Effect of pH, mucin and bovine serum on rifampicin permeability through Caco-2 cells.

Abstract:

:Rifampicin, a poorly soluble drug, has great importance in therapeutics as it is the main drug used to treat tuberculosis. The characterization of its permeability and the factors that influence it represent an important tool for predicting its bioavailability. Caco-2 cell monolayers were used as models of the intestinal mucosa to assess the uptake and transport of rifampicin and the effects of various experimental conditions were investigated, in order to establish the influence of these variables on rifampicin permeability. Different pHs (5.8, 6.8 and 7.4) in the apical medium, the presence or absence of mucin (3.0% w/v) in the donor site and the presence or absence of bovine serum albumin (4.0% v/v) in the receptor chamber were the evaluated conditions. The quantification of rifampicin in the apical or basolateral chambers was performed by a validated HPLC-UV method. The change in the donor chamber pH showed that permeability values were greater at pH 6.8, although this increase does not result in an alteration of the qualitative classification of rifampicin, which has high permeability. Mucin and bovine serum showed no effects on the permeability of rifampicin at the concentration tested. Overall, the current study suggests that pH, artificial mucin and bovine serum proteins have no influence on rifampicin permeability.

journal_name

Biopharm Drug Dispos

authors

Gonçalves JE,Ballerini Fernandes M,Chiann C,Gai MN,De Souza J,Storpirtis S

doi

10.1002/bdd.1802

subject

Has Abstract

pub_date

2012-09-01 00:00:00

pages

316-23

issue

6

eissn

0142-2782

issn

1099-081X

journal_volume

33

pub_type

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