Cationic supramolecular hydrogels for overcoming the skin barrier in drug delivery

Limon, David and Jimenez-Newman, Claire and Rodrigues, Mafalda and Gonzalez-Campo, Arantzazu and Amabilino, David B. and 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

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Abstract

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.

Item Type: Article
Keywords: drug delivery; hydrogels; skin permeation; supramolecular chemistry; surfactants
Schools/Departments: University of Nottingham, UK > Faculty of Science > School of Pharmacy
Identification Number: https://doi.org/10.1002/open.201700040
Depositing User: Perez Garcia, Lluisa
Date Deposited: 05 Feb 2018 10:43
Last Modified: 05 Feb 2018 10:47
URI: http://eprints.nottingham.ac.uk/id/eprint/49509

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