The surface of layered double hydroxide nanoparticles, a potential drug-delivery nanovehicle, is modified with the cancer-cell-specific ligand, folic acid. The surface modification is successfully accomplished through step-by-step coupling reactions with aminopropyltriethoxysilane and 1-ethyl-3-(3-dimethyl aminopropyl)-carbodiimide. In order to evaluate the cancer-cell targeting effect of folic-acid-grafted layered double hydroxide utilizing fluorescence-related assay, both layered double hydroxide with and without folic acid moiety are labeled with fluorescein 5′-isothiocyanate. The uptake of layered double hydroxide and folic acid conjugated into KB and A549 cells is visualized using fluorescence microscopy and measured by flow cytometry. Both chemical and biological assay results demonstrate that the folic acid molecules are indeed conjugated to the surface of layered double hydroxide and thus the selectivity of nanovehicles to cancer cells overexpressing folate receptors increases. In this study, it is suggested that layered double hydroxide nanoparticles can be used as drug-delivery carriers with a targeting function due to the chemical conjugation with specific ligand.