As a potential drug carrier, the toxicity of gold nanorods (AuNRs) has been extensively studied to ensure their safety. Some of these studies reported that AuNRs caused a series of toxic cell responses and inspired the hypothesis that AuNRs may act as anti-cancer agents. In the present study, we synthesized AuNRs (72× 17 nm) and low density lipoprotein (LDL) peptide-RLT modified AuNRs to test this hypothesis. A tumor cell inhibition assay was conducted in five cell lines, and RLT-AuNRs demonstrated the most efficient inhibition of SGC-7901 cells. RLT-AuNRs inhibited SGC-7901 cells and increased SGC-7901 cell apoptosis more effectively than did AuNRs and DOX in vitro. Treatment with RLT-AuNRs reduced the tumor volume, decreased the tumor weight, and enhanced the tumor inhibition rates. RLT-AuNRs showed comparable anti-tumor efficacy with DOX but possessed higher in vivo safety than did DOX. Nude mice treated with RLT-AuNRs showed good health and gained weight during the ten-day anti-tumor therapy. Histological results showed no tissue toxicity of RLT-AuNRs. Therefore, RLT-AuNRs may be a viable anti-tumor agent for gastric cancer.

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