Citric acid is more effective than sodium thiosulfate in chelating calcium in a dissolution model of calcinosis

Abstract Calcinosis cutis affects 20–40% of patients with systemic sclerosis. This study tests the hypothesis that calcium-chelating polycarboxylic acids can induce calcium dissolution without skin toxicity or irritancy. We compared citric acid (CA) and ethylenediaminetetraacetic acid (EDTA) to sodi...

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Main Authors: Kyle A. Burgess, Richard E. P. Winpenny, Alberto Saiani, Aline F. Miller, Ariane L. Herrick, Rachel E. B. Watson
Format: Article
Language:English
Published: Nature Portfolio 2024-12-01
Series:Scientific Reports
Online Access:https://doi.org/10.1038/s41598-024-65761-3
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author Kyle A. Burgess
Richard E. P. Winpenny
Alberto Saiani
Aline F. Miller
Ariane L. Herrick
Rachel E. B. Watson
author_facet Kyle A. Burgess
Richard E. P. Winpenny
Alberto Saiani
Aline F. Miller
Ariane L. Herrick
Rachel E. B. Watson
author_sort Kyle A. Burgess
collection DOAJ
description Abstract Calcinosis cutis affects 20–40% of patients with systemic sclerosis. This study tests the hypothesis that calcium-chelating polycarboxylic acids can induce calcium dissolution without skin toxicity or irritancy. We compared citric acid (CA) and ethylenediaminetetraacetic acid (EDTA) to sodium thiosulfate (STS) for their ability to chelate calcium in vitro using a pharmaceutical dissolution model of calcinosis (hydroxyapatite (HAp) tablet), prior to evaluation of toxicity and irritancy in 2D in vitro skin models. Resultant data was used to predict therapeutic concentrations for application in a validated 3D skin irritation model (SkinEthic™; EpiSkin SA) and to assay maximal percutaneous absorption. Dissolution performance was further assessed via ability to dissolve a calcified matrix laid down in vitro. Pharmacological dissolution studies identified that polycarboxylic acids were superior to STS in dissolving HAp tablets. In vitro, compounds had little effect on cell numbers at concentrations of < 10 mM. When applied topically to 3D models as near-saturated solutions, chelators were not irritant nor did they impact model structure histologically. CA was the most efficient chelator of calcium salts. This study highlights polycarboxylic acids, particularly CA, as potential therapies to target calcinosis cutis: these should now be investigated in human studies.
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spelling doaj-art-c4f8ceec09ba4d7ca85689d798137dfa2024-12-29T12:18:39ZengNature PortfolioScientific Reports2045-23222024-12-0114111010.1038/s41598-024-65761-3Citric acid is more effective than sodium thiosulfate in chelating calcium in a dissolution model of calcinosisKyle A. Burgess0Richard E. P. Winpenny1Alberto Saiani2Aline F. Miller3Ariane L. Herrick4Rachel E. B. Watson5Division of Musculoskeletal and Dermatological Sciences, School of Biological Sciences, Faculty of Biology, Medicine and Health, The University of Manchester and Northern Care Alliance NHS Foundation Trust, Manchester Academic Health Science CentreDepartment of Chemistry, The University of ManchesterDepartment of Materials, The University of ManchesterManchester Institute of Biotechnology, Department of Chemical Engineering, School of Engineering, The University of ManchesterDivision of Musculoskeletal and Dermatological Sciences, School of Biological Sciences, Faculty of Biology, Medicine and Health, The University of Manchester and Northern Care Alliance NHS Foundation Trust, Manchester Academic Health Science CentreDivision of Musculoskeletal and Dermatological Sciences, School of Biological Sciences, Faculty of Biology, Medicine and Health, The University of Manchester and Northern Care Alliance NHS Foundation Trust, Manchester Academic Health Science CentreAbstract Calcinosis cutis affects 20–40% of patients with systemic sclerosis. This study tests the hypothesis that calcium-chelating polycarboxylic acids can induce calcium dissolution without skin toxicity or irritancy. We compared citric acid (CA) and ethylenediaminetetraacetic acid (EDTA) to sodium thiosulfate (STS) for their ability to chelate calcium in vitro using a pharmaceutical dissolution model of calcinosis (hydroxyapatite (HAp) tablet), prior to evaluation of toxicity and irritancy in 2D in vitro skin models. Resultant data was used to predict therapeutic concentrations for application in a validated 3D skin irritation model (SkinEthic™; EpiSkin SA) and to assay maximal percutaneous absorption. Dissolution performance was further assessed via ability to dissolve a calcified matrix laid down in vitro. Pharmacological dissolution studies identified that polycarboxylic acids were superior to STS in dissolving HAp tablets. In vitro, compounds had little effect on cell numbers at concentrations of < 10 mM. When applied topically to 3D models as near-saturated solutions, chelators were not irritant nor did they impact model structure histologically. CA was the most efficient chelator of calcium salts. This study highlights polycarboxylic acids, particularly CA, as potential therapies to target calcinosis cutis: these should now be investigated in human studies.https://doi.org/10.1038/s41598-024-65761-3
spellingShingle Kyle A. Burgess
Richard E. P. Winpenny
Alberto Saiani
Aline F. Miller
Ariane L. Herrick
Rachel E. B. Watson
Citric acid is more effective than sodium thiosulfate in chelating calcium in a dissolution model of calcinosis
Scientific Reports
title Citric acid is more effective than sodium thiosulfate in chelating calcium in a dissolution model of calcinosis
title_full Citric acid is more effective than sodium thiosulfate in chelating calcium in a dissolution model of calcinosis
title_fullStr Citric acid is more effective than sodium thiosulfate in chelating calcium in a dissolution model of calcinosis
title_full_unstemmed Citric acid is more effective than sodium thiosulfate in chelating calcium in a dissolution model of calcinosis
title_short Citric acid is more effective than sodium thiosulfate in chelating calcium in a dissolution model of calcinosis
title_sort citric acid is more effective than sodium thiosulfate in chelating calcium in a dissolution model of calcinosis
url https://doi.org/10.1038/s41598-024-65761-3
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