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Letters in Drug Design & Discovery
ISSN (Print): 1570-1808
ISSN (Online): 1875-628X
DOI: 10.2174/1570180811666131217002719      Price:  $58

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
Pages 601-610 (10)
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.
Cancer, Chitosan, Drug conjugate, Polyphosphazene, Polymer, Prodrug.
Polymer Chemistry and Technology Research Laboratory, Department of Pharmaceutical Chemistry, Indo- Soviet friendship (I.S.F) College of Pharmacy, Ferozepur Road, Moga-142 001, India.