Objective       To prepare arginine-glycine-aspartic acid (RGD)-conjugated paclitaxel (PTX) and microRNA-34a co-loaded liposome (RGDmiLPs-34a/PTX)

and to evaluate their properties

and targeting inhibitory effects in A549 cells.       Methods       The liposomes RGDmiLPs-34a/PTX were prepared by thin film hydration. The particle size

zeta potential and entrapment efficiency were evaluated. The efficiency of cellular uptake and tumor spheroids penetration of RGDLP and LP on A549 cells

in vitro

was evaluated by cellular uptaking test and cofocal laser scanning microscopy. The anti-proliferation efficiency of RGDmiLPs-34a/PTX to A549 cells was evaluated by MTT assay. Tumor spheroids were used to evaluate anti-tumor ability of RGDmiLPs-34a/PTX.       Results       The particle diameter of the RGDmiLPs-34a/PTX was 125.0±11.8 nm with a zeta potential of 21.00±4.85 mV. The entrapment efficiency of PTX and microRNA-34a were 81.5% and 94.6% respectively. The result of cellular uptaking test demonstrated that RGDLP were uptaken by A549 cells by 2.6 times higher than LP (

P

<

0.01). MTT assay confirmed RGDmiLPs-34a/PTX had stronger inhibitory effect to A549 cells than miLPs-34a/PTX

RGDmiLPs-34a and RGDLP-PTX. The tumor spheroid was inhibited by 81%

77%

64% and 37% respectively when treated by miLPs-34a/PTX

RGDmiLPs-34a

RGDLP-PTX and RGDmiLPs-34a/PTX

with the latest having the strongest inhibitory effect (

P

<

0.01).       Conclusion       RGD-conjugated PTX and microRNA-34a co-loaded liposomes RGDmiLPs-34a/PTX are well targeting to and exerting inhibitory effect on lung cancer cells

and they are a potential delivery system for the treatment of lung cancer.