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Adsorption properties, the pH-sensitive release of 5-fluorouracil and cytotoxicity studies of mesoporous silica drug delivery matrix 

Abstract : Mesoporous silica materials were investigated as the carriers for pH-sensitive drug delivery systems. Porous silica SBA-15 was first functionalized by anchoring N-[3-(trimethoxysilyl) propyl] aniline groups on the surface. After loading of an antineoplastic agent 5-fluorouracil, the pores were capped by β-cyclodextrin molecules. The studied samples were characterized by N 2 adsorption/desorption measurements, thermal analysis, powder X-Ray Diffraction, and Transmission Electron Microscopy. Adsorption properties of 5-fluorouracil were explored via the construction of adsorption isotherms. The amount of 5-FU adsorbed on amine-functionalized SBA-15 was 60 mg per 1 g of solid. The adsorption of 5-fluorouracil on silica was also monitored by microcalorimetry, showing low adsorption enthalpies. Drug release properties from matrices were studied using UV-Visible spectroscopy with the un-blocked and blocked pores configuration to demonstrate the efficiency of the pH-responsive nanovalves and evaluated using different kinetic models. It was shown that no drug release occurred at neutral pH and that more than 80% of drug adsorbed amount was released at pH = 5. Working at the equilibrium, the initial burst of the drug from the silica surface, usually observed in other porous silica drug delivery systems, was avoided. The interaction between the β-cyclodextrin molecules and grafted amine functions were also studied as a function of pH. Finally, the cytotoxicity tests were performed using human glioma U87 MG cells.
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https://hal-amu.archives-ouvertes.fr/hal-02295579
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Submitted on : Thursday, February 25, 2021 - 3:42:17 PM
Last modification on : Saturday, February 27, 2021 - 3:25:57 AM
Long-term archiving on: : Wednesday, May 26, 2021 - 6:57:43 PM

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Eva Beňová, David Bergé-Lefranc, Vladimír Zeleňák, Miroslav Almáši, Veronika Huntosova, et al.. Adsorption properties, the pH-sensitive release of 5-fluorouracil and cytotoxicity studies of mesoporous silica drug delivery matrix . Applied Surface Science, Elsevier, In press, 504, pp.144028. ⟨10.1016/j.apsusc.2019.144028⟩. ⟨hal-02295579⟩

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