Co‐Delivery of 131I and Prima‐1 by Self‐Assembled CD44‐Targeted Nanoparticles for Anaplastic Thyroid Carcinoma Theranostics

Abstract New radionuclide‐labeled targeting nanocarrier systems have generated new opportunities for tumor treatment and imaging. Nevertheless, such therapeutic strategy is clinically unfeasible on anaplastic thyroid carcinoma (ATC) patients, because of lacking suitable targets and resistance to radiation. In order to figure out a potential treatment, immuno‐histochemical staining is performed in human ATC tissue species and high expression of cluster determinant 44 (CD44) is found. Therefore, a CD44‐targeted delivery system is designed and constructed by self‐assembly of tyrosine (Tyr)–hyaluronic acid (HA)–polyethyleneimine (PEI), which can radiolabel 131/125 I and load a p53 mutant restoring regent, Prima‐1. The 125 I‐labeled nanocomposites display an impressive tumor imaging as well as a long radiation treatment cycle. The 131 I‐labeled nanoparticles show remarkable anti ATC‐tumor effects in vitro and in vivo, due to radiosensitization of Prima‐1 by reactivation of the p53 mutants.