporters can selectively deliver therapeutics to hepatic parenchymal cells. Applying this strategy to a murine model of sepsis, we observed the PI3Kγ‐dependent restoration of biliary canalicular architecture, maintained excretory liver function, and improved survival without impairing host defense mechanisms. This strategy carries the potential to expand targeted nanomedicines to disease entities with systemic inflammation and concomitantly impaired barrier functionality.
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spelling doaj-art-0fad10ab812d436c8a511f93c2eb66d82025-08-20T02:11:22ZengSpringer NatureEMBO Molecular Medicine1757-46761757-46842021-09-01131011710.15252/emmm.202114436Targeted delivery of a phosphoinositide 3‐kinase γ inhibitor to restore organ function in sepsisAdrian T Press0Petra Babic1Bianca Hoffmann2Tina Müller3Wanling Foo4Walter Hauswald5Jovana Benecke6Martina Beretta7Zoltán Cseresnyés8Stephanie Hoeppener9Ivo Nischang10Sina M Coldewey11Markus H Gräler12Reinhard Bauer13Falk Gonnert14Nikolaus Gaßler15Reinhard Wetzker16Marc Thilo Figge17Ulrich S Schubert18Michael Bauer19Department of Anesthesiology and Intensive Care Medicine, Jena University HospitalDepartment of Anesthesiology and Intensive Care Medicine, Jena University HospitalResearch Group Applied Systems Biology, Leibniz Institute for Natural Product Research and Infection Biology ‐ Hans Knoell InstituteDepartment of Anesthesiology and Intensive Care Medicine, Jena University HospitalDepartment of Anesthesiology and Intensive Care Medicine, Jena University HospitalLeibniz Institute of Photonic TechnologyDepartment of Anesthesiology and Intensive Care Medicine, Jena University HospitalDepartment of Anesthesiology and Intensive Care Medicine, Jena University HospitalResearch Group Applied Systems Biology, Leibniz Institute for Natural Product Research and Infection Biology ‐ Hans Knoell InstituteJena Center for Soft Matter (JCSM), Friedrich Schiller University JenaJena Center for Soft Matter (JCSM), Friedrich Schiller University JenaDepartment of Anesthesiology and Intensive Care Medicine, Jena University HospitalDepartment of Anesthesiology and Intensive Care Medicine, Jena University HospitalInstitute of Molecular Cell Biology, Jena University HospitalDepartment of Anesthesiology and Intensive Care Medicine, Jena University HospitalSection of Pathology, Institute of Forensic Medicine, Jena University HospitalDepartment of Anesthesiology and Intensive Care Medicine, Jena University HospitalCenter for Sepsis Control and Care, Jena University HospitalCenter for Sepsis Control and Care, Jena University HospitalDepartment of Anesthesiology and Intensive Care Medicine, Jena University HospitalAbstract Jaundice, the clinical hallmark of infection‐associated liver dysfunction, reflects altered membrane organization of the canalicular pole of hepatocytes and portends poor outcomes. Mice lacking phosphoinositide 3‐kinase‐γ (PI3Kγ) are protected against membrane disintegration and hepatic excretory dysfunction. However, they exhibit a severe immune defect that hinders neutrophil recruitment to sites of infection. To exploit the therapeutic potential of PI3Kγ inhibition in sepsis, a targeted approach to deliver drugs to hepatic parenchymal cells without compromising other cells, in particular immune cells, seems warranted. Here, we demonstrate that nanocarriers functionalized through DY‐635, a fluorescent polymethine dye, and a ligand of organic anion transporters can selectively deliver therapeutics to hepatic parenchymal cells. Applying this strategy to a murine model of sepsis, we observed the PI3Kγ‐dependent restoration of biliary canalicular architecture, maintained excretory liver function, and improved survival without impairing host defense mechanisms. This strategy carries the potential to expand targeted nanomedicines to disease entities with systemic inflammation and concomitantly impaired barrier functionality.https://doi.org/10.15252/emmm.202114436cholestasisdrug deliveryliver failurePI3Ksepsis
spellingShingle Adrian T Press
Petra Babic
Bianca Hoffmann
Tina Müller
Wanling Foo
Walter Hauswald
Jovana Benecke
Martina Beretta
Zoltán Cseresnyés
Stephanie Hoeppener
Ivo Nischang
Sina M Coldewey
Markus H Gräler
Reinhard Bauer
Falk Gonnert
Nikolaus Gaßler
Reinhard Wetzker
Marc Thilo Figge
Ulrich S Schubert
Michael Bauer
Targeted delivery of a phosphoinositide 3‐kinase γ inhibitor to restore organ function in sepsis
EMBO Molecular Medicine
cholestasis
drug delivery
liver failure
PI3K
sepsis
title Targeted delivery of a phosphoinositide 3‐kinase γ inhibitor to restore organ function in sepsis
title_full Targeted delivery of a phosphoinositide 3‐kinase γ inhibitor to restore organ function in sepsis
title_fullStr Targeted delivery of a phosphoinositide 3‐kinase γ inhibitor to restore organ function in sepsis
title_full_unstemmed Targeted delivery of a phosphoinositide 3‐kinase γ inhibitor to restore organ function in sepsis
title_short Targeted delivery of a phosphoinositide 3‐kinase γ inhibitor to restore organ function in sepsis
title_sort targeted delivery of a phosphoinositide 3 kinase γ inhibitor to restore organ function in sepsis
topic cholestasis
drug delivery
liver failure
PI3K
sepsis
url https://doi.org/10.15252/emmm.202114436
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