Design, Synthesis and In-Vitro Evaluation of Polymer-linked Prodrug of Methotrexate for the Targeted Delivery to the Colon
Nishu Singla, Rajiv Sharma and T.R. Bhardwaj
Affiliation: 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.
Keywords: Cancer, Chitosan, Drug conjugate, Polyphosphazene, Polymer, Prodrug.
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.
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