2, 3-Dimercaptosuccinic Acid-Modified Iron Oxide Clusters for Magnetic Resonance Imaging

Over the last decade, various magnetic nanomaterials have been developed as magnetic resonance imaging (MRI) contrast agents; the greatest challenges encountered for clinical application have been insufficient stability. In this paper, a lyophilization method for 2, 3-dimercaptosuccinic acid-modified iron oxide (γ-Fe2O3@DMSA) nanoparticles was developed to simultaneously overcome two disadvantages; these include insufficient stability and low-magnetic response. After lyophilization, the clusters of γ-Fe2O3@DMSA with the size of 156.7 ± 15.3 nm were formed, and the stability of the lyophilized powder (γ-Fe2O3@DMSA-LP) increased up to over 3 years. It was also found that rehydrated γ-Fe2O3@DMSA-LP could be ingested by RAW264.7 cells in very large quantities. Results of pharmacokinetics and biodistribution studies in vivo indicated that γ-Fe2O3@DMSA-LP is a promising liver-targeted material. Furthermore, it also exhibited higher MRI efficiency and longer imaging time in the liver than the well-known product Feridex®. Moreover, results of vascular irritation and long-term toxicity experiments demonstrated γ-Fe2O3@DMSA-LP could be a nontoxic, biocompatible contrast agent in vivo. Therefore, the proposed γ-Fe2O3@DMSA-LP can be used as a potential MRI contrast agent in clinic for hepatic diseases. © 2014 Wiley Periodicals, Inc. and the American Pharmacists Association.