Sialic acid-conjugated PLGA nanoparticles enhance the protective effect of lycopene in chemotherapeutic drug-induced kidney injury.

Lycopene (LYC) is known to protect cells from oxidative damage caused by free radicals in human tissues. In the present study, the authors designed a LYC-loaded sialic acid (SA)-conjugated poly(D,L-lactide-co-glycolide) (PLGA) nanoparticle (LYC-NP) to enhance the therapeutic efficacy of LYC in acute kidney injury. The characteristics of the LYC-NPs were defined according to particle size, morphology, and in vitro drug release. The LYC-NPs exhibited a controlled release of LYC over 48 h. Confocal laser scanning microscopy clearly highlighted the targeting potential of SA. Enhanced green fluorescence was observed for the LYC-NPs in H2O2-treated human umbilical vein endothelial cells, indicating enhanced internalisation of NPs. The LYC-NPs showed significantly greater cell viability than H2O2-treated cells. In addition, the LYC-NPs remarkably reduced proinflammatory cytokine levels, attributable mainly to the increased cellular internalisation of the SA-based carrier delivery system. Furthermore, protein levels of caspase-3 and -9 were significantly down-regulated after treatment with the LYC-NPs. Overall, they have demonstrated that SA-conjugated PLGA-NPs containing LYC could be used to treat kidney injury.