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Abstract
Objective of the present investigation was to prepare and evaluate the potential of enteric coated dextran microspheres for colon targeting of 5-fluorouracil (5-FU). Dextran microspheres were prepared by emulsification-crosslinking method and the formulation variables studied included different molecular weights of dextran, drug:polymer ratio, volume of crosslinking agent, stirring speed and time. Enteric coating (Eudragit S-100) of dextran microspheres was performed by oil-in-oil solvent evaporation method using different coat:core ratios (4:1 or 8:1). Uncoated and coated dextran microspheres were characterized by particle size, surface morphology, entrapment efficiency, DSC, in vitro drug release in the presence of dextranase and 2% rat cecal contents. The release study of 5-FU from coated dextran microspheres was pH dependent. No release was observed at acidic pH; however, the drug was released quickly where Eudragit starts solublizing there was continuous release of drug from the microspheres. Organ distribution study was suggested that coated dextran microspheres retard the release of drug in gastric and intestinal pH environment and released of drug from microspheres in colon due to the degradation of dextran by colonic enzymes.
Acknowledgements
The authors gratefully acknowledge Head, Dept. Pharm. Sci., Dr. H.S. Gour University, Sagar, India, for providing the necessary facilities to carry out the research work. The authors thank Dr. Rajesh Pathania, All India Institute of Medical Sciences, New Delhi, India, for providing SEM facility. The authors also thank Dr. S. Dhaneshwar, Bharati Vidyapeeth Deemed University, Pune, India, for providing DSC facility.
Declaration of interest
The authors report no conflicts of interest. The authors alone are responsible for the content and writing of this article.