SN-38 active loading in poly(lactic-co-glycolic acid) nanoparticles and assessment of their anticancer properties on COLO-205 human colon adenocarcinoma cells

Abstract

SN-38 is a highly effective drug against many cancers. The development of an optimal delivery system for SN-38 is extremely challenging due to its low solubility and labile lactone ring. Herein, SN-38 encapsulated in poly(d,l-lactide-co-glycolide) nanoparticles (NPs) is introduced to enhance its solubility, stability and cellular uptake. SN-38-loaded NPs prepared by spontaneous emulsification solvent diffusion (SESD) method had an average diameter of 310 nm, a zeta potential of −9.69 mV and a loading efficiency of 71%. They were able to protect the active lactone ring of SN-38 against inactivation under physiological condition. A colorectal adenocarcinoma cell line (COLO-205) was used to assess the NPs effects on cytotoxicity and cellular uptake. Result showed a significant decreased cell proliferation and cell apoptosis. These results suggest that these SN-38-loaded NPs can be an effective delivery system for the treatment of colon cancer and potentially for other types of cancers.

• Apoptosis
• cellular uptake
• colorectal adenocarcinomacancer cell
• PLGA nanoparticles
• SN-38 anticancer drug
• SN-38 delivery system
• SN-38 solubility and stability
• spontaneous emulsification solvent diffusion

Acknowledgments

The authors would like to thank Line Mongeon for her assistance with TEM.

Declaration of interest

The research was supported by the Fonds Québécois de Recherche en Science et en Génie-MITACS scholarship, Consortium québécois sur la découverte du medicament and the Natural Sciences and Engineering Research Council of Canada (NSERC).