Research on mesoporous materials for biomedical and biological applications has experienced an outstanding increase during recent years. This review with ca. 420 references provides an overview of mesoporous structures covering synthesis and bioapplications. Various methods of mesoporous material preparation and modification are discussed as controlled synthesis of these molecular sieves has great impact on their properties and applications. In the area of bioapplications, mesoporous materials offer the potential for drug delivery, bioimaging, regenerative medicine, optical and electrochemical biosensing, enzyme immobilization, biomolecule sorption and separation and many others. We also discuss the cytotoxicity aspects of mesoporous structures being of crucial importance for successful application of these novel tools in the biomedical field. Future prospects of mesoporous materials have been also briefly discussed. We believe that the present review will serve as a comprehensive guide for scientists in the area of biosciences giving the background in regard to mesoporous materials.