Recent developments in materials science and specific surface functionalization of materials are providing new tools for the rational design of precisely engineered drug delivery systems. Particular interest has been paid to the exploitation of functionalized materials in the administration of biopharmaceuticals by the oral route, traditionally challenging and frequently compromised when using conventional pharmaceutical approaches. Using such materials for producing particulate systems is a common approach to obtain advanced drug delivery systems capable of providing stable and biocompatible environments and allowing for a targeted delivery of the associated biopharmaceuticals. This work intends to provide a thorough, up-to-date and holistic discussion on specific engineering and surface functionalization strategies of multistage platforms towards the development of novel delivery platforms for oral drug administration, with particular focus on the different materials and their interactions at the biological-material-host interface. This review will also address the safety and toxicity concerns of the resulting drug delivery systems, as well as their regulatory status and pathway towards the market approval of novel biopharmaceutical products based on particulate delivery systems. (C) 2017 Elsevier Ltd. All rights reserved.