Polysaccharide matrices for microbially triggered drug delivery to the colon.
Matrix tablets were prepared using xanthan gum (XG) and guar gum (GG) in varying proportions, and the suitability of the prepared tablets was evaluated for colon specific drug delivery. Indomethacin was used as a model drug. The ability of the prepared matrices to retard drug release in the upper gastrointestinal tract (GIT) and to undergo enzymatic hydrolysis by the colonic bacteria was evaluated. For this, drug release studies were carried out in the presence of rat cecal content. Further cecal content of rats with induced enzymatic activity were used. To ascertain the role of bacterial flora in carrying out the hydrolysis of the tablet, cecal content of rats treated with antibiotics were used in the dissolution media. Presence of XG in combination with GG in the tablets could retard drug release in the conditions of the upper GIT. However, the presence of GG and starch made these matrices microbially degradable. Guar gum alone as a drug release-retarding excipient in the matrices does not achieve the desired retardation. Presence of XG in the tablets not only retards the initial drug release from the tablets, but due to high swelling, makes them more vulnerable to digestion by the microbial enzymes in the colon.
Sinha
V R
VR
University Institute of Pharmaceutical Sciences, Panjab University, Chandigarh, India. vr_sinha@yahoo.com
Kumria
Rachna
R
D000818:Animals; D000900:Anti-Bacterial Agents / Q000494:pharmacology; D002432:Cecum / Q000201:enzymology / Q000378:metabolism / Q000382:microbiology; D003106:Colon / Q000378:metabolism* / Q000382:microbiology; D004337:Drug Carriers; D005685:Galactans / Q000737:chemistry*; D066298:In Vitro Techniques; D007213:Indomethacin / Q000008:administration & dosage / Q000737:chemistry / Q000493:pharmacokinetics; D008351:Mannans / Q000737:chemistry*; D008795:Metronidazole / Q000494:pharmacology; D053149:Plant Gums; D011135:Polysaccharides, Bacterial / Q000737:chemistry*; D051381:Rats; D017208:Rats, Wistar; D012995:Solubility; D013608:Tablets, Enteric-Coated
D000900:Anti-Bacterial Agents; D004337:Drug Carriers; D005685:Galactans; D008351:Mannans; D053149:Plant Gums; D011135:Polysaccharides, Bacterial; D013608:Tablets, Enteric-Coated; D008795:Metronidazole; C007894:guar gum; C002563:xanthan gum; D007213:Indomethacin