An unusual nanocage-based framework of [Zn2(L)(H2O)1.5]·5H2O (1) was used as a drug carrier of 5-fluorouracil (5-FU) for drug delivery. The incorporation of drug 5-FU into the 1 was around 48.6 wt% per gram of dehydrated 1. 5-FU is released in a highly controlled and progressive manner with 98% of the drug release after 101 h at acidic condition and with 62% after 72 h at PBS. 1 did not exhibit any significant cytotoxicity using the vitro cytotoxicity assays. The result from this study suggested a new approach for MOFs to be used as potential drug delivery.