Preparation and bioassay explore of methotrexatum/zinc-aluminum layered double hydroxides

Abstract

Methotrexatum/zinc-aluminum layered double hydroxides(MTX/Zn-Al-LDHs) compounds were prepared by the improved coprecipitation method in the alcohol-aqueous mixed solvent. The influence of molar ratios of Zn2+/Al3+/MTX(R value) on the structure and morphologies of the compounds was systematically studied. The MTX/LDHs compounds were characterized by X-ray diffraction(XRD), fourier transform infrared spectroscopy(FT-IR), transmission electron microscope(TEM), scanning electron microscope(SEM), atomic force microscope(AFM) and UV-visible diffuse spectroscopy(UV-Vis). The results indicate that the particles display curly sheet form with a little agglomeration, for the crystallite nucleation and growth along the a-b axes are more favorable than c axe, and the size of particles decreases with increasing the content of MTX. Then in vitro release behavior of the drugs from LDHs in pH 7.4 phosphate buffered saline(PBS) was observed, and two kinetics models(modified Freundlich model and parabolic diffusion model) were chosen to simulate the release kinetics of the drugs from LDHs. The release process involved two stages: firstly surface diffusion and secondly intraparticle diffusion. Moreover, the anticancer efficacy of both MTX and MTX/LDHs compounds were also estimated in vitro by the bioassay such as MTT assay with the human lung cancers(A549). According to the cell-line tests, LDHs itself does not exhibit obvious cytotoxicity within the studied concentration, and the anticancer efficacy tests for the MTX/LDHs compounds turn out to be more effective in cell suppression compared to the MTX itself, and the smaller the particle size is, the better anticancer efficacy could be.