Unraveling the Effect of Nondrug Spacers on a True Drug-Polymer and a Comparative Study of Their Antimicrobial Activity AITranslate

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DOI：https://doi.org/10.1021/acsapm.2c00413

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Several studies have been conducted on the polymerization of drug units using spacers or other polymeric units. In order to study the importance of spacers in drug-polymers, we designed polymers with and without spacers. As a proof of concept, herein, we present a comparative study on the efficacy of antibacterial activity using a polymeric biocide (PB) C0P1 having no spacer (0%) and two other PBs with varied spacer content (C2P2:29%, C10P3:53%). We considered C0P1 as a potential new type of PB generated from a widely used fluoroquinolone antibiotic, ciprofloxacin 1, by a simple self-condensation activation with thionyl chloride. Monomer 2 (formylated methyl ester of 1) was polymerized with ethylenediamine (C2) and 1,10-diaminodecane (C10) to provide C2P2 and C10P3, respectively. The trend for minimum inhibitory concentration study against Escherichia coli (E. coli) and Staphylococcus aureus (S. aureus) was observed as 1 > C0P1 > C2P2 = C10P3>> 2. Furthermore, after coating on nylon threads, the nonspacer polymer C0P1 showed an enhanced zone of inhibition (ZOI) than monomer 1 as well as the spacer polymers owing to its superior coating ability and sustained drug release capabilities. Thus, this study clearly states that the bioefficacy of a drug-polymer could be retained and enhanced in the absence of nonbioactive spacer units.