8-Hydroxyquinoline platinum( ii ) loaded nanostructured lipid carriers: synthesis, physicochemical characterization and evaluation of antitumor activity

BOZTEPE, T.; SCIOLI-MONTOTO, S.; RUIZ, M. E.; ALVAREZ, V. A.; CASTRO, G. R.; LEÓN, I. E.

NEW JOURNAL OF CHEMISTRY

ROYAL SOC CHEMISTRY

Lugar: CAMBRIDGE; Año: 2020

1144-0546

The incidence of cancer and the death rate increases every year in the world. The drug 8-hydroxyquinoline platinum(II) [PtCl(8-O-quinoline)(dmso)] (8HQ-Pt) has been identified as a promising antitumor complex. Nanostructured lipid carriers (NLC) are the second-generation drug nanocarrier systems that present superior advantages over other kinds of colloidalcarrier systems. 8HQ-Pt compound loaded NLC formulations of cetyl esters (SS) were synthesized by ultrasonication in presence of two different liquid oils; capric triglyceride, or olive oil. The physicochemical and microscopic characterizations of NLC were analyzed by dynamic light scattering (DLS), transmission electron microscopy (TEM), fourier transformed infrared spectroscopy (FTIR), thermogravimetric analysis (TGA), differential scanning calorimetry (DSC) and X-ray diffraction analysis (XRD). In vitro drug release and cytotoxicity, cell uptake and apoptosis assays against the human colon cancer HT - 29 were investigated. The results showed that NLCs indicated a narrow size distribution in the range of 136-159 nm mean particle diameter. The thermal characteristics analysis confirmed the stability of NLCs up to 185 °C. Encapsulation efficienciesof the 8HQ-Pt compound in NLCs were about 80% and 8HQ-Pt compound in the formulations showed controlled release profile during 72 h. The release profile of these two different formulations and the antitumor effect on HT-29 cell line were compared with the free 8HQ-Pt compound. The cellular uptake of two different NLC groups was proved by fluorescencemicroscopy and the presence of capric triglyceride liquid oil in the formulation increased the capacity of drug delivery to intracellularly when compared with olive oil.