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Docetaxel-loaded folate-modified TPGS-transfersomes for glioblastoma multiforme treatment
Marcela Tavares Luiz1, Juliana Santos Rosa Viegas1, Juliana Palma Abriata1
1School of Pharmaceutical Science of Ribeirao Preto, University of Sao Paulo (USP), Ribeirao Preto, São Paulo, Brazil.
Abstract:
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.
Insights
This study developed folate-modified transfersomes carrying docetaxel to enhance glioblastoma treatment. These nanocarriers show improved tumor cell targeting and reduced viability in vitro, overcoming blood-brain barrier challenges.
Area of Science:
- Nanotechnology
- Drug Delivery
- Oncology
Background:
- Glioblastoma multiforme (GBM) is a lethal brain tumor with challenging treatment due to the blood-brain barrier (BBB) and non-specific chemotherapy.
- Overcoming the BBB and achieving targeted drug delivery are critical for effective GBM therapy.
Purpose of the Study:
- To develop and characterize folate-modified TPGS transfersomes loaded with docetaxel (TF-DTX-FA) for improved glioblastoma treatment.
- To evaluate the in vitro efficacy, cellular uptake, and BBB penetration of TF-DTX-FA.
Main Methods:
- TF-DTX-FA and TF-DTX were prepared using thin-film hydration and extrusion.
- Physicochemical characterization included particle size, polydispersity index, zeta potential, and encapsulation efficiency.
- In vitro efficacy was assessed using cytotoxicity assays on U-87 MG cells (2D and 3D models) and cellular uptake studies.
Main Results:
- Formulations exhibited small particle sizes (<200 nm), narrow PDI (<0.2), negative zeta potential, and high encapsulation efficiency (>75%).
- TF-DTX-FA demonstrated superior cytotoxicity against U-87 MG cells in both 2D and 3D cultures compared to docetaxel and unmodified transfersomes.
- TF-DTX-FA showed enhanced cellular uptake and greater permeability into 3D spheroids, indicating folate receptor-mediated targeting.
Conclusions:
- Folate-modified TPGS transfersomes (TF-DTX-FA) represent a promising nanocarrier system for targeted docetaxel delivery in glioblastoma.
- The folate modification enhances cellular uptake and penetration, suggesting potential for improved GBM therapy by overcoming BBB limitations.
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