Novel capsaicin releasing system targeted protects ischemic brain from cardiac arrest

Abstract

Objectiveas a fatal cardiovascular emergency, cardiac arrest causes cerebral ischemic injury as a main complication. Recently, capsaicin has attracted great attention for its activating effect on TRPV1 as well as various organ protective effects especially in brain. However, the poor water-solubility and extremely short biological half-life of capsaicin largely impedes the clinical use of it. Blood-brain barrier (BBB) consist another great challenge of application of capsaicin in ischemic brain. Methodsin this study, we employed the mesoporous iron oxide nanoparticles (MIONs) for carriers to load capsaicin. The nanoparticles were further modified with polyethylene glycol (PEG) and lactoferrin (LF). Resultsa novel capsaicin releasing system was developed (Capsaicin-MIPL), with controlled and slow releasing manner and brain targeted ability. The novel system showed excellent biocompatibility. Fluorescent nanoparticles were found to be localized in mice brain areas, with increased capsaicin levels in brain tissues. The protective effects of Capsaicin-MIPL were both investigated in the in vitro hypoxic neuron models and the in vivo cardiac arrest models, and significant neuroprotective effects were observed. ConclusionThis study offers a practical tool for controlled release of capsaicin in vivo especially in brain, and provides a novel method for cerebral protection after cardiac arrest.