Docetaxel-loaded folate-modified TPGS-transfersomes for glioblastoma multiforme treatment
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Glioblastoma multiforme (GBM) is a first primary Central Nervous System tumor with high incidence and lethality. Its treatment is hampered by the difficulty to overcome the blood-brain barrier (BBB) and by the non-specificity of chemotherapeutics to tumor cells. This study was based on the development characterization and in vitro efficacy of folate-modified TPGS transfersomes containing docetaxel (TF-DTX-FA) to improve GBM treatment. TF-DTX-FA and unmodified transfersomes (TF-DTX) were prepared through thin-film hydration followed by extrusion technique and characterized by physicochemical and in vitro studies. All formulations showed low particles sizes (below 200 nm), polydispersity index below 0.2, negative zeta potential (between -16.75 to -12.45 mV) and high encapsulation efficiency (78.72 ± 1.29% and 75.62 ± 0.05% for TF-DTX and TF-DTX-FA, respectively). Furthermore, cytotoxicity assay of TF-DTX-FA showed the high capacity of the nanocarriers to reduce the viability of U-87 MG in both 2D and 3D culture models, when compared with DTX commercial formulation and TF-DTX. In vitro cellular uptake assay indicated the selectivity of transfersomes to tumoral cells when compared to normal cells, and the higher ability of TF-DTX-FA to be internalized into 2D U-87 MG in comparison with TF-DTX (72.10 and 62.90%, respectively, after 24 h). Moreover, TF-DTX-FA showed higher permeability into 3D U-87 MG spheroid than TF-DTX, suggesting the potential FA modulation to target treatment of GBM.
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Folate receptor is overexpressed on the surface of a variety of cancers including breast, kidney, colorectal, brain, and ovarian cancers.
“The folate receptor (FR) is overexpressed on the surface of a variety of cancers, including breast, kidney, colorectal, brain, and ovarian cancers.263–265”
From Smart nanoparticles for cancer therapy (2023) · cites this paper as [264]
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- Authors
- Luiz, M. T., Viegas, J. S. R., Abriata, J. P., Tofani, L. B., Vaidergorn, M. D. M., Emery, F. D. S., Chorilli, M., & Marchetti, J. M.
- Affiliations
- Universidade de São Paulo (BR)
- Universidade Estadual Paulista (Unesp) (BR)
- Corresponding author
- Marchetti, Juliana Maldonado
- ORCID
- Venue
- Materials Science and Engineering: C
- Publisher
- Elsevier BV
- Published
- 2021-05
- Volume
- 124
- Pages
- 112033
- ISSN
- 0928-4931 (ISSN-L)
- OpenAlex
- W3136454776
- Cited by
- 62
- References
- 56
- Citations by year
- 2026: 6 · 2025: 10 · 2024: 12 · 2023: 16 · 2022: 12 · 2021: 6
- FWCI
- 3.01
- Type
- journal article
- Language
- en
- Open access
- green
- hdl.handle.net
- Licence
- Locations
- Materials Science and Engineering C (publishedVersion)
- PubMed (publishedVersion)
- LA Referencia (Red Federada de Repositorios Institucionales de Publicaciones Científicas) (submittedVersion, other-oa)
- Funders
- Coordenação de Aperfeiçoamento de Pessoal de Nível Superior
- Topics
- Physical Sciences › Materials Science › Biomaterials › Nanoparticle-Based Drug Delivery
- Health Sciences › Medicine › Genetics › Glioma Diagnosis and Treatment
- Life Sciences › Pharmacology, Toxicology and Pharmaceutics › Pharmaceutical Science › Advanced Drug Delivery Systems
- Keywords
- glioblastoma, docetaxel, TPGS, blood-brain barrier, nanocarriers, drug delivery, U87 cells, cellular uptake, tumor spheroids, encapsulation efficiency, cytotoxicity
- MeSH terms
- Docetaxel, Antineoplastic Agents, Drug Carriers, Folic Acid, Glioblastoma, Humans, Vitamin E, Cell Line, Tumor, Nanoparticles
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