Angiopep‐Conjugated Electro‐Responsive Hydrogel Nanoparticles: Therapeutic Potential for Epilepsy
Abstract
A safe and effective therapy for epilepsy requires a drug delivery system that can penetrate the blood–brain barrier and subsequently release antiepileptic drugs rapidly to suppress neuronal discharges in a timely manner. We have developed electro‐responsive hydrogel nanoparticles (ERHNPs) modified with angiopep‐2 (ANG) to facilitate the delivery of the antiepileptic drug phenytoin sodium. The resulting ANG‐ERHNPs had an average diameter of (102.3±16.8) nm and were electro‐sensitive with regard to particle size and drug release in vitro. ANG‐ERHNPs have the characteristics of penetrate the BBB easily, resulting in a higher distribution in the central system. The improved antiepileptic effects were investigated with the amygdala kindling model. The results demonstrate that the ANG‐ERHNPs were able to transport antiepileptic drugs into the brain and release them under electroencephalograph epileptiform abnormalities to greatly improve the therapeutic index of existing drugs in clinical use.
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Functionalization of electro-responsive nanogels with angiopep-2, a dual-targeting ligand towards LRP-1, significantly improved brain accumulation.
“The brain accumulation of electro-responsive nanogels was significantly improved by the functionalization.”
From The blood–brain barrier: Structure, regulation and drug delivery (2023) · cites this paper as [181]
Cites
Targeted Delivery of Nanoparticles to Ischemic Muscle for Imaging and Therapeutic Angiogenesis
Kim, J., Cao, L., Shvartsman, D., Silva, E. A., & Mooney, D. J. (2011) · Nano Letters · doi:10.1021/nl103812a · Cited by 150 · 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
“Previously, our group has reported an angiopep-2 (a dual-targeting ligand towards LRP-1) modified nanogel for targeted delivery of anti-epileptic drugs.(181,182) The brain accumulation of electro-responsive nanogels was significantly improved by the functionalization.”
BackgroundSelf-citationThe Smart Drug Delivery System and Its Clinical Potential
Liu, D., Yang, F., Xiong, F., & Gu, N. (2016) · Theranostics · doi:10.7150/thno.14858 · Cited by 1,066 · see citing works
Ultrasound‐Activated Sensitizers and Applications
Lin, X., Song, J., Chen, X., & Yang, H. (2020) · Angewandte Chemie International Edition · doi:10.1002/anie.201906823 · Cited by 501 · see citing works
- Authors
- Ying, X., Wang, Y., Liang, J., Yue, J., Xu, C., Lu, L., Xu, Z., Gao, J., Du, Y., & Chen, Z.
- Affiliations
- Zhejiang University (CN)
- Corresponding author
- Du, Yongzhong
- Chen, Zhong
- Venue
- Angewandte Chemie International Edition
- Publisher
- Wiley
- Published
- 2014-07-18
- Volume
- 53
- Issue
- 46
- Pages
- 12436-12440
- ISSN
- 1433-7851 (ISSN-L)
- 1521-3773
- OpenAlex
- W2117643610
- Cited by
- 143
- References
- 1
- Citations by year
- 2026: 3 · 2025: 6 · 2024: 16 · 2023: 11 · 2022: 15 · 2021: 17 · 2020: 11 · 2019: 16 · 2018: 19 · 2017: 5 · 2016: 16 · 2015: 8
- FWCI
- 3.66
- Type
- journal article
- Language
- en
- Open access
- closed
- Locations
- Angewandte Chemie International Edition (publishedVersion)
- PubMed (publishedVersion)
- Topics
- Physical Sciences › Materials Science › Biomaterials › Nanoparticle-Based Drug Delivery
- Life Sciences › Pharmacology, Toxicology and Pharmaceutics › Pharmaceutical Science › Advanced Drug Delivery Systems
- Health Sciences › Medicine › Psychiatry and Mental health › Epilepsy research and treatment
- Keywords
- Angiopep-2, epilepsy, phenytoin sodium, blood-brain barrier penetration, amygdala kindling, epileptiform discharges
- MeSH terms
- Amygdala, Animals, Anticonvulsants, Blood-Brain Barrier, Cell Line, Electricity, Epilepsy, Humans, Peptides, Phenytoin, Drug Delivery Systems, Hydrogel, Polyethylene Glycol Dimethacrylate, Mice, Nanoparticles
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