Development of amine-functionalized porous organosilica nanoparticles as pH-responsive drug delivery system

This study presents the synthesis and characterization of amine-functionalized biodegradable periodic mesoporous organosilica (BPMO-NH2) as a promising drug delivery nano-system for 5-fluorouracil (5-FU). The aim of this work is to enhance the drug loading capacity and achieve controlled and pH-responsive release. The successful amino-functionalization was confirmed by Fourier-transform infrared spectroscopy (FTIR) and zeta potential measurements. The morphology and porosity of nanoparticles were characterized via scanning electron microscope (SEM) and N2 isotherm sorption. The drug, 5-FU, a water-soluble pyrimidine analogue anticancer drug, was efficiently loaded onto the BPMO-NH2 nanoparticles. Results of the loading and release investigation revealed that BPMO-NH2 exhibited significantly higher loading capacity in comparison to the original nanoparticles, with a gradual and pH-responsive release profile observed at the acidic extracellular pH characteristic of cancer cells. Furthermore, the cytotoxicity studies on L929 fibroblast and MCF7 breast cancer cells also demonstrated efficient cellular uptake, negligible cytotoxicity of pristine BPMO-NH2, and enhanced cytotoxicity towards cancer cells upon encapsulation of 5-FU. Overall, these promising results highlight the potential of BPMO-NH2 as a pH-responsive and slow-release nanocarrier, holding great promise for efficient drug delivery applications in cancer therapy.