Design and characterization of a novel amphiphilic chitosan nanocapsule-based thermo-gelling biogel with sustained in vivo release of the hydrophilic anti-epilepsy drug ethosuximide.
Abstract
Thermo-gelling injectable nanogels, with no burst release of loaded drug, were prepared by a simple route by combining self assembled nanocapsules of amphiphilically modified chitosan with glycerophosphate di-sodium salt and glycerol. The potential as a depot drug delivery system was demonstrated in vivo through the therapeutic effect of ethosuximide (ESM) loaded nanogels, suppressing spike wave discharges (SWDs) in Long Evan rat model. Simultaneously clearance of gels from the site of administration was monitored non-invasively using MRI. The gel structure was characterized using TEM and SEM, confirming the gels to be an assembly of nanocapsules and using two-photon microscopy to visualize the network structure. In vitro drug release studies using ESM revealed that the nanogels exhibited extended, mostly Fickian release. Finally, all investigated formulations displayed excellent cytotoxicity data determined by MTT assay using human retinal pigmented epithelium cells. All presented properties are highly desirable for injectable depot gels for drug delivery.
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Subcutaneous administration of ethosuximide loaded chitosan nanocapsules decreases spike wave discharge in a rat model.
“it was found that the subcutaneous administration of the ethosuximide loaded chitosan nanocapsules decrease the spike wave discharge”
From Nanotechnology: A Promising Approach for Delivery of Neuroprotective Drugs (2020) · cites this paper as Hsiao et al., 2012
Because of their ability to provide stable release of the drug, nano-formulations can be fabricated as depot drug delivery systems for long-term use of antiepileptic drugs.
“Because of their ability to provide stable release of the drug, these nano-formulations can be fabricated as depot drug delivery systems for long-term use of antiepileptic drugs”
From Nanotechnology: A Promising Approach for Delivery of Neuroprotective Drugs (2020) · cites this paper as Hsiao et al., 2012
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Nanotechnology: A Promising Approach for Delivery of Neuroprotective Drugs
Naqvi, S., Panghal, A., & Flora, S. J. S. (2020) · Frontiers in Neuroscience · doi:10.3389/fnins.2020.00494 · Cited by 305 · see citing works
- Authors
- Hsiao, M.-H., Larsson, M., Larsson, A., Evenbratt, H., Chen, Y.-Y., Chen, Y.-Y., & Liu, D.-M.
- Affiliations
- National Yang Ming Chiao Tung University (TW)
- Chalmers University of Technology (SE)
- University of Southern California (US)
- Corresponding author
- Liu, Dean-Mo
- Venue
- Journal of Controlled Release
- Publisher
- Elsevier BV
- Published
- 2012-08
- Volume
- 161
- Issue
- 3
- Pages
- 942-948
- ISSN
- 0168-3659 (ISSN-L)
- OpenAlex
- W2071993278
- Cited by
- 104
- References
- 34
- Citations by year
- 2026: 1 · 2025: 6 · 2024: 4 · 2023: 9 · 2022: 9 · 2021: 6 · 2020: 12 · 2019: 3 · 2018: 8 · 2017: 7 · 2016: 12 · 2015: 12 · 2014: 9 · 2013: 4 · 2012: 1
- FWCI
- 5.15
- Type
- journal article
- Language
- en
- Open access
- closed
- Licence
- Locations
- Journal of Controlled Release (publishedVersion)
- PubMed (publishedVersion)
- Adelaide Research & Scholarship (AR&S) (University of Adelaide) (submittedVersion)
- UCL Discovery (University College London) (submittedVersion)
- Chalmers Publication Library (Chalmers University of Technology) (submittedVersion)
- Chalmers Research (Chalmers University of Technology) (submittedVersion)
- Topics
- Life Sciences › Pharmacology, Toxicology and Pharmaceutics › Pharmaceutical Science › Advanced Drug Delivery Systems
- Life Sciences › Biochemistry, Genetics and Molecular Biology › Molecular Medicine › Hydrogels: synthesis, properties, applications
- Physical Sciences › Materials Science › Biomaterials › Supramolecular Self-Assembly in Materials
- Keywords
- chitosan nanocapsules, ethosuximide, sustained drug release, glycerophosphate, spike-wave discharges, epilepsy, cytotoxicity, Fickian release, two-photon microscopy
- MeSH terms
- Animals, Anticonvulsants, Cell Line, Cell Survival, Delayed-Action Preparations, Drug Carriers, Ethosuximide, Gels, Humans, Seizures, Rats, Long-Evans, Chitosan, Rats, Nanocapsules, Hydrophobic and Hydrophilic Interactions
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