Sustained release of antibacterial lipopeptides from biodegradable polymers against oral pathogens

Lea H. Eckhard, Yael Houri-Haddad, Asaf Sol, Rotem Zeharia, Yechiel Shai, Shaul Beyth, Abraham J. Domb, Gilad Bachrach, Nurit Beyth

Research output: Contribution to journalArticlepeer-review

12 Scopus citations


The development of antibacterial drugs to overcome various pathogenic species, which inhabit the oral cavity, faces several challenges, such as salivary flow and enzymatic activity that restrict dosage retention. Owing to their amphipathic nature, antimicrobial peptides (AMPs) serve as the first line of defense of the innate immune system. The ability to synthesize different types of AMPs enables exploitation of their advantages as alternatives to antibiotics. Sustained release of AMPs incorporated in biodegradable polymers can be advantageous in maintaining high levels of the peptides. In this study, four potent ultra-short lipopeptides, conjugated to an aliphatic acid chain (16C) were incorporated in two different biodegradable polymers: poly (lactic acid co castor oil) (PLACO) and ricinoleic acid-based poly (ester-anhydride) (P(SA-RA)) for sustained release. The lipopeptide and polymer formulations were tested for antibacterial activity during one week, by turbidometric measurements of bacterial outgrowth, anti-biofilm activity by live/dead staining, biocompatibility by hemolysis and XTT colorimetric assays, mode of action by fluorescence-activated cell sorting (FACS) and release profile by a fluorometric assay. The results show that an antibacterial and anti-biofilm effect, as well as membrane disruption, can be achieved by the use of a formulation of lipopeptide incorporated in biodegradable polymer.

Original languageEnglish
Article numbere0162537
JournalPLoS ONE
Issue number9
StatePublished - Sep 2016
Externally publishedYes

Bibliographical note

Publisher Copyright:
© 2016 Eckhard et al. This is an open access article distributed under the terms of the Creative Commons Attribution License, which permits unrestricted use, distribution, and reproduction in any medium, provided the original author and source are credited.


This research was supported by The Legacy Heritage Clinical Research Initiative of the Israel Science Foundation (Grant No.1764/11). The authors would like to thank Ester Abtew for her help in preparing the polymers.

FundersFunder number
Israel Science Foundation1764/11


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