One-pot synthesis of acid-induced in situ aggregating theranostic gold nanoparticles with enhanced retention in tumor cellsElectronic supplementary information (ESI) available. See DOI: 10.1039/c9bm00014c

• Main Authors: Cheng, Mingbo, Zhang, Yahui, Zhang, Xiaolei, Wang, Wei, Yuan, Zhi
• Format: Journal Article
• Published: 23.04.2019
• ISSN: 2047-4830; 2047-4849
• DOI: 10.1039/c9bm00014c

In this work, we took advantage of a one-pot reaction to prepare tumor-targeting nanoparticles (Au@T), which could respond to the intracellular acidic environment and form aggregates to enhance the retention effect of nanoparticles in tumor cells. Au@T is composed of gold nanoparticles (Au NPs) modified with 4-mercaptobenzoic acid (MCBA), p -hydroxythiophenol (HTP), LA (lipoic acid)-PEG 2K -OCH 3 and LA-PEG 2K -biotin. During blood circulation, Au@T remains well dispersed, making it inconspicuous. Then, with the help of active targeted transport, much more Au@T becomes internalized at the tumor site. After being internalized by tumor cells, Au@T aggregates under the condition of pH = 6.0, thereby improving the retention effect of Au@T, stymieing exocytosis and reducing the amount of nanoparticles returned to the blood stream. Furthermore, the in vivo experimental results showed that aggregated Au@T exhibits excellent photothermal effects, with a tumor inhibition rate of 86.40%. The computed tomography (CT) value was found to be 1.5 times higher than that of the control group (Au@Bio), as Au@Bio was unable to aggregate in tumor cells. In conclusion, this work provides a simple method for synthesizing a type of gold nanoparticles (Au@T) with promising potential for tumor diagnosis and treatment through enhancing the retention effect in tumor cells. In this work, we took advantage of a one-pot reaction to prepare tumor-targeting nanoparticles (Au@T), which could respond to the intracellular acidic environment and form aggregates to enhance the retention effect of nanoparticles in tumor cells, for tumor dual-mode diagnose and photothermal therapy.