Design of lactoferrin modified lipid nano-carriers for efficient brain-targeted delivery of nimodipine

摘要

Blood-brain barrier (BBB) was the major obstacle for efficient delivery of therapeutic agents to brain tissue. To overcome this barrier, a novel lactoferrin modified long circulation nanostructured lipid carriers (Lf-NLC) was designed and synthesized for the efficient delivery of neuroprotective agent nimodipine (NMD) to brain tissue. NMD loaded Lf-NLC was optimized to exhibit a small and uniform particle size distribution and high loading content. More interestingly, Lf-NLC showed the excellent neuroprotective effect due to the efficient intracellular delivery NMD, in PC12 based stroke cell model induced by sodium nitroprusside (SNP). Cellular uptake assay indicated that Lf-NLC could be internalized into cytoplasmviaLf-receptor mediated endocytosis pathway.In vivobiodistribution assay demonstrated Lf-NLC could efficiently deliver therapeutic agent to brain tissue, indicating its promising application in brain delivery.