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Triclosan nanoparticles via emulsion-freeze-drying for enhanced antimicrobial activity

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Abstract

Low water solubility and poor bioavailability of hydrophobic pharmaceuticals are significant problems in drug formulation. This research presents a bottom-up route to prepare nanoparticles of hydrophobic actives which is synthetically straightforward, robust, and can be applied to a range of active molecules. A series of amphiphilic branched diblock copolymers have been prepared via the conventional radical polymerization of a vinyl monomer (styrene, butylmethacrylate, or N-isopropylacrylamide) and a corresponding divinyl cross-linker facilitated by a poly(ethylene glycol)-based macro-initiator. These materials were employed as stabilizers in the emulsion-freeze-drying methodology to prepare nanoparticles of hydrophobic pharmaceuticals. It is demonstrated that these branched diblock copolymers are able to facilitate the formation of Triclosan nanoparticles which display enhanced antimicrobial activity against Candida albicans, when compared to non-processed (used as received) Triclosan. This process requires significantly lower levels of stabilizer compared to previously reported surfactant/polymer systems after optimization of polymer properties and morphology.

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Acknowledgments

Ulrike Wais acknowledges the joint PhD studentship between the University of Liverpool and the A*Star Research Attachment Program (ARAP) scholarship. The authors would like to thank Wendy Rusli (of A* Star, Institute of Chemical and Engineering Sciences) for performing cryo-TEM analysis.

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Authors and Affiliations

  1. Department of Chemistry, University of Liverpool, Liverpool, L69 7ZD, UK

    Ulrike Wais & Haifei Zhang

  2. Institute of Chemical and Engineering Science, 1 Pesek Road, Jurong Island, 627833, Singapore

    Ulrike Wais, Margarete M. Nawrath & Alexander W. Jackson

  3. Institute of Biochemistry, University of Leipzig, 04103, Leipzig, Germany

    Margarete M. Nawrath

Authors
  1. Ulrike Wais
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  2. Margarete M. Nawrath
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  3. Alexander W. Jackson
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  4. Haifei Zhang
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Correspondence to Alexander W. Jackson or Haifei Zhang.

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1H NMR spectra, and additional optical microscopy and SEM image (DOCX 1640 kb)

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Wais, U., Nawrath, M.M., Jackson, A.W. et al. Triclosan nanoparticles via emulsion-freeze-drying for enhanced antimicrobial activity. Colloid Polym Sci 296, 951–960 (2018). https://doi.org/10.1007/s00396-018-4312-0

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  • DOI: https://doi.org/10.1007/s00396-018-4312-0

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