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

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

Volume: 11 Issue: 5

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

Affiliation:

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

Abstract: 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.

Cite this article as:

Singla Nishu, Sharma Rajiv and Bhardwaj T.R., Design, Synthesis and In-Vitro Evaluation of Polymer-linked Prodrug of Methotrexate for the Targeted Delivery to the Colon, Letters in Drug Design & Discovery 2014; 11 (5) . https://dx.doi.org/10.2174/1570180811666131217002719