title: 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.
authors: University of São Paulo, São Paulo, SP, Brazil. jgoncalves@usp.br
authors: José Eduardo
authors: JE
authors: Gonçalves
authors: Mariane
authors: M
authors: Ballerini Fernandes
authors: Chang
authors: C
authors: Chiann
authors: Maria Nella
authors: MN
authors: Gai
authors: Jacqueline
authors: J
authors: De Souza
authors: Sílvia
authors: S
authors: Storpirtis
mesh_terms: D000904:Antibiotics, Antitubercular / Q000737:chemistry / Q000378:metabolism*; D018938:Caco-2 Cells; D002851:Chromatography, High Pressure Liquid; D006801:Humans; D006863:Hydrogen-Ion Concentration; D007408:Intestinal Absorption; D007413:Intestinal Mucosa / Q000378:metabolism*; D009077:Mucins / Q000378:metabolism*; D010539:Permeability; D012293:Rifampin / Q000737:chemistry / Q000378:metabolism*; D012710:Serum Albumin, Bovine / Q000378:metabolism*; D012995:Solubility; D013056:Spectrophotometry, Ultraviolet
chemical_list: D000904:Antibiotics, Antitubercular; D009077:Mucins; D012710:Serum Albumin, Bovine; D012293:Rifampin