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.
Especial agradecimento à Profa. Sílvia Storpirtis e ao Prof. Leoberto Costa Tavares pela orientação, esforço, ética, profissionalismo e, sobretudo, pelos formidáveis ensinamentos não restritos apenas aos temas envolvidos neste trabalho, mas também nas várias facetas da vida, o que os tornam exemplos de educadores e orientadores.Aos amigos José Eduardo Gonçalves e Marcus Tullius Scotti pela amizade e companheirismo durante todos estes anos, pelos preciosos ensinamentos, pela paciência e pela imensa colaboração oferecida desde a elaboração até a conclusão deste trabalho.Aos meus pais, Aitemar e Josiane, que, além de proporcionarem uma ótima infância e vida acadêmica, formaram os fundamentos do meu caráter e estão sempre presentes em minha vida de forma indispensável.A minha irmã e eterna bonequinha, Tatiane, por ter sido sempre meu incentivo para crescer.Ao meu noivo, Jorge Luís, pela paciência, companheirismo e força. Aos meus padrinhos, tios e primos pela constante torcida e apoio.
scite is a Brooklyn-based organization that helps researchers better discover and understand research articles through Smart Citations–citations that display the context of the citation and describe whether the article provides supporting or contrasting evidence. scite is used by students and researchers from around the world and is funded in part by the National Science Foundation and the National Institute on Drug Abuse of the National Institutes of Health.