Biocompatible unimolecular micelles obtained via the Passerini reaction as versatile nanocarriers for potential medical applications

A Passerini three-component polymerization was performed for the synthesis of amphiphilic star-shaped block copolymers with hydrophobic cores and hydrophilic coronae. The degree of polymerization of the hydrophobic core was varied from 5 to 10 repeating units, and the side chain ends were conjugated...

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Main Authors: Oelmann, Stefan, Travanut, Alessandra, Barther, Dennis, Romero, Manuel, Howdle, Steven M., Alexander, Cameron, Meier, Michael A.R.
Format: Article
Published: American Chemical Society 2018
Online Access:https://eprints.nottingham.ac.uk/53154/
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author Oelmann, Stefan
Travanut, Alessandra
Barther, Dennis
Romero, Manuel
Howdle, Steven M.
Alexander, Cameron
Meier, Michael A.R.
author_facet Oelmann, Stefan
Travanut, Alessandra
Barther, Dennis
Romero, Manuel
Howdle, Steven M.
Alexander, Cameron
Meier, Michael A.R.
author_sort Oelmann, Stefan
building Nottingham Research Data Repository
collection Online Access
description A Passerini three-component polymerization was performed for the synthesis of amphiphilic star-shaped block copolymers with hydrophobic cores and hydrophilic coronae. The degree of polymerization of the hydrophobic core was varied from 5 to 10 repeating units, and the side chain ends were conjugated by performing a Passerini-3CR with PEG-isocyanide and PEG-aldehyde (950 g/mol). The resulting amphiphilic star-shaped block copolymers contained thioether groups, which could be oxidized to sulfones in order to further tune the polarity of the polymer chains. The ability of the amphiphilic copolymers to act as unimolecular micellar encapsulants was tested with the water-insoluble dye Orange II, the water-soluble dye Para Red and the macrolide antibiotic azithromycin. The results showed that the new copolymers were able to retain drug cargo at pH levels corresponding to circulating blood and selectively release therapeutically effective doses of antibiotic as measured by bacterial cell kill. The polymers were also well-tolerated by differentiated THP-1 macrophages in the absence of encapsulated drugs.
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spelling nottingham-531542020-05-04T19:39:31Z https://eprints.nottingham.ac.uk/53154/ Biocompatible unimolecular micelles obtained via the Passerini reaction as versatile nanocarriers for potential medical applications Oelmann, Stefan Travanut, Alessandra Barther, Dennis Romero, Manuel Howdle, Steven M. Alexander, Cameron Meier, Michael A.R. A Passerini three-component polymerization was performed for the synthesis of amphiphilic star-shaped block copolymers with hydrophobic cores and hydrophilic coronae. The degree of polymerization of the hydrophobic core was varied from 5 to 10 repeating units, and the side chain ends were conjugated by performing a Passerini-3CR with PEG-isocyanide and PEG-aldehyde (950 g/mol). The resulting amphiphilic star-shaped block copolymers contained thioether groups, which could be oxidized to sulfones in order to further tune the polarity of the polymer chains. The ability of the amphiphilic copolymers to act as unimolecular micellar encapsulants was tested with the water-insoluble dye Orange II, the water-soluble dye Para Red and the macrolide antibiotic azithromycin. The results showed that the new copolymers were able to retain drug cargo at pH levels corresponding to circulating blood and selectively release therapeutically effective doses of antibiotic as measured by bacterial cell kill. The polymers were also well-tolerated by differentiated THP-1 macrophages in the absence of encapsulated drugs. American Chemical Society 2018-06-05 Article PeerReviewed Oelmann, Stefan, Travanut, Alessandra, Barther, Dennis, Romero, Manuel, Howdle, Steven M., Alexander, Cameron and Meier, Michael A.R. (2018) Biocompatible unimolecular micelles obtained via the Passerini reaction as versatile nanocarriers for potential medical applications. Biomacromolecules . ISSN 1526-4602 http://dx.doi.org/10.1021/acs.biomac.8b00592 doi:10.1021/acs.biomac.8b00592 doi:10.1021/acs.biomac.8b00592
spellingShingle Oelmann, Stefan
Travanut, Alessandra
Barther, Dennis
Romero, Manuel
Howdle, Steven M.
Alexander, Cameron
Meier, Michael A.R.
Biocompatible unimolecular micelles obtained via the Passerini reaction as versatile nanocarriers for potential medical applications
title Biocompatible unimolecular micelles obtained via the Passerini reaction as versatile nanocarriers for potential medical applications
title_full Biocompatible unimolecular micelles obtained via the Passerini reaction as versatile nanocarriers for potential medical applications
title_fullStr Biocompatible unimolecular micelles obtained via the Passerini reaction as versatile nanocarriers for potential medical applications
title_full_unstemmed Biocompatible unimolecular micelles obtained via the Passerini reaction as versatile nanocarriers for potential medical applications
title_short Biocompatible unimolecular micelles obtained via the Passerini reaction as versatile nanocarriers for potential medical applications
title_sort biocompatible unimolecular micelles obtained via the passerini reaction as versatile nanocarriers for potential medical applications
url https://eprints.nottingham.ac.uk/53154/
https://eprints.nottingham.ac.uk/53154/
https://eprints.nottingham.ac.uk/53154/