title: The biopharmaceutical classification system of excipients.
abstract: The increasing number of new chemical entities is bringing new challenges to the field of drug delivery. These drugs present bioavailability issues that are frequently associated with intestinal metabolism or efflux mechanisms. Some excipients, particularly surfactants, have demonstrated a capacity to interfere with these mechanisms, improving drug bioavailability. Consequently, these excipients can no longer be considered as inert and should be subject to special considerations from a regulatory perspective. In the present manuscript, the state-of-the-art research related to these abilities of excipients to interfere with intestinal metabolism and efflux mechanisms are presented and discussed. Here, a biopharmaceutical classification system of excipients is proposed for the first time as a tool in the development of new products and for regulatory purposes.
authors.affiliation: BIAL-Portela & Cª, S.A. À Avenida da Siderugia Nacional, Trofa, Portugal.|Instituto de Ciências Biomédicas Abel Salazar, University of Porto, Porto, Portugal.|I3S - Instituto de Investigação e Inovação em Saúde, University of Porto, Porto, Portugal.|INEB - Instituto de Engenharia Biomédica, University of Porto, Porto, Portugal.
authors.forename: Teófilo
authors.initials: T
authors.lastname: Vasconcelos
authors.affiliation: Instituto de Ciências Biomédicas Abel Salazar, University of Porto, Porto, Portugal.|CIBIO/InBIO-UP - Research Centre in Biodiversity & Genetic Resources, University of Porto, Vairão, Portugal.
authors.forename: Sara
authors.initials: S
authors.lastname: Marques
authors.affiliation: I3S - Instituto de Investigação e Inovação em Saúde, University of Porto, Porto, Portugal.|INEB - Instituto de Engenharia Biomédica, University of Porto, Porto, Portugal.|CESPU, Instituto de Investigação e Formação Avançada em Ciências e Tecnologias da Saúde & Instituto Universitário de Ciências da Saúde, Gandra, Portugal.
authors.forename: Bruno
authors.initials: B
authors.lastname: Sarmento
mesh_terms: D001682:Biological Availability; D016503:Drug Delivery Systems; D005079:Excipients / Q000737:chemistry* / Q000145:classification*; D006801:Humans; D004364:Pharmaceutical Preparations; D013501:Surface-Active Agents
chemical_list: D005079:Excipients; D004364:Pharmaceutical Preparations; D013501:Surface-Active Agents
keywords: P-gp; biopharmaceutical classification system of excipients (BCSE); efflux transporters; efflux transporters inhibitors; intestinal metabolism inhibitors; permeability enhancers