http://repository.iitr.ac.in/handle/123456789/14889
Title: | Synthesis and bio-evaluation of xylan-5-fluorouracil-1-acetic acid conjugates as prodrugs for colon cancer treatment |
Authors: | Sauraj Kumar S.U. Gopinath, Packirisamy Negi, Yuvraj Singh. |
Published in: | Carbohydrate Polymers |
Abstract: | In the present study, xylan-5-fluorouracil-1-acetic acid (Xyl-5-FUAC) conjugates as colon specific prodrugs 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 of 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. © 2016 Elsevier Ltd |
Citation: | Carbohydrate Polymers (2017), 157(): 1442-1450 |
URI: | https://doi.org/10.1016/j.carbpol.2016.09.096 http://repository.iitr.ac.in/handle/123456789/14889 |
Issue Date: | 2017 |
Publisher: | Elsevier Ltd |
Keywords: | 5-Fluorouracil-1-acetic acid (5-FUAC) Cell cytotoxicity Drug release Gastrointestinal contents Xylan |
ISSN: | 1448617 |
Author Scopus IDs: | 57192377506 55500572500 56242963200 6701821524 |
Author Affiliations: | Sauraj, Department of Polymer and Process Engineering, Indian Institute of Technology Roorkee, Roorkee, Uttarakhand 247667, India Kumar, S.U., Nanobiotechnology Laboratory, Centre for Nanotechnology, Indian Institute of Technology Roorkee, Roorkee, Uttarakhand 247667, India Gopinath, P., Nanobiotechnology Laboratory, Centre for Nanotechnology, Indian Institute of Technology Roorkee, Roorkee, Uttarakhand 247667, India, Department of Biotechnology, Indian Institute of Technology Roorkee, Roorkee, Uttarakhand 247667, India Negi, Y.S., Department of Polymer and Process Engineering, Indian Institute of Technology Roorkee, Roorkee, Uttarakhand 247667, India |
Funding Details: | One of the authors, Mr. Sauraj is highly thankful to the Ministry of Human Resource Development (MHRD), New Delhi for financial support during his Ph.D. program. Authors are also thankful to Sapience bio-analytical research lab (Bhopal, M.P. India) for providing animal facility. Appendix A |
Corresponding Author: | Negi, Y.S.; Department of Polymer and Process Engineering, Indian Institute of Technology RoorkeeIndia; email: yuvrajnegi@gmail.com |
Appears in Collections: | Journal Publications [BT] Journal Publications [PE] |
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