Objective To study effective carriers that can enhance the antitumor effect of paclitaxel (PTX). Methods PTX-loaded polylactic-co-glycolic acid (PLGA) nanoparticles (NPs) (PTX-PLGA NPs), constructed using the emulsification solvent evaporation method, were characterized by scanning electron microscopy and dynamic light scattering. Non-small-cell lung carcinoma (NSCLC) cells were divided into the dimethyl sulfoxide (DMSO) group, PLGA NPs group, PTX group, and PTX-PLGA NPs group. Cell viability was detected by 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT), cell apoptosis was determined by flow cytometry, and cell migration and invasion were assessed using Transwell assay. Results PTX-PLGA NPs were smooth in the surface and spherical in shape, with a particle size of 268 ± 1.3 nm. Both PTX and PTX-PLGA NPs could effectively inhibit the activity of A549 and H1650 cells. At 12 and 24 h, PTX-PLGA NPs presented weaker inhibition on the activity of NSCLC cells than PTX, but at 48 and 72 h, PTX-PLGA NPs presented stronger inhibition. Compared with PTX, PTX-PLGA NPs were more effective in enhancing apoptosis and inhibiting migration and invasion of NSCLC cells. Conclusion With good sustained release and the ability to promote cellular uptake, PTX-PLGA NPs can strongly inhibit the malignant activities of NSCLC cells, which can be used as a promising drug carrier.