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.
Authors
- Y Li
- Xiyi Chen (ORCID: https://orcid.org/0000-0001-7855-1177)
- Wei-Dong Le
- Zhen Li
- Xia Cheng
- Yan Zhao
- Yue Wang
- Qixian Chen
Institutions
- 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)
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
- 0.00