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

• Type: Article in International Scientific Journal
• Date: 2013

Authors

N. Vilaça (Author) Other; R. Amorim (Author) Other; A.F. Machado (Author) Other; P. Parpot (Author) Other; Manuel Fernando R Pereira (Author) FEUP; M. Sardo (Author) Other; J. Rocha (Author) Other; A.M. Fonseca (Author) Other; I.C. Neves (Author) Other; F. Baltazar (Author) Other

Journal

Title: Colloids and Surfaces B: Biointerfaces

Vol. 112

Pages: 237-244

ISSN: 0927-7765

Publisher: Elsevier

Indexing

ISI Web of Knowledge - 45 Citations

ISI Web of Science

Scopus - 63 Citations

Scientific classification

FOS: Engineering and technology > Chemical engineering

Other information

Authenticus ID: P-008-DF8

DOI: 10.1016/j.colsurfb.2013.07.042

Abstract (EN): 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.

Language: English

Type (Professor's evaluation): Scientific

No. of pages: 8