Doxorubicin-conjugated multifunctional dendrimer-entrapped gold nanoparticles for pH-responsive drug delivery and targeted CT imaging of cancer cells

• 1、State Key Laboratory for Modification of Chemical Fibers and Polymer Materials, College of Materials Science and Engineering, Donghua University, Shanghai, 201620
• 2、College of Chemistry, Chemical Engineering and Biotechnology, Donghua University, Shanghai, 201620

Abstract：In this paper, the anti-cancer agent doxorubicin (DOX) was covalently conjugated onto the surface of folic acid-modified multifunctional dendrimers through pH-sensitive cis-aconityl linkage, followed by entrapment of gold nanoparticles to form a theranostic nanosystem. In the formed theranostic nanosystem, every dendrimer was conjugated with 9 DOX molecules, and the mean diameter of Au core nanoparticle is 2.8 nm. The formed DOX-conjugated Au nanoparticles diaplay an acid-sensitive drug release effect with a higher release rate under a lower pH condition due to the introduction of cis-aconityl linkage. The loading of DOX makes the theranostic nanosystem demonstrate a certain anti-cancer efficiency in vitro. At the same time, the folic acid modification enables the theranostic nanosystem to target cancer cells overexpressing folic acid receptors and achieve targeted CT imaging of the cancer cells.

Keywords： multifunctional dendrimers doxorubicin gold nanoparticles pH-responsive drug release targeted theranostics