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Revista Brasileira de Ciências Farmacêuticas

Print version ISSN 1516-9332

Abstract

FREIRE, Ana Cristina; PODCZECK, Fridrun; SOUSA, João  and  VEIGA, Francisco. Colonic drug delivery. I- The colon as a site for drug delivery. Rev. Bras. Cienc. Farm. [online]. 2006, vol.42, n.3, pp.319-335. ISSN 1516-9332.  http://dx.doi.org/10.1590/S1516-93322006000300003.

Drug delivery to the colon has become attractive to researchers interested in the treatment of local diseases and for its potential for the delivery of proteins and therapeutic peptides. The treatment of colonic disorders like the inflammatory bowel disease can be improved by the use of systems capable of delivering the appropriate pharmacological agent selectively in the active site of inflammation, because it reduces the oral dose and its systemic side effects. The activity of the peptidases in the colon is very low, which makes possible to such labile molecules like proteins and peptides to be orally administered, without compromising their bioavailability. In the development of these systems it is fundamental to fully understand the colon as a site for drug delivery and, in particular, aspects like transit time, pH and enzyme activity of the colon, which are the basic mechanisms used to trigger release of a drug in the colon. Another important aspect is the absorptive capacity of the colon. In this context, the long residence time and the presence of some biological and chemical barriers might, respectively, enhance or limit drug absorption. The impact of the active inflammatory bowel disease on the efficacy of the systems used for targeting drugs to the colon might have been underestimated, since this pathology can alter the colonic pH and the enzyme activity of the colon.

Keywords : Colon; Gastrointestinal transit; Colonic pH; Colonic microflora; Absorption; Inflammatory bowel disease.

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