Potentiation of 5-fluorouracil encapsulated in zeolites as drug delivery systems for in vitro models of colorectal carcinoma

作者: Natália Vilaça , Ricardo Amorim , Ana F. Machado , Pier Parpot , Manuel F.R. Pereira

DOI: 10.1016/J.COLSURFB.2013.07.042

关键词:

摘要: The studies of potentiation 5-fluorouracil (5-FU), a traditional drug used in the treatment several cancers, including colorectal (CRC), were carried out with zeolites Faujasite sodium form, different particle sizes (NaY, 700nm and nanoNaY, 150nm) Linde type L potassium form (LTL) size 80nm. 5-FU was loaded into by liquid-phase adsorption. Characterization spectroscopic techniques (FTIR, (1)H NMR (13)C (27)Al solid-state MAS NMR), chemical analysis, thermal analysis (TGA), nitrogen adsorption isotherms scanning electron microscopy (SEM), demonstrated successful loading zeolite hosts. In vitro release (PBS buffer pH 7.4, 37°C) revealed 80-90% first 10min. To ascertain kinetics, profiles fitted to zero-order, first-order, Higuchi, Hixson-Crowell, Korsmeyer-Peppas Weibull kinetic models. dissolution from delivery systems (DDS) explained model. DDS efficacy evaluated using two human carcinoma cell lines, HCT-15 RKO. Unloaded presented no toxicity both cancer cells, while all allowed an important effect on viability. Immunofluorescence provided evidence for zeolite-cell internalization.

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