Brain-targeted delivery of obidoxime, using aptamer-modified liposomes, for detoxification of organophosphorus compounds
Abstract
Effective intracerebral delivery acetylcholinesterase (AChE) reactivator is key for the acute organophosphorus (OPs) poison treatment. However, the blood-brain barrier (BBB) restricts the transport of these drugs from blood into the brain. Herein, we developed transferrin receptor (TfR) aptamer-functionalized liposomes (Apt-LP) that could deliver AChE reactivator (obidoxime) across the BBB to act against paraoxon (POX) poisoning. The aptamer had strong affinity for TfR and was modified with 3'-inverted deoxythymidine (dT) to improve serum stability. The uptake of Apt-LP by bEnd.3 cells was significantly higher than that of non-targeting liposomes. The ability of Apt-LP to penetrate intact BBB was confirmed in in vitro BBB mice model and in vivo biodistribution studies. Treatment of POX-poisoned mice with Apt-LP-LuH-6 reactivated 18% of the brain AChE activity and prevented brain damage to some extent. Taken together, these results showed that Apt-LP may be used as a promising brain-targeted drug delivery system against OPs toxicity.
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Transferrin receptor aptamer-functionalized liposomes have higher BBB penetration efficiency than non-targeting liposomes confirmed by in vitro BBB model and in vivo biodistribution.
“Compared with non-targeting liposomes, this functionalized system has higher BBB penetration efficiency confirmed by both in vitro BBB model and in vivo biodistribution study.”
From The blood–brain barrier: Structure, regulation and drug delivery (2023) · cites this paper as [254]
Cites
Crossing the blood-brain barrier with nanoparticles
Zhou, Y., Peng, Z., Seven, E. S., & Leblanc, R. M. (2018) · Journal of Controlled Release · doi:10.1016/j.jconrel.2017.12.015 · Cited by 837 · see citing works
Nanomaterial-based blood-brain-barrier (BBB) crossing strategies
Xie, J., Shen, Z., Anraku, Y., Kataoka, K., & Chen, X. (2019) · Biomaterials · doi:10.1016/j.biomaterials.2019.119491 · Cited by 604 · see citing works
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The blood–brain barrier: Structure, regulation and drug delivery
Wu, D., Chen, Q., Chen, X., Han, F., Chen, Z., & Wang, Y. (2023) · Signal Transduction and Targeted Therapy · doi:10.1038/s41392-023-01481-w · Cited by 1,906 · see citing works
“254 But it begs for the question that how can targeting ligand-modi fi ed liposomes bypass through the BBB via receptor-mediated transcytosis.”
BackgroundMethodSelf-citation
- Authors
- Zhang, Y., He, J., Shen, L., Wang, T., Yang, J., Li, Y., Wang, Y., & Quan, D.
- Affiliations
- Academy of Military Medical Sciences (CN)
- Corresponding author
- Wang, Yongan
- Quan, Dongqin
- Venue
- Journal of Controlled Release
- Publisher
- Elsevier BV
- Published
- 2021-01
- Volume
- 329
- Pages
- 1117-1128
- ISSN
- 0168-3659 (ISSN-L)
- OpenAlex
- W3094417048
- Cited by
- 59
- References
- 2
- Citations by year
- 2026: 2 · 2025: 12 · 2024: 10 · 2023: 15 · 2022: 14 · 2021: 5
- FWCI
- 2.21
- Type
- journal article
- Language
- en
- Open access
- closed
- Locations
- Journal of Controlled Release (publishedVersion)
- PubMed (publishedVersion)
- Funders
- Academy of Military Medical Sciences
- Topics
- Physical Sciences › Materials Science › Biomaterials › Nanoparticle-Based Drug Delivery
- Life Sciences › Biochemistry, Genetics and Molecular Biology › Molecular Biology › RNA Interference and Gene Delivery
- Life Sciences › Neuroscience › Neurology › Barrier Structure and Function Studies
- Keywords
- obidoxime, organophosphate poisoning, paraoxon, blood-brain barrier, brain drug delivery, transferrin receptor, acetylcholinesterase reactivators, serum stability, bEnd.3 cells, tissue distribution, neuroprotection
- MeSH terms
- Animals, Brain, Cholinesterase Reactivators, Liposomes, Obidoxime Chloride, Organophosphorus Compounds, Tissue Distribution, Mice
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