Synthesis and in vitro Antimicrobial Activity of Chloramphenicol- Conjugated Copolymers

Abstract

Two copolymers of maleic anhydride, 10-undecendyl chloride-co- maleic anhydride and acryloyl chloride-co-maleic anhydride, were synthesized, esterified with chloramphenicol, and tested for antimicrobial activity via Kirby-Bauer disk sensitivity and broth dilution methods. Both polymer-drug conjugates exhibited antimicrobial activities of at least 10% of that exhibited by unconjugated chloramphenicol. As maleic anhydride copolymers are taken up selectively by macrophages, they should be effective in concentrating the an tibiotic in these cells allowing for its use at lower dosage. Such agents might prove effective in treating diseases such as legionellosis with fewer toxic side- effects such as aplastic anemia.