OBJECTIVE: To prepare paclitaxel(PTX) and curcumin (CUR) chemically conjugated gold nanorod (GNR) (PTX/CUR-BPGNR), and to preliminarily study its anti-multidrug-resistant(MDR) tumor effect in vitro and mechanisms. METHODS: GNR was prepared by seed growth method and modified with biotin-polyethylene glycol (Biotin-PEG) to obtain BPGNRs. Lipoic acid PTX and CUR (PIXLA and CURLA) were synthesized; 1H-NMR and MS were used to confirm their chemical structures. PTXLA and CURLA were connected to BPGNR surface to obtain PIX and CUR-bonding BPGNR (PTX/CUR-BPGNR) via strong binding of Au-S bond. The morphology of PTX/CUR-BPGNR was observed, and drug-loading amount and in vitro drug release were investigated (under near-infrared illumination and esterase condition). Adriamycin (ADR) MDR breast cancer MCF-7/ADR cells were selected as research objects, and MTT assay was used to investigate the survival rate of cells after treated with BPGNR, PTX, CUR, PTX/CUR mixture and PTX/CUR-BPGNR, and ELISA was used to detect the expression of P-gp. RESULTS: PTX/CUR-BPGNR was prepared successfully with uniform size and shape. The maximum absorption wavelength was 808 nm, and drug-loading amount of PTX and CUR were 16.1% and 8.4%, respectively. The preparations were given near-infrared illumination and esterase to promote the release of PTX and CUR. 64 h accumulative drug release rates were 37.2% and 39.1%. Survival rates of MCF-7/ADR cells after treated with BPGNR, PTX, CUR and PTX/CUR mixture, PTX/CUR-BPGNR were 95.8%, 71.2%, 91.9%, 45.8% and 22.5%, respectively. The relative expressions of P-gp in cells were 105.6%, 75.2%, 73.8%, 51.7%, respectively. CONCLUSIONS: PTX/CUR-BPGNR is successfully prepared and can improve the ability of CUR inhibiting the expression of P-gp so as to strengthen its anti-MDR effects.