Nose-to-brain delivery of temozolomide-loaded PLGA nanoparticles functionalized with anti-EPHA3 for glioblastoma targeting
Open accessAbstract
Glioblastoma is the most common malignant brain tumor. Efficient delivery of drugs targeting glioblastomas remains a challenge. Ephrin type-A receptor 3 (EPHA3) tyrosine kinase antibody-modified polylactide-co-glycolide (PLGA) nanoparticles (NPs) were developed to target glioblastoma via nose-to-brain delivery. Anti-EPHA3-modified, TBE-loaded NPs were prepared using an emulsion-solvent evaporation method, showed a sustained in vitro release profile up to 48 h and a mean particle size of 145.9 ± 8.7 nm. The cellular uptake of anti-EPHA3-modified NPs by C6 cells was significantly enhanced compared to that of nontargeting NPs (p < .01). In vivo imaging and distribution studies on the glioma-bearing rats showed that anti-EPHA3-modified NPs exhibited high fluorescence intensity in the brain and effectively accumulated to glioma tissues, indicating the targeting effect of anti-EPHA3. Glioma-bearing rats treated with anti-EPHA3-modified NPs resulted in significantly higher tumor cell apoptosis (p < .01) than that observed with other formulations and prolonged the median survival time of glioma-bearing rats to 26 days, which was 1.37-fold longer than that of PLGA NPs. The above results indicated that anti-EPHA3-modified NPs may potentially serve as a nose-to-brain drug carrier for the treatment of glioblastoma.
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The uptake of anti-EPHA3 modified NPs in cells was significantly enhanced, and showed a higher distribution in the brain, indicating that anti-EPHA3 has a brain-targeting effect.
“The uptake of anti-EPHA3 modified NPs in cells was significantly enhanced, and showed a higher distribution in the brain, indicating that anti-EPHA3 has a brain-targeting effect.210”
From Smart nanoparticles for cancer therapy (2023) · cites this paper as [210]
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- Authors
- Chu, L., Wang, A., Ni, L., Yan, X., Song, Y., Zhao, M., Sun, K., Mu, H., Liu, S., Wu, Z., & Zhang, C.
- Affiliations
- Yantai University (CN)
- Luye Pharma (China) (CN)
- Corresponding author
- Wang, Aiping
- Sun, Kaoxiang
- Venue
- Drug Delivery
- Publisher
- Informa UK Limited
- Published
- 2018-01-01
- Volume
- 25
- Issue
- 1
- Pages
- 1634-1641
- ISSN
- 1071-7544 (ISSN-L)
- 1521-0464
- PMC
- PMC6127843
- OpenAlex
- W2889706401
- Cited by
- 127
- References
- 35
- Citations by year
- 2026: 5 · 2025: 16 · 2024: 20 · 2023: 14 · 2022: 25 · 2021: 27 · 2020: 10 · 2019: 10
- FWCI
- 3.81
- Type
- journal article
- Language
- en
- Open access
- gold
- doi.org
- Licence
- Locations
- Drug Delivery (publishedVersion, cc-by)
- Europe PMC (PubMed Central) (publishedVersion, cc-by)
- PubMed Central (publishedVersion, cc-by)
- PubMed (publishedVersion)
- DOAJ (DOAJ: Directory of Open Access Journals) (submittedVersion, cc-by-sa)
- ResearchSpace (University of Auckland) (submittedVersion, cc-by)
- Funders
- Natural Science Foundation of Shandong Province (LH076, HB58)
- 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 › Genetics › Glioma Diagnosis and Treatment
- Keywords
- glioblastoma, nose-to-brain delivery, temozolomide, PLGA nanoparticles, targeted drug delivery, brain tumor therapy, tumor cell apoptosis
- MeSH terms
- Temozolomide, Animals, Antibodies, Monoclonal, Antineoplastic Agents, Brain Neoplasms, Drug Carriers, Glioblastoma, Humans, Male, Polyglactin 910, Rats, Sprague-Dawley, Receptor Protein-Tyrosine Kinases, Receptor, EphA3, Cell Line, Tumor, Rats, Nanoparticles, Molecular Targeted Therapy
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