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Evaluation of mechanisms involved in the permeability of antiretroviral drugs through in situ perfusion model in rats


The bioavailability of a drug is the determinant factor of clinical efficacy and it depends on the release of active ingredient from the dosage form and its absorption. Thus, the control of the extent and rate of absorption of an orally administered drug depends on two aspects: solubility in the physiological fluids and permeability through biological membranes. Based on these characteristics, the Biopharmaceutical Classification System (BCS) was proposed for application in development of new compounds, new formulations and biowaiver processes. After, another tool was proposed for classification of drugs and it was designated of BDDCS (Biopharmaceutics Drug Disposition Classification System), which considers the solubility and metabolism of the compounds. Then, with the development of biopharmaceutical systems (BCS and BDDCS) and its wide applicability in research and drug development, several models for permeability studies have been developed and the in situ perfusion model has been increasingly employed because it is a model that most closely resembles of in vivo conditions and it allows to evaluate and characterize the different mechanisms involved in the permeability of the drugs, considering that occurs by passive transport and by active transport or when there are other mechanisms involved as pre-systemic metabolism or efflux transport by glycoprotein-P. The mechanisms involved in the permeability of antiretroviral drugs are still not fully understood and some information is scarce in the literature. Furthermore, the bioavailability of compounds as stavudine, lamivudine and zidovudine indicates variability in permeation processes. Thus, the objective of this study is to elucidate the mechanisms involved in the permeability of antiretroviral drugs through in situ perfusion model, considering aspects related to pre-systemic metabolism in enterocytes and efflux of these substances. (AU)

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(References retrieved automatically from Web of Science and SciELO through information on FAPESP grants and their corresponding numbers as mentioned in the publications by the authors)
DEZANI, THAISA MARINHO; DEZANI, ANDRE BERSANI; COQUEMALA DA SILVA, MONICA MARIA; DOS REIS SERRA, CRISTINA HELENA. In Situ Intestinal Perfusion in Rodents: Future Perspectives for Application on Absorption Studies and Classification of Drugs. MINI-REVIEWS IN MEDICINAL CHEMISTRY, v. 17, n. 9, p. 746-757, 2017. Web of Science Citations: 2.

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