Nanohydroxyapatite-Mediated Imatinib Delivery for Specific Anticancer Applications

Molecules. 2020 Oct 9;25(20):4602. doi: 10.3390/molecules25204602.

Abstract

In the present study, a nanoapatite-mediated delivery system for imatinib has been proposed. Nanohydroxyapatite (nHAp) was obtained by co-precipitation method, and its physicochemical properties in combination with imatinib (IM) were studied by means of XRPD (X-ray Powder Diffraction), SEM-EDS (Scanning Electron Microscopy-Energy Dispersive X-ray Spectroscopy), FT-IR (Fourier-Transform Infrared Spectroscopy), absorption spectroscopy as well as DLS (Dynamic Light Scattering) techniques. The obtained hydroxyapatite was defined as nanosized rod-shaped particles with high crystallinity. The amorphous imatinib was obtained by conversion of its crystalline form. The beneficial effects of amorphous pharmaceutical agents have been manifested in the higher dissolution rate in body fluids improving their bioavailability. Imatinib-to-hydroxyapatite interactions on the surface were confirmed by SEM images as well as absorption and FT-IR spectroscopy. The cytotoxicity of the system was tested on NI-1, L929, and D17 cell lines. The effectiveness of imatinib was not affected by nHAp modification. The calculated IC50 values for drug-modified nHAp were similar to those for the drug itself. However, higher cytotoxicity was observed at higher concentrations of imatinib, in comparison with the drug alone.

Keywords: anticancer targeted therapies; cytotoxicity; imatinib; nanohydroxyapatite.

MeSH terms

  • Antineoplastic Agents / chemistry
  • Antineoplastic Agents / pharmacology
  • Cell Line, Tumor
  • Cell Survival / drug effects
  • Durapatite / chemistry*
  • Dynamic Light Scattering
  • Humans
  • Imatinib Mesylate / chemistry*
  • Microscopy, Atomic Force
  • Spectrometry, X-Ray Emission
  • Spectroscopy, Fourier Transform Infrared

Substances

  • Antineoplastic Agents
  • Imatinib Mesylate
  • Durapatite