Gold nanoparticles (AuNPs) have demonstrated increasingly wide applications in drug delivery due to their unique physicochemical
and optical properties as well as low toxicity. Compared to the organic nanocarriers for therapeutic agents, AuNPs have shown
superior performance as drug delivery vectors, including the inert nature, well-developed synthesis strategies, tunable size, and flexible
and easy surface modification with various chemical and biological molecules. In this review, we emphasize on the applications of
AuNPs in the aspect of improving pharmaceutical property and therapeutic efficacy of drugs, especially those covalently and noncovalently
connected to the surface of AuNPs. Acting as a solid core to link drugs and their derivatives, AuNPs provide the nano-prodrug
system with compressed size, high loading efficiency, three-dimension structure, and enhanced cellular uptake capability. With the intensive
and systematical investigation of the drug-connected AuNPs, several important issues will become the hot but emergent topics for
future research in this field, such as the toxicity in live human subjects, ultimate destination, and possible pathways and mechanisms for
their absorption, circulation, distribution, metabolism, and excretion.
Conjugates, drug delivery system, gold nanoparticles, toxicity.
Key Laboratory of Drug Quality Control and Pharmacovigilance, China Pharmaceutical University, Ministry of Education, Nanjing 210009, China.