Nanoporous materials are currently being developed for use in implantable drug delivery systems, bioartificial organs, and other novel medical devices. Advances in nanofabrication have made it possible to precisely control the pore size, pore distribution, porosity, and chemical properties of pores in nanoporous materials. As a result, these materials are attractive for regulating and sensing transport at the molecular level. In this work, the use of nanoporous membranes for biomedical applications is reviewed. The basic concepts underlying membrane transport are presented in the context of design considerations for efficient size sorting. Desirable properties of nanoporous membranes used in implantable devices, including biocompatibility and antibiofouling behavior, are also discussed. In addition, the use of surface modification techniques to improve the function of nanoporous membranes is reviewed. An intriguing possibility involves functionalizing nanoporous materials with smart polymers in order to modulate biomolecular transport in response to pH, temperature, ionic concentration, or other stimuli. These efforts open up avenues to develop smart medical devices that respond to specific physiological conditions.