Effect of co-administration of probiotics with polysaccharide based colon targeted delivery systems to optimize site specific drug release

Eur J Pharm Biopharm. 2015 Nov;97(Pt A):164-72. doi: 10.1016/j.ejpb.2015.09.012. Epub 2015 Sep 28.

Abstract

Significant clinical success of colon targeted dosage forms has been limited by their inappropriate release profile at the target site. Their failure to release the drug completely in the colon may be attributed to changes in the colonic milieu because of pathological state, drug effect and psychological stress accompanying the diseased state or, a combination of these. Alteration in normal colonic pH and bacterial picture leads to incomplete release of drug from the designed delivery system. We report the effectiveness of a targeted delivery system wherein the constant replenishment of the colonic microbiota is achieved by concomitant administration of probiotics along with the polysaccharide based drug delivery system. Guar gum coated spheroids of sulfasalazine were prepared. In the dissolution studies, these spheroids showed markedly higher release in the simulated colonic fluid. In vivo experiments conducted in rats clearly demonstrated the therapeutic advantage of co-administration of probiotics with guar gum coated spheroids. Our results suggest that concomitant use of probiotics along with the polysaccharide based delivery systems can be a simple strategy to achieve satisfactory colon targeting of drugs.

Keywords: Colon targeted delivery system; Dissolution; Probiotics; Spheroids; Sulfasalazine; Ulcerative colitis.

MeSH terms

  • Animals
  • Colon / metabolism*
  • Colon / microbiology
  • Drug Delivery Systems*
  • Drug Liberation
  • Galactans / chemistry
  • Male
  • Mannans / chemistry
  • Microbiota
  • Plant Gums / chemistry
  • Polysaccharides / chemistry
  • Probiotics / administration & dosage*
  • Probiotics / pharmacokinetics
  • Rats
  • Rats, Sprague-Dawley
  • Sulfasalazine / administration & dosage*
  • Sulfasalazine / pharmacokinetics

Substances

  • Galactans
  • Mannans
  • Plant Gums
  • Polysaccharides
  • Sulfasalazine
  • guar gum