Teucrium polium extract-loaded solid lipid nanoparticles: A design and in vitro anticancer study.

Abstract

Teucrium polium extract (TPE) is a natural product with potent anticancer activity because of its terpenoid and flavonoid content. The aim of this study was to synthesize solid lipid nanoparticles (SLN) containing T. polium extract (TPE-SLNs) and to evaluate its anti-cancer effect. Formulations of TPE-SLNs were prepared using high-shear homogenization followed by the ultra-sonication technique. Then the TPE-SLNs were characterized by dynamic light scattering (DLS), Zetasizer and field-emission scanning electron microscopy (FESEM), and Fourier transform infrared spectroscopy methods. After confirming the presence of nanoparticles, its anti-proliferative activity was evaluated on Ntra-2 cancer cells and compared to human foreskin fibroblasts (HFF) as a normal cell line by MTT (3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide) assay. The pro-apoptotic (flow cytometry) and quantitative PCR (qPCR) and anti-angiogenic (chick chorioallantoic membrane (CAM)) and anti-inflammatory (qPCR) effects of TPE-SLNs were assessed by various methods. TPE-SLNs (85.5nm, PDI: 0.39, and zeta potential: -25.5 mv) were inhibited by the proliferation of Ntra-2 cancer cells with half-maximal inhibitory concentration (IC50 ; 106.58µg/ml). Moreover, by increasing the expression of caspase-3,9 and decreasing the expression of interleukin 6 (IL-6), IL-1b, and Bcl-2 genes, apoptosis and anti-inflammatory effects were observed. Reduction of angiogenesis was observed by the reduction of genes involved in angiogenesis and reduction of vascular and embryonic factors in the CAM assay. Activation of various mechanisms of inhibiting cancer cells in the treatment of nanoparticles was demonstrated in the present study. Therefore, these nanoparticles can be recommended for therapeutic purposes. PRACTICAL APPLICATIONS: Solid lipid nanoparticles (SLNs) are composed of pure solid fats and have been researched for many applications. Advantages such as high safety, low toxicity, control of drug release, and increase in chemical stability of loaded drugs distinguish these systems from other colloidal systems. According to the results of this study, solid lipid nanoparticles (SLN) containing T. polium extract showed their anti-cancer effects through various strategies such as inhibiting angiogenesis, inhibiting inflammation, and inducing apoptosis on Ntra-2 cells. These results make it possible to apply these nanocarriers in the loading and transport of drugs to treat various diseases such as cancer.