Ultrathin mesoporous TiO 2 coatings with a wormhole-like architecture were synthesized using evaporation-induced self-assembly method. The morphological and chemical structures of TiO 2 films were characterized using small-angle and large-angle X-ray diffraction, scanning electron microscopy (SEM), transmission electron microscopy (TEM) and Fourier transformed infrared spectrometry (FTIR). The films demonstrated a thickness of ∼120 nm and open-porous nanostructure. By taking advantage of the tortuosity of the worm-like mesoporous architecture associated with the chemistry of the TiO 2 film, a sustained drug release using ibuprofen and vancomycin as model molecules from the film was determined. Besides, adhesion behavior of osteoblast cells, together with an in vitro apaptitic formation substantiated the cytocompatibility and bioactivity of the mesoporous TiO 2 films. Such combined bioactive and drug-releasing functions of the TiO 2 films with worm-like mesoporosity ensure an improved therapeutic performance for potential applications included orthopedics, dentistry, and drug delivery.