Journal
CARBOHYDRATE POLYMERS
Volume 157, Issue -, Pages 1442-1450Publisher
ELSEVIER SCI LTD
DOI: 10.1016/j.carbpol.2016.09.096
Keywords
Xylan; 5-Fluorouracil-l-acetic acid (5-FUAC); Drug release; Gastrointestinal contents; Cell cytotoxicity
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Funding
- Ministry of Human Resource Development (MHRD), New Delhi
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In the present study, xylan-5-fluorouracil-1-acetic acid (Xyl-5-FUAC) conjugates as colon specific pro drugs were synthesized and evaluated by in-vitro release study. The chemical stability of the conjugates was performed in acidic (pH 1.2) and basic buffers (pH 7.4), which showed their stability in upper gastrointestinal tract. The in-vitro drug release profiles of the conjugates were studied in the presence of rat's gastrointestinal contents. The results showed that the low amounts or drug 3-4% and 5-7% were released in gastric and small intestine contents respectively, while 53-61% of the drug was released in cecum and colonic contents. The cytotoxicity studies of the conjugates were also evaluated on human colorectal cancer cell line (HTC-15 and HT-29), which showed that the conjugates are more cytotoxic than the free drug. Therefore the results reveal that Xyl-5-FUAC conjugates are potential candidates for colon specific drug delivery in the treatment of colonic cancer with minimal undesirable side effects. (C) 2016 Elsevier Ltd. All rights reserved.
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