Tripodal amphiphilic pseudopeptidic nanovesicles as p-coumaric acid delivery systems for brain cancer cells
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https://doi.org/10.1016/j.mtchem.2022.101266 |
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Title
Tripodal amphiphilic pseudopeptidic nanovesicles as p-coumaric acid delivery systems for brain cancer cellsAuthor (s)
Date
2022-11Publisher
ElsevierBibliographic citation
LOTFALLAH, A. H., et al. Tripodal amphiphilic pseudopeptidic nanovesicles as p-coumaric acid delivery systems for brain cancer cells. Materials Today Chemistry, 2023, vol. 27, p. 101266.Type
info:eu-repo/semantics/articlePublisher version
https://www.sciencedirect.com/science/article/pii/S2468519422004955Version
info:eu-repo/semantics/publishedVersionSubject
Abstract
Nanovesicles based on tripodal amphiphilic pseudopeptides are prepared as carriers for p-coumaric acid
(p-CA) delivery. Loaded nanovesicles are obtained by both thin film hydration and ethanol injection
methods with ... [+]
Nanovesicles based on tripodal amphiphilic pseudopeptides are prepared as carriers for p-coumaric acid
(p-CA) delivery. Loaded nanovesicles are obtained by both thin film hydration and ethanol injection
methods with positive Z-potential values. The last technique renders lower particle sizes and excellent
polydispersity index, with average values of 130 nm and 0.123, respectively, although the drug loading
obtained after ultracentrifugation is lower. In vitro release experiments, including the use of different
external stimuli such as pH and proteolytic enzymes, provide interesting results. The prepared nanovesicles are tested on normal cells (VERO), displaying a high safety profile scoring with a 50% inhibitory
concentration (IC50) of 1,822 mg/mL. A 40-times increase in the in vitro cytotoxic effect of p-CA on Glioma
GL261 brain cancer cells, from IC50 1,082 mg/mL to 29 mg/mL, is observed using the loaded pseudopeptide
nanovesicles. 1
H NMR studies reveal that the drug is mainly located inside the nanoparticle bilayer.
Transmembrane carboxyfluorescein studies reveal that the amphiphilic compound does not provide a
significant membrane fluidification. Experimental data suggest that the observed biological activity can
be associated to an enhanced permeability and retention effect. The present results highlight the potential of such nanovesicles as potent p-CA carriers for brain cancer therapy. [-]
Is part of
Materials Today Chemistry, 2023, vol. 27.Funder Name
Universitat Jaume I | Generalitat Valenciana | Ministerio de Ciencia e Innovación | European Regional Development Fund
Project code
UJI-B2021-31 | AICO/2021/139 | MCIN/AEI/10.13039/501100011033 | PDI2021-124695OB-C22
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2468-5194/© 2022 Elsevier Ltd. All rights reserved.
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