Background: Gold nanoparticles (AuNPs), owing to their elegant physicochemical
properties, have recently been introduced as promising theranostic nanoparticles.
Folic acid is a necessary vitamin for cell proliferation. Accordingly, the surface functionalization
of AuNP with folic acid may offer a great potential for the development of a
strategy to increase the efficiency of cancer diagnosis and therapy based on the new
nanotechnology. In this study, we have reviewed the recent progress made in the design
and the biomedical application of various folate-conjugated gold nanoparticles (FAuNPs).
Methods: We performed a structured search in bibliographic databases and made a comprehensive
list of relevant papers. The main subjects considered in this review included
(1) methods for the preparation of F-AuNPs, (2) applications of F-AuNPs in computed
tomography (CT), and (3) the use of F-AuNPs in targeted cancer therapy.
Results: As many as 96 papers were selected for the review. Accordingly, we explained
the noncovalent and the covalent methods of fabricating the various types of F-AuNPs.
Particular applications of F-AuNP in cancer diagnosis using the CT scan modality were
described. In addition, the applications of F-AuNPs in targeted radiation therapy, chemotherapy,
and hyperthermia were elucidated in depth. In the hyperthermia section, we presented
certain extra explanations on F-AuNP-based laser, radiofrequency, and ultrasoundbased
Conclusion: This review identifies the important roles of F-AuNPs in current cancer studies
that are being undertaken worldwide. The findings of this review confirm that F-AuNP
is a new theranostic agent, which has a great potential for simultaneous cancer therapy