Colonic targeting

F Harboe, C Larsen, MJ Johansen, HP Olesen. Macromolecular prodrugs. XV. Colon-targeted delivery—Bioavailability of naproxen from orally administered dextran-naproxen ester prodrugs varying in molecular size in the pig. Pharm Res 6(11) 919—923, 1989. 

F. Hirayama, K. Minami, K. Uekama, In vitro Evaluation of Biphenylyl Acetic Acid-/3-cyclodextrin Conjugates as Colon-Targeting Prodrugs Drug Release Behaviour in Rat Biological Media , J. Pharm. Pharmacol. 1996, 48, 27-31. 

FIG. 5. Design of the colon-targeted delivery capsule (a) gelatin capsule (b) active ingredient (c) organic acid (d) enteric layer (e) hydrophilic layer and (f) acid-soluble layer (adapted from Ref 69). 

Mrsny, R.J., The colon as a site for drug delivery, J. Contr. Pel., 22 15-34 (1992). Hovgard, L., and Bronsted, H., Current applications of polysaccharides in colon targeting, Crit. Rev. Ther. Drug Carr. Syst., 13 185-223 (1996). 

Hirayama, F., Minami, K., and Uekama, K., In-vitro evaluation of biphenylyl acetic acid-beta-cyclodextrin conjugates as colon-targeting prodrugs drug release behaviour in rat biological media, J. Pharm. Pharmacol., 48 27-31 (1996). 

Villar-Lopez, M.E., Nieto-Reyes, L., Aguiano-Igea, S., Otero-Espinar, F.J., and Blanco-Mendez, J., Formulation of triamcinolone acetonide pellets suitable for coating and colon targeting, 7 r. J. Pharm., 179 229-235 (1999). 

Gazzaniga, A., Bussetti, C., Moro, L., Sangali, M.E., and Giordano, F., Time dependent oral delivery systems for colon targeting, STP Pharma. Sci., 5 83-88 (1995). 

Figure 6.3. OROS-CT (Oral Osmotic System for Colon Targeting) and COER-24 (Controlled Onset Extended Release) delivery systems.

Chourasia MK, Jain SK. Polysaccharides for colon targeted drug delivery. Drug Deliv. 2004 11 129—148. 

Klotz U. Colonic targeting of aminosalicylates for the treatment of ulcerative colitis. Dig Liver Dis. 2005 37 381-388. 

R. Wilding, S. S. Davis, F. Pozzi, P. Furlani, A. Gazzaniga, Enteric coated timed release for colonic targeting, Int J Pharmaceutics 777 99-102 (1994). 

Colonic targeting has gained increasing interest over the past years. A considerable number of publications dealing with colon targeting, colon-specific drug delivery, and absorption from the cecum and other colon sections indicates a growing focus of research activities in this area. 

In general terms, colonic targeting must be based on ... 

It was for these reasons that we engaged in a colon-targeted systems design project that was based on a more effective and predictable gradient like microflora differences between small and large intestine to eventually replace simple time-or pH-triggered systems. 

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