Folate-linked lipid-based nanoparticles deliver a NFκB decoy into activated murine macrophage-like RAW264.7 cells

Activated macrophages are the key effector cells in rheumatoid arthritis (RA) and secrete multiple mediators of inflammation including proinflammatory cytokines. We investigated delivery of a nuclear factor kappa B (NF kappa B) decoy by folate-linked lipid-based nanoparticles (NP-F) into murine macrophages. The expression of folate receptor (FR) in RAW264.7 cells activated by lipopolysaccaride was confirmed by strong expression of FR mRNA, and association of FITC-labeled folate-BSA conjugate. When transfected via NP-F, the NF kappa B decoy was strongly detected in the cytoplasm, and an inhibitory effect on the translocation of NF kappa B into the nucleus was observed at 0.03 mu m of the decoy, suggesting that NP-F effectively delivered the NF kappa B decoy into the cytoplasm. This information is of value for the design of NF kappa B decoy carrier systems targeting FR in activated macrophages in gene therapy for autoimmune diseases such as RA.