Abstract
This study focuses on the designing and characterization, and anticancer evaluation of chitosan-based nanoparticles (NPs) loaded (enriched) with a Biginelli hybrid compound (BH). NPs based on chitosan (CH) or chitosan oligosaccharide lactate (CHOL), are carefully designed to encapsulate a tetrahydropyrimidine derivative (BH) with already proven anticancer properties. The formulations were evaluated for their physicochemical properties, including particle size distribution and morphology, using techniques such as infrared spectroscopy, scanning electron microscopy, and X-ray diffraction. The cytotoxicity profiles were assessed on different cancer cell lines, showing a higher selectivity towards HeLa and A549 cells related to BH. BH-CH showed better cytotoxic profile related to BH-CHOL NPs. A cell cycle analysis revealed an accumulation of cells in the G2/M phase after a treatment with these NPs, indicating the ability to induce mitotic arrest in cancer cells. In summary, the results underscore the promising application of CH-based natural nanocarriers for the targeted delivery of Biginelli hybrids, showcasing a significant potential for further in vivo testing.