Preparation and In-vitro characterization of ethylcellulose coated pectin alginate microspheres of 5-fluorouracil for colon targeting.
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Date
2011-10
Authors
Ramana, G
Chaitanya, A Krishna
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Abstract
The main objective of the present study was to prepare and evaluate the colon-specific
pectin alginate microspheres of 5-fluorouracil (5-FU) for the treatment of colon cancer. Calcium
alginate beads were prepared by extruding 5-FU loaded alginate solution to calcium chloride
solution and gelled spheres were formed instantaneously by ionotropic gelation reaction using
different ratios of 5- FU and alginate, alginate and calcium chloride, stirring speeds (500-1500
rpm) and reaction time. The core beads were coated with ethyl cellulose to prevent drug release in
the stomach and provide controlled dissolution of enteric coat in the small intestine and
maximum drug release in the colon. Morphology and surface characteristics of the formulation
were determined by scanning electron microscopy. In vitro drug release studies were performed
in conditions simulating stomach to colon transit in the presence and absence of pectinase
enzyme. No significant release was observed at acidic pH, however, when it reached the intestinal
pH where ethyl cellulose starts to dissolve, drug release was observed. Also, release of drug was
found to be higher in presence of pectinase enzyme. The DSC and FT-IR studies were also
indicates there were no interactions between the drug and the polymers used.
Description
Keywords
5-FU, Pectin alginate beads, Ethyl cellulose, Scanning Electron Microscopy and Pectinase enzyme
Citation
Ramana G, Chaitanya A Krishna. Preparation and In-vitro characterization of ethylcellulose coated pectin alginate microspheres of 5-fluorouracil for colon targeting. Journal of Applied Pharmaceutical Science. 2011 Oct; 1(8): 170-176.