Antimicrobial Hyperbranched Polymer–Usnic Acid Complexes through a Combined ROP‐RAFT Strategy

Polymer–drug conjugates have received considerable attention over the last decades due to their potential for improving the clinical outcomes for a range of diseases. It is of importance to develop methods for their preparation that have simple synthesis and purification requirements but maintain hi...

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Bibliographic Details
Published in:Macromolecular rapid communications. 2020-09, Vol.41 (18), p.e2000190-n/a
Main Authors: Rauschenbach, Moritz, Lawrenson, Stefan B., Taresco, Vincenzo, Pearce, Amanda K., O'Reilly, Rachel K.
Format: Article
Language:English
Subjects:
Addition polymerization
Antiinfectives and antibacterials
antimicrobials
Biodegradability
Biodegradation
Block copolymers
Chemical synthesis
Conjugates
Copolymers
drug complexation
hyperbranched polymers
Macromolecules
Nanoparticles
Polycarbonate
Polymerization
Polymers
Ring opening polymerization
Usnic acid
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Summary:Polymer–drug conjugates have received considerable attention over the last decades due to their potential for improving the clinical outcomes for a range of diseases. It is of importance to develop methods for their preparation that have simple synthesis and purification requirements but maintain high therapeutic efficacy and utilize macromolecules that can be cleared via natural excretory pathways upon breakdown. Herein, the combination of ring‐opening polymerization (ROP) and reversible addition−fragmentation chain‐transfer (RAFT) polymerization is described for the straightforward synthesis of amphiphilic, stimuli‐responsive, biodegradable, and highly functionalizable hyperbranched polymers. These unimolecular nanoparticles demonstrate a versatile platform for the synthesis of polymer–drug conjugates owing to the inclusion of a Boc‐protected polycarbonate moiety in either a block or random copolymer formation. A proof‐of‐concept study on the complexation of the poorly water‐soluble antimicrobial drug usnic acid results in polymer‐drug complexes with powerful antimicrobial properties against gram‐positive bacteria. Therefore, this work highlights the potential of amphiphilic and biodegradable hyperbranched polymers for antimicrobial applications. This work describes the combination of ring‐opening and reversible addition−fragmentation chain‐transfer polymerizations for the straightforward synthesis of amphiphilic, biodegradable, and highly functionalizable hyperbranched polymers. These unimolecular nanoparticles could complex the poorly water‐soluble antimicrobial drug usnic acid, resulting in polymer–drug complexes with powerful antimicrobial properties against gram‐positive bacteria, highlighting the potential of amphiphilic and biodegradable hyperbranched polymers for antimicrobial applications .
ISSN:1022-1336
1521-3927
DOI:10.1002/marc.202000190