caffeine-loaded poly lactic co-glycolic acid nanoparticles for treatment of triple negative breast cancer

Caffeine is a methylxanthine alkaloid commonly found in beverages like coffee and tea, as well as in pharmaceutical formulations. current evidence indicates that caffeine possesses multiple bioactive properties, such as neuroprotection, antioxidative and anti-inflammatory actions, performance enhancement, and possible antitumor activity. however, its therapeutic efficacy is limited by rapid metabolism, short half-life, and variable bioavailability. to overcome these challenges, caffeine was incorporated into poly(lactic-co-glycolic acid) (plga) nanoparticles to enhance its stability and enable sustained drug release, optimizing its therapeutic effectiveness. this study focused on encapsulating caffeine in plga nanoparticles to improve its physicochemical characteristics, followed by an assessment of its anticancer potential against 4t1 murine breast cancer cells. poly (d, l-lactide-co-glycolide) (plga) nanoparticles (nps) containing caffeine were prepared using a double-emulsion solvent evaporation technique, and then surface morphology and size distribution were assessed by scanning electron microscopy (fesem), and also encapsulation efficiency was measured. to investigate the anticancer effects of caffeine and caffeine nanoparticles, 4t1 cancer cells were treated with various concentrations (25, 50, 100, and 200 µm) of each compound. cell viability was assessed using the mtt assay. the growth rate and morphological changes were observed with an inverted light microscope. after treating the cells with the ic50 concentration of the compounds and incubating them for 48 hours, they were examined at 400x magnification, and images were captured. 75±3.7 nm of average diameters and uniform morphology of the particles were confirmed by fesem, and the encapsulation efficiency was 83.4 %±1.2. the results of the mtt assay demonstrated a notably higher cytotoxic effect of the caffeine-loaded nanoparticles on 4t1 cells than the free caffeine. so that the ic50 concentration of free caffeine was 103 µm, and the ic50 concentration of nano caffeine was 33 µm. in morphological analysis, the results showed that caffeine nanoparticles killed more cancer cells than free caffeine, and the remaining cells also underwent apoptosis. notably, the caffeine nanoparticles exhibited significantly stronger anticancer effects on mouse mammary cancer cell line compared to free caffeine. further studies in mouse models are needed to confirm the results.