In the present study, in situ synthesis of a drug-loaded metal–organic framework (MOF) was accomplished at room temperature. The produced drug-loaded MOF [{Zn2(1,4-bdc)2(dabco)}n] was then studied as a drug delivery system and exhibited the ability to entrap ibuprofen model drug. The ibuprofen loading efficiency of the MOF was 15% (w/w) in the selected synthesis conditions. The drug release was also monitored and 80% of the loaded drug was released over 12 days. The MOF was characterized by IR spectroscopy, X-ray powder diffraction (XRD), thermogravimetric analysis (TGA), UV–vis spectroscopy, N2 adsorption porosimetric (BET), and field emission scanning electron microscopy (FE-SEM). The IC50 value, cytotoxicity, of Zn2(1,4-bdc)2(dabco) for human Hepatoma cell (HuH7) was determined to be 1 mg/ml by MTT assay.