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Published on: June 23, 2020
Surface Functionalization of Gold Nanoparticles for Targeting the Tumor Microenvironment to Improve Antitumor
Kin Fai Tan1, Lionel Lian Aun In2, Palanirajan Vijayaraj Kumar1
1Department of Pharmaceutical Technology, Faculty of Pharmaceutical Sciences, UCSI University, No. 1, Jalan Menara Gading, Taman Connaught, Cheras, Kuala Lumpur 56000, Malaysia.
Abstract:
Gold nanoparticles (AuNPs) have undergone significant research for their use in the treatment of cancer. Numerous researchers have established their potent antitumor properties, which have greatly impacted the treatment of cancer. AuNPs have been used in four primary anticancer treatment modalities, namely radiation, photothermal therapy, photodynamic therapy, and chemotherapy. However, the ability of AuNPs to destroy cancer is lacking and can even harm healthy cells without the right direction to transport them to the tumor microenvironment. Consequently, a suitable targeting technique is needed. Based on the distinct features of the human tumor microenvironment, this review discusses four different targeting strategies that target the four key features of the tumor microenvironment, including abnormal vasculature, overexpression of specific receptors, an acidic microenvironment, and a hypoxic microenvironment, to direct surface-functionalized AuNPs to the tumor microenvironment and increase antitumor efficacies. In addition, some current completed or ongoing clinical trials of AuNPs will also be discussed below to further reinforce the concept of using AuNPs in anticancer therapy.
Insights
Gold nanoparticles (AuNPs) show promise for cancer treatment but require targeted delivery. This review explores four strategies to direct AuNPs to tumors, enhancing their effectiveness and safety in cancer therapy.
Area of Science:
- Biomedical Engineering
- Nanotechnology
- Oncology
Background:
- Gold nanoparticles (AuNPs) possess significant antitumor properties.
- AuNPs are utilized in radiation, photothermal, photodynamic, and chemotherapy for cancer treatment.
- Current limitations include lack of targeted delivery and potential harm to healthy cells.
Purpose of the Study:
- To review targeting strategies for AuNPs in cancer therapy.
- To enhance the efficacy and specificity of AuNPs by directing them to the tumor microenvironment.
- To discuss the clinical translation of AuNP-based cancer treatments.
Main Methods:
- Discussion of four targeting strategies based on tumor microenvironment features: abnormal vasculature, receptor overexpression, acidic pH, and hypoxia.
- Review of surface-functionalized AuNPs for targeted delivery.
- Analysis of current clinical trials involving AuNPs.
Main Results:
- Targeting strategies can effectively direct AuNPs to the tumor microenvironment.
- Surface functionalization enhances AuNP accumulation in tumors.
- Clinical trials indicate the potential of AuNPs in various cancer treatments.
Conclusions:
- Targeted delivery of AuNPs is crucial for maximizing anticancer efficacy and minimizing side effects.
- Exploiting unique tumor microenvironment features offers promising avenues for AuNP-based cancer therapy.
- Further clinical investigation is warranted to fully realize the therapeutic potential of AuNPs.

