Cationic supramolecular hydrogels for overcoming the skin barrier in drug delivery

A cationic bis-imidazolium-based amphiphile was used to form thermoreversible nanostructured supramolecular hydrogels incorporating neutral and cationic drugs for the topical treatment of rosacea. The concentration of the gelator and the type and concentration of the drug incorporated were found to...

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Main Authors: Limon, David, Jimenez-Newman, Claire, Rodrigues, Mafalda, Gonzalez-Campo, Arantzazu, Amabilino, David B., Calpena, Ana C., Pérez-García, Lluïsa
Format: Article
Published: Wiley Open Access 2017
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Online Access:https://eprints.nottingham.ac.uk/49509/
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author Limon, David
Jimenez-Newman, Claire
Rodrigues, Mafalda
Gonzalez-Campo, Arantzazu
Amabilino, David B.
Calpena, Ana C.
Pérez-García, Lluïsa
author_facet Limon, David
Jimenez-Newman, Claire
Rodrigues, Mafalda
Gonzalez-Campo, Arantzazu
Amabilino, David B.
Calpena, Ana C.
Pérez-García, Lluïsa
author_sort Limon, David
building Nottingham Research Data Repository
collection Online Access
description A cationic bis-imidazolium-based amphiphile was used to form thermoreversible nanostructured supramolecular hydrogels incorporating neutral and cationic drugs for the topical treatment of rosacea. The concentration of the gelator and the type and concentration of the drug incorporated were found to be factors that strongly influenced the gelling temperature, gel-formation period, and overall stability and morphology. The incorporation of brimonidine tartrate resulted in the formation of the most homogeneous material of the three drugs explored, whereas the incorporation of betamethasone resulted in a gel with a completely different morphology comprising linked particles. NMR spectroscopy studies proved that these gels kept the drug not only at the interstitial space but also within the fibers. Due to the design of the gelator, drug release was up to 10 times faster and retention of the drug within the skin was up to 20 times more effective than that observed for commercial products. Experiments in vivo demonstrated the rapid efficacy of these gels in reducing erythema, especially in the case of the gel with brimonidine. The lack of coulombic attraction between the gelator–host and the guest–drug seemed particularly important in highly effective release, and the intermolecular interactions operating between them were found to lie at the root of the excellent properties of the materials for topical delivery and treatment of rosacea.
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spelling nottingham-495092020-05-04T19:07:10Z https://eprints.nottingham.ac.uk/49509/ Cationic supramolecular hydrogels for overcoming the skin barrier in drug delivery Limon, David Jimenez-Newman, Claire Rodrigues, Mafalda Gonzalez-Campo, Arantzazu Amabilino, David B. Calpena, Ana C. Pérez-García, Lluïsa A cationic bis-imidazolium-based amphiphile was used to form thermoreversible nanostructured supramolecular hydrogels incorporating neutral and cationic drugs for the topical treatment of rosacea. The concentration of the gelator and the type and concentration of the drug incorporated were found to be factors that strongly influenced the gelling temperature, gel-formation period, and overall stability and morphology. The incorporation of brimonidine tartrate resulted in the formation of the most homogeneous material of the three drugs explored, whereas the incorporation of betamethasone resulted in a gel with a completely different morphology comprising linked particles. NMR spectroscopy studies proved that these gels kept the drug not only at the interstitial space but also within the fibers. Due to the design of the gelator, drug release was up to 10 times faster and retention of the drug within the skin was up to 20 times more effective than that observed for commercial products. Experiments in vivo demonstrated the rapid efficacy of these gels in reducing erythema, especially in the case of the gel with brimonidine. The lack of coulombic attraction between the gelator–host and the guest–drug seemed particularly important in highly effective release, and the intermolecular interactions operating between them were found to lie at the root of the excellent properties of the materials for topical delivery and treatment of rosacea. Wiley Open Access 2017-09-17 Article PeerReviewed Limon, David, Jimenez-Newman, Claire, Rodrigues, Mafalda, Gonzalez-Campo, Arantzazu, Amabilino, David B., Calpena, Ana C. and Pérez-García, Lluïsa (2017) Cationic supramolecular hydrogels for overcoming the skin barrier in drug delivery. ChemistryOpen, 6 (4). pp. 585-598. ISSN 2191-1363 drug delivery; hydrogels; skin permeation; supramolecular chemistry; surfactants http://onlinelibrary.wiley.com/doi/10.1002/open.201700040/full doi:10.1002/open.201700040 doi:10.1002/open.201700040
spellingShingle drug delivery; hydrogels; skin permeation; supramolecular chemistry; surfactants
Limon, David
Jimenez-Newman, Claire
Rodrigues, Mafalda
Gonzalez-Campo, Arantzazu
Amabilino, David B.
Calpena, Ana C.
Pérez-García, Lluïsa
Cationic supramolecular hydrogels for overcoming the skin barrier in drug delivery
title Cationic supramolecular hydrogels for overcoming the skin barrier in drug delivery
title_full Cationic supramolecular hydrogels for overcoming the skin barrier in drug delivery
title_fullStr Cationic supramolecular hydrogels for overcoming the skin barrier in drug delivery
title_full_unstemmed Cationic supramolecular hydrogels for overcoming the skin barrier in drug delivery
title_short Cationic supramolecular hydrogels for overcoming the skin barrier in drug delivery
title_sort cationic supramolecular hydrogels for overcoming the skin barrier in drug delivery
topic drug delivery; hydrogels; skin permeation; supramolecular chemistry; surfactants
url https://eprints.nottingham.ac.uk/49509/
https://eprints.nottingham.ac.uk/49509/
https://eprints.nottingham.ac.uk/49509/