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Letters in Drug Design & Discovery


ISSN (Print): 1570-1808
ISSN (Online): 1875-628X

Design, Synthesis and In-Vitro Evaluation of Polymer-linked Prodrug of Methotrexate for the Targeted Delivery to the Colon

Author(s): Nishu Singla, Rajiv Sharma and T.R. Bhardwaj

Volume 11 , Issue 5 , 2014

Page: [601 - 610] Pages: 10

DOI: 10.2174/1570180811666131217002719

Price: $65


The different substituted polyphosphazene-linked azo prodrug of Methotrexate (9-12) and chitosan-linked azo prodrug of methotrexate (13) were synthesized and characterized by modern analytical techniques such as IR, 1H NMR, 31P NMR and GPC. The in-vitro stability study showed that all polymeric drug conjugates are stable in upper GIT (pH = 1.2) and small intestine (pH = 7.4). In-vitro drug release showed that polyphosphazene-linked azo prodrug of methotrexate (12) has maximum release (88.4%) in the presence of rat cecal content compared to chitosan linked azo prodrug of methotrexate (13). Therefore, the synthesized polyphosphazene linked azo based drug conjugates of methotrexate (9-12) are the potential candidates for colon targeted drug delivery system with minimal undesirable side effects.

Keywords: Cancer, Chitosan, Drug conjugate, Polyphosphazene, Polymer, Prodrug.

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