@misc{10481/59367,
year = {2019},
month = {11},
url = {http://hdl.handle.net/10481/59367},
abstract = {The absorption study of drugs through different biological membranes constitutes
an essential step in the development of new pharmaceutical dosage forms. Concerning orally
administered forms, methods based on monolayer cell culture of Caco-2 (Caucasian colon
adenocarcinoma) have been developed to emulate intestinal mucosa in permeability studies. Although
it is widely accepted, it has disadvantages, such as high costs or high technical complexity, and
limitations related to the simplified structure of the monolayer or the class of molecules that can be
permeated according to the transport mechanisms. The aim of this work was to develop a new ex vivo
methodology which allows the evaluation of the intestinal apparent permeability coefficient (Papp)
while using fewer resources and to assess the correlation with Caco-2. To this end, pig (Sus scrofa)
duodenum segments were mounted in Franz diffusion cells and used to permeate four different drugs:
ketorolac tromethamine (Kt), melatonin (Mel), hydrochlorothiazide (Htz), and furosemide (Fur).
No statistically significant differences (p > 0.05) were observed corelating Papp values from Franz
diffusion cells and Caco-2 cell experiments for Kt, Htz, and Fur. However, there were statistically
significant differences (p < 0.05) correlating Papp values and Mel. The difference is explained by the
role of Mel in the duodenal epithelial paracellular permeability reduction. Ex vivo permeation may
be an equivalent method to Caco-2 for drugs that do not produce intestinal membrane phenomena
that could affect absorption.},
publisher = {MDPI},
keywords = {Franz cells},
keywords = {Caco-2 cells},
keywords = {Intestinal permeability},
keywords = {Apparent permeability},
title = {Validation of an Ex Vivo Permeation Method for the Intestinal Permeability of Different BCS Drugs and Its Correlation with Caco-2 In Vitro Experiments},
doi = {10.3390/pharmaceutics11120638},
author = {Sánchez, Aroha B. and Calpena, Ana C. and Mallandrich, Mireia and Clares Naveros, Beatriz},
}