Enhancement of the antitumor effect of cisplatin and ginsenoside Rg3 by encapsulation in polylactic-co-glycolic acid nanoparticles

Abstract

Purpose: To develop dual-loaded polylactic-co-glycolic acid (PLGA) nanoparticles (NPs) with two chemotherapeutic agents, i.e., cisplatin (DDP) and 20(R)-ginsenoside Rg3(Rg3), and to evaluate the drug release profiles and synergistic inhibitory effects of the nanoparticles on lung cancer A549 cells.Methods: The dual-laden PLGA NPs were synthesized using modified emulsion and solvent vaporization procedures. Drug loading (DL) and efficacy of co-encapsulation (EE) were determined with a modification of column elution technique. The cytotoxic and inhibitory effects of individual and combined drugs on A549 lung cancer cells were evaluated using MTT assay.Results: A sustained pattern of drug release was shown by PLGA/DDP, PLGA/Rg3, and PLGA/DDP+Rg3. The formulated PLGA and unbound drugs exerted dose- and time-reliant cytotoxic effects on A549 cells. At all concentrations tested, drugs encapsulated in PLGA nanoparticles were more effective in killing the cells than the free drugs (p < 0.05). In particular, PLGA/DDP + Rg3 formulation produced a synergistic inhibitory effect on the proliferation of A549 cells.Conclusion: Single- and dual-load PLGA groups display variabilities in profiles of drug release and in vitro cytotoxic effect. Furthermore, dual-load PLGA group produces significantly enhanced treatment effect. These results suggest that PLGA formulations hold great potential for future drug delivery.