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

Abstract

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 (NFκB) 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 NFκB decoy was strongly detected in the cytoplasm, and an inhibitory effect on the translocation of NFκB into the nucleus was observed at 0.03 μM of the decoy, suggesting that NP-F effectively delivered the NFκB decoy into the cytoplasm. This information is of value for the design of NFκB decoy carrier systems targeting FR in activated macrophages in gene therapy for autoimmune diseases such as RA. © 2006 Pharmaceutical Society of Japan.