Multifunctional theranostic agents having targeting function, therapeutic function and imaging function are promising for cancer treatment and diagnosis. Herein, gold nanorods (AuNRs) covered with mercaptohexadecanoic acid (MHA) for functionalizing the surface to bind amino group from both, antibody and functional dendrimer using condensing reagents. Trastuzumab was conjugated to improve cellular uptake by HER2-overexpressing cancer cells. Beforehand, AuNRs was stabilized by polyamidoamine (PAMAM) dendrimer which was modified with Gd-DOTA molecule for MRI detection and poly(ethylene glycol) (PEG) chain to provide the colloidal stability and enhanced permeability and retention effect in the bloodstream after intravenous injection. The fabricated nanohybrid (Trastuzumab-AuNRs-functional dendrimer) had homogeneous hydrodynamic size about 75 nm and showed typical surface plasmon absorption peaks at 520 nm and 820 nm, which corresponds to the transverse and longitudinal electronic oscillation of AuNRs, respectively. Trastuzumab-modified nanohybrids were efficiently internalized by SKOV-3 cells, HER2-overexpressing ovarian cancer cells, even at low concentration (5 µg/mL of AuNRs). Furthermore, nanohybrid exhibits low toxicity to SKOV-3 cells even at high concentration (200 µg/mL of AuNRs). In addition, the photothermal effect induced by near-infrared (NIR) laser irradiation to nanohybrid was sufficient to induce 80-90% of cancer cell killing. Therefore, fabricated nanohybrids are promising for targeted photothermal therapy and imaging.

Development of multifunctional nanohybrid: antibody-conjugated gold nanorods stabilized by functional dendrimer for targeted photothermal therapy and imaging

255th National Meeting (2018)

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