The present invention provides a composition and prodrug for targeted drug delivery to the central nervous system of a patient. The inventive composition and prodrug include a pharmaceutically acceptable active agent and at least one protein selected from the group consisting of a fimbrial adhesin protein, a membrane protein, and combinations thereof. The inventive compositions and prodrugs of the present invention selectively target the blood-brain barrier and deliver hydrophilic and lipophilic active agents of varying sizes to the central nervous system.