Pharmaceutical Functionalization of Monomeric Ionic Liquid for the Preparation of Ionic Graft Polymer Conjugates

Polymerizable choline-based ionic liquid (IL), i.e., [2-(methacryloyloxy)ethyl]-trimethylammonium (TMAMA/Cl over bar ), was functionalized by an ion exchange reaction with pharmaceutical anions, i.e., cloxacillin (CLX over bar ) and fusidate (FUS over bar ), as the antibacterial agents. The modified biocompatible IL monomers (TMAMA/CLX over bar , TMAMA/FUS over bar ) were copolymerized with methyl methacrylate (MMA) to prepare the graft copolymers (19-50 mol% of TMAMA units) serving as the drug (co)delivery systems. The in vitro drug release, which was driven by the exchange reaction of the pharmaceutical anions to phosphate ones in PBS medium, was observed for 44% of CLX over bar (2.7 mu g/mL) and 53% of FUS over bar (3.6 mu g/mL) in the single systems. Similar amounts of released drugs were detected for the dual system, i.e., 41% of CLX over bar (2.2 mu g/mL) and 33% of FUS over bar (2.0 mu g/mL). The investigated drug ionic polymer conjugates were examined for their cytotoxicity by MTT test, showing a low toxic effect against human bronchial epithelial cells (BEAS-2B) and normal human dermal fibroblasts (NHDF) as the normal cell lines. The satisfactory drug contents and the release profiles attained for the well-defined graft polymers with ionically bonded pharmaceuticals in the side chains make them promising drug carriers in both separate and combined drug delivery systems.

Automated summary

In this study, polymerizable choline-based ionic liquid was functionalized with pharmaceutical anions to prepare drug delivery systems. The in vitro drug release was observed and low cytotoxicity was found for normal cell lines.