Immune cell uptake of glycinated nanoparticles conjugated to anti-fibrotic peptides enables their prolonged activity and oral administration

Abstract

Background: Fibrosis is a hallmark of various chronic diseases, for which there is no effective cure. Whilst the recombinant form of the human peptide hormone, relaxin (RLX), is being clinically evaluated for its cardioprotective including anti-fibrotic effects in heart failure patients, this is as an injectable which is invasive. This study therefore used biodegradable nanoparticles as a delivery platform to facilitate the prolonged activity and oral application of RLX and a related mimetic as therapeutics. Methods: RLX was conjugated to glycine-functionalised biodegradable superparamagnetic iron oxide nanoparticles (SPION-RLX), enabling therapeutic levels of RLX to be systemically or orall..