Metabolic GLUT1 Priming with Disulfide-Stabilized Micelles Enables Noninvasive mRNA Delivery across the Blood–Brain Barrier

The blood-brain barrier (BBB) remains the single most obstructive bottleneck to mRNA therapeutics for central nervous system (CNS) disorders. Here we introduce a metabolically primed, redox-locked nanoplatform that converts the brain's glucose addiction into a gate-cracking key. A disulfide-stabilized, glucose-decorated block-cationic copolymer self-assembles with mRNA into 36 nm micelles (ζ potential approximately +4.5 mV) that withstand serum nucleases and polyanionic assault yet disassemble on cytosolic glutathione. Fasting-induced GLUT1 upregulation (4.2-fold) is exploited as a transiently overexpressed "receptor"; a subsequent glycemic spike drives receptor-mediated transcytosis, yielding 160-fold higher cerebral mRNA accumulation versus untargeted controls. Single-cell intravital imaging confirms parenchymal penetration within 120 min and pan-brain GFP expression. The strategy affords spatiotemporally sharp CNS transfection without BBB disruption or systemic toxicity, offering a generalizable, nonviral avenue for genomic medicine of neurological diseases.

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Publication Details

Journal
Bioconjugate Chemistry
Published
2026-01-16
DOI
https://doi.org/10.1021/acs.bioconjchem.5c00621
Primary Topic
RNA Interference and Gene Delivery
Type
article
Field-Weighted Citation Impact
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article

Metabolic GLUT1 Priming with Disulfide-Stabilized Micelles Enables Noninvasive mRNA Delivery across the Blood–Brain Barrier

Y Li, Xiyi Chen, Wei-Dong Le, Zhen Li et al.
Bioconjugate Chemistry
RNA Interference and Gene Delivery
article

Metabolic GLUT1 Priming with Disulfide-Stabilized Micelles Enables Noninvasive mRNA Delivery across the Blood–Brain Barrier

Y Li, Xiyi Chen, Wei-Dong Le, Zhen Li, Xia Cheng, Yan Zhao, Yue Wang, Qixian Chen
article en

Abstract

The blood-brain barrier (BBB) remains the single most obstructive bottleneck to mRNA therapeutics for central nervous system (CNS) disorders. Here we introduce a metabolically primed, redox-locked nanoplatform that converts the brain's glucose addiction into a gate-cracking key. A disulfide-stabilized, glucose-decorated block-cationic copolymer self-assembles with mRNA into 36 nm micelles (ζ potential approximately +4.5 mV) that withstand serum nucleases and polyanionic assault yet disassemble on cytosolic glutathione. Fasting-induced GLUT1 upregulation (4.2-fold) is exploited as a transiently overexpressed "receptor"; a subsequent glycemic spike drives receptor-mediated transcytosis, yielding 160-fold higher cerebral mRNA accumulation versus untargeted controls. Single-cell intravital imaging confirms parenchymal penetration within 120 min and pan-brain GFP expression. The strategy affords spatiotemporally sharp CNS transfection without BBB disruption or systemic toxicity, offering a generalizable, nonviral avenue for genomic medicine of neurological diseases.

Bioconjugate ChemistryVol. 37(2)
Dalian Medical University (CN), Dalian University of Technology (CN), Second Affiliated Hospital of Dalian Medical University (CN), Affiliated Hospital of Liaoning University of Traditional Chinese Medicine (CN), Affiliated Zhongshan Hospital of Dalian University (CN), Liaoning Cancer Hospital & Institute (CN), China Medical University (CN)
Good health and well-being
Openalex Percentile: Top 87%
RNA Interference and Gene Delivery
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