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The Synthesis and Characterization of a Delivery System Based on Polymersomes and a Xanthone with Inhibitory Activity in Glioblastoma

Title
The Synthesis and Characterization of a Delivery System Based on Polymersomes and a Xanthone with Inhibitory Activity in Glioblastoma
Type
Article in International Scientific Journal
Year
2024
Authors
Alves, A
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Silva, AM
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Nunes, C
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Cravo, S
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Salette Reis
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Pinto, M
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Emilia Sousa
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Rodrigues, F
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Ferreira, D
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Paulo Costa
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Marta Correia da Silva
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Journal
Title: LIFE-BASELImported from Authenticus Search for Journal Publications
Vol. 14
Final page: 132
ISSN: 2075-1729
Publisher: MDPI
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Publicação em ISI Web of Knowledge ISI Web of Knowledge - 0 Citations
Publicação em Scopus Scopus - 0 Citations
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Authenticus ID: P-00Z-YPJ
Abstract (EN): Glioblastoma (GBM) is the most common and deadly primary malignant brain tumor. Current therapies are insufficient, and survival for individuals diagnosed with GBM is limited to a few months. New GBM treatments are urgent. Polymeric nanoparticles (PNs) can increase the circulation time of a drug in the brain capillaries. Polymersomes (PMs) are PNs that have been described as having attractive characteristics, mainly due to their stability, prolonged circulation period, biodegradability, their ability to sustain the release of drugs, and the possibility of surface functionalization. In this work, a poly(ethylene glycol)-epsilon-caprolactone (PEG-PCL) copolymer was synthesized and PMs were prepared and loaded with an hydrolytic instable compound, previously synthesized by our research team, the 3,6-bis(2,3,4,6-tetra-O-acetyl-beta-glucopyranosyl)xanthone (XGAc), with promising cytotoxicity on glioblastoma cells (U-373 MG) but also on healthy cerebral endothelial cells (hCMEC/D3). The prepared PMs were spherical particles with uniform morphology and similar sizes (mean diameter of 200 nm) and were stable in aqueous suspension. The encapsulation of XGAc in PMs (80% encapsulation efficacy) protected the healthy endothelial cells from the cytotoxic effects of this compound, while maintaining cytotoxicity for the glioblastoma cell line U-373 MG. Our studies also showed that the prepared PMs can efficiently release XGAc at intratumoral pHs.
Language: English
Type (Professor's evaluation): Scientific
No. of pages: 17
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