New Targeted-colon Delivery System: In Vitro And In Vivo Evaluation Using X-ray Imaging | 8931
ISSN-2155-9929
Journal of Molecular Biomarkers & Diagnosis
Open Access
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T
he aim of this study was to formulate a new orally-administered colon delivery system of 5-flurouracil (5-FU) for the treatment
of colon cancer. The system was designed to target 5-FU directly to the colon with high potential of much more effective and less
toxic colon cancer treatment. The system was prepared by compression coating technique using granulated chitosan. The method
was optimized by studying the effect of granulation and thickness of the coat with respect to the in vitro performance in a medium
mimicking mouth-to-colon environment. The
in vivo
selectivity of the system was assessed by X-ray imaging technique using beagle
dogs. Results showed that granulation of chitosan were effective in protecting against the known acid solubility of the polymer. Formula
(F7) with coat weight of 50 mg/tablet exhibited the best protection profile with <10% of the drug released after 6 h. The resistance of the
system to the simulated gastro-intestinal media was reduced as the chitosan coat weight decreases. The performance of the system in a
rat caecal contents containing-medium showed that the susceptibility of this system for the enzymatic degradation by colonic enzymes.
The X-ray imaging gave rise to the
in vivo
selectivity of this system for colon targeting by showing the resistivity of the system to the
stomach and small intestine environment and the selective disintegration of the system inside the large bowel
Biography
Ibrahim A. Alsarra received his Bachelor of Pharmacy (B.S.), in 1996 from College of Pharmacy, King Saud University, Kingdom of Saudi Arabia and
his Doctor of Philosophy (Ph.D.) in Pharmaceutical Biotechnology and Drug Formulation Development, Division of Pharmaceutical Sciences, School
of Pharmacy, University of Missouri-Kansas City, Missouri 64110-2265, USA. He joined King Saud University in 2002 and is currently the Deputy
Director for Research and Technical Affairs, Centre of Excellence in Biotechnology Research, the only biotechnology center in Saudi Arabia, King
Saud University. He is the President of Saudi Pharmaceutical Society and the Editor-in-Chief of Saudi Pharmaceutical Journal, a peer-reviewed and
ISI-Indexed Journal
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