Potentiation of 5-fluorouracil encapsulated in zeolites as drug delivery systems for in vitro models of colorectal carcinoma
authors Vilaca, N; Amorim, R; Machado, AF; Parpot, P; Pereira, MFR; Sardo, M; Rocha, J; Fonseca, AM; Neves, IC; Baltazar, F
nationality International
journal COLLOIDS AND SURFACES B-BIOINTERFACES
author keywords Zeolites; 5-Fluorouracil (5-FU); Encapsulation; Drug delivery; Cytotoxicity; Potentiation
keywords SYNTHETIC ZEOLITES; CANCER; RELEASE; NANOPARTICLES; CAPECITABINE; FLUOROURACIL; RELAXIVITY; THERAPY; HY
abstract The studies of potentiation of 5-fluorouracil (5-FU), a traditional drug used in the treatment of several cancers, including colorectal (CRC), were carried out with zeolites Faujasite in the sodium form, with different particle sizes (NaY, 700 nm and nanoNaY, 150 nm) and Linde type L in the potassium form (LTL) with a particle size of 80 nm. 5-FU was loaded into zeolites by liquid-phase adsorption. Characterization by spectroscopic techniques (FTIR, H-1 NMR and C-13 and Al-27 solid-state MAS NMR), chemical analysis, thermal analysis (TGA), nitrogen adsorption isotherms and scanning electron microscopy (SEM), demonstrated the successful loading of 5-FU into the zeolite hosts. In vitro drug release studies (PBS buffer pH 7.4, 37 degrees C) revealed the release of 80-90% of 5-FU in the first 10 min. To ascertain the drug release kinetics, the release profiles were fitted to zero-order, first-order, Higuchi, Hixson-Crowell, Korsmeyer-Peppas and Weibull kinetic models. The in vitro dissolution from the drug delivery systems (DDS) was explained by the Weibull model. The DDS efficacy was evaluated using two human colorectal carcinoma cell lines, HCT-15 and RKO. Unloaded zeolites presented no toxicity to both cancer cells, while all DDS allowed an important potentiation of the 5-FU effect on the cell viability. Immunofluorescence studies provided evidence for zeolite-cell internalization. (C) 2013 Elsevier B.V. All rights reserved.
publisher ELSEVIER SCIENCE BV
issn 0927-7765
year published 2013
volume 112
beginning page 237
ending page 244
digital object identifier (doi) 10.1016/j.colsurfb.2013.07.042
web of science category Biophysics; Chemistry, Physical; Materials Science, Biomaterials
subject category Biophysics; Chemistry; Materials Science
unique article identifier WOS:000328593100034
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journal impact factor 3.997
5 year journal impact factor 4.294
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