Synthesis, characterization of catechin-loaded folate-conjugated chitosan nanoparticles and their anti-proliferative effect

Abstract

Catechin-loaded folate-conjugated chitosan nanoparticles (CFC-NPs) were synthesized through ionic gelation reactions between folate-modified chitosan and sodium tripolyphosphate. Their chemical structures, size distribution and morphology, drug loading capacity and entrapment efficiency, in vitro release behavior, and anti-proliferative effects were investigated. Results showed that CFC-NPs dispersed as a near-spherical shape with an average diameter of 255 nm. Drug loading capacity and entrapment efficiency reached 8.66–11.53% and 19.02–43.28%, respectively. Meanwhile, the loaded catechin exhibited a sustainable release from the nanoparticles, with the cumulative release ratio being 75.20% over 36 h. Blank folate-conjugated chitosan nanoparticles (FC-NPs) at 0.5 mg/mL had little or no cytotoxicity toward MCF-7 and HepG2 cells, while CFC-NPs had significant anti-proliferative activity in a dose-dependent manner. After incubation for 36 h, cell viability reached 35.22 ± 3.42% and 58.44 ± 3.85% in MCF-7 and HepG2 cells, respectively. These results suggest that CFC-NPs might be effective carrier of catechins with antitumor activity.