One-step, Rapid and Green Synthesis of Multifunctional Gold Nanoparticles for Tumor-Targeted Imaging and Therapy

Feng Gan,Hua Qin Yin,Gang Ye,Guang Shao

doi:10.1186/s11671-019-3232-3

Feng Gan, Hua Qin Yin + Show 2 more

Open Access

https://doi.org/10.1186/s11671-019-3232-3

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Abstract

Gold nanoparticles (GNPs) have always been used as doxorubicin (DOX) transport vectors for tumor diagnosis and therapy; however, the synthesis process of these vectors is to prepare GNPs via chemical reduction method firstly, followed by conjugation with DOX or specific peptides, so these meth•ods faced some common problems including multiple steps, high cost, time consuming, complicated preparation, and post-processing. Here, we present a one-step strategy to prepare the DOX-conjugated GNPs on the basis of DOX’s chemical constitution for the first time. Moreover, we prepare a multifunctional GNPs (DRN-GNPs) with a one-step method by the aid of the reductive functional groups possessed by DOX, RGD peptides, and nuclear localization peptides (NLS), which only needs 30 min. The results of scattering images and cell TEM studies indicated that the DRN-GNPs could target the Hela cells’ nucleus. The tumor inhibition rates of DRN-GNPs via tumor and tail vein injection of nude mice were 66.7% and 57.7%, respectively, which were significantly enhanced compared to control groups. One step synthesis of multifunctional GNPs not only saves time, materials, but also it is in line with the development direction of green chemistry, and it would lay the foundation for large-scale applications within the near future. Our results suggested that the fabrication strategy is efficient, and our prepared DRN-GNPs possess good colloidal stability in the physiological system; they are a potentially contrast agent and an efficient DOX transport vector for cervical cancer diagnosis and therapy.

Highlights

Doxorubicin (DOX) is a commonly used anticancer drug which has been widely used in a variety of cancer chemotherapy, such as blood malignant tumor [1], a variety of adenocarcinoma [2–5], soft tissue sarcoma [6], and so on
This is the first report for synthesis of DOX, RGD, and nuclear localizing signal (NLS) peptides conjugated multifunctional Gold nanoparticles (GNPs) with a one-step method, and their application in tumor diagnosis and therapy
The one-step synthesized DRN-GNPs still possess good colloidal stability in the physiological system, and the peptides conjugated on the surface remained the targeted ability and DOX still possesses its anti-tumor ability

Summary

Introduction

Doxorubicin (DOX) is a commonly used anticancer drug which has been widely used in a variety of cancer chemotherapy, such as blood malignant tumor [1], a variety of adenocarcinoma [2–5], soft tissue sarcoma [6], and so on. It is very necessary to develop a drug carrier with good biocompatibility and high drug loading ability. The highlight of their work is that the GNPs enter tumor cells via receptor-mediated endocytosis of RGD peptides and enter nucleus by the aid of NLS peptides, which makes DOX effectively interfere with DNA synthesis. It needed at least 120 h by coupling peptides or drugs layer by layer on the GNPs, and each process needed at least 24 h. It is necessary to develop a simple and rapid method for synthesis of multifunctional gold nanomaterials

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