Targeted and Specific Modification with 4‐Carboxybenzeneboronic Acid and TPGS of Fluorescent Gold Nanoparticles and the Enhanced Antitumor Activity Research

Abstract A targeting and specific fluorescent gold nanoparticle is prepared for tracing of drug and effective treatment of cancers. First, 4‐carboxybenzeneboronic acid (CBPA) and D‐α‐tocopheryl polyethylene glycol 1000 succinate (TPGS) are used to modify cyclodextrins (CDs), then modified cyclodextrins and polyethylene glycol (PEG) are used to stabilize gold nanoclusters to prepare fluorescent gold nanoparticles (AuNCs@CD‐TPGS‐CBPA/PEG). CBPA has targeting and TPGS can induce apoptosis, therefore, AuNCs@CD‐TPGS‐CBPA/PEG has targeting and certain anti‐tumor activity. The structure and morphology of the nanomaterial are characterized by using nuclear magnetic resonance (NMR) spectroscopy and transmission electron microscope (TEM). Paclitaxel (PTX) is loaded into the hydrophobic cavity of CDs to form targeting specific drug‐loaded fluorescent gold nanoparticles (AuNCs@CD‐TPGS‐CBPA/PEG/PTX). Biological performances of AuNCs@CD‐TPGS‐CBPA/PEG are studied by in vitro and in vivo experiments. In vitro test results confirm that AuNCs@CD‐TPGS‐CBPA/PEG could be internalized by tumor cells, and effectively against tumor cells, but it is biocompatible to normal cells. In vivo experiments prove that AuNCs@CD‐TPGS‐CBPA/PEG has excellent targeting, biocompatibility, and enhanced antitumor capability, could enrich and stay for a long time in the tumor regions, effectively prolong the lifetime of tumor‐bearing mice. Therefore, this work provides an insight into the development of fluorescent gold nanomaterials for practical biomedical application.