Development of a chiral HPLC method for the separation and quantification of hydroxychloroquine enantiomers

Abstract Hydroxychloroquine (2-[[4-[(7-Chloroquinolin-4-yl) amino]pentyl](ethyl) amino]-ethanol, HCQ), an effective anti-malarial drug, has been tested in the clinics for potential treatment of severe coronavirus disease 2019 (COVID-19). Despite the controversy around the clinical benefits of HCQ, t...

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Autores principales:	Xisheng Xiong, Kun Wang, Tao Tang, Jinzhi Fang, Yijun Chen
Formato:	article
Lenguaje:	EN
Publicado:	Nature Portfolio 2021
Materias:	Medicine R Science Q
Acceso en línea:	https://doaj.org/article/e54785540d284a2aa92dfad0c0791fb2
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spelling	oai:doaj.org-article:e54785540d284a2aa92dfad0c0791fb22021-12-02T14:26:13ZDevelopment of a chiral HPLC method for the separation and quantification of hydroxychloroquine enantiomers10.1038/s41598-021-87511-52045-2322https://doaj.org/article/e54785540d284a2aa92dfad0c0791fb22021-04-01T00:00:00Zhttps://doi.org/10.1038/s41598-021-87511-5https://doaj.org/toc/2045-2322Abstract Hydroxychloroquine (2-[[4-[(7-Chloroquinolin-4-yl) amino]pentyl](ethyl) amino]-ethanol, HCQ), an effective anti-malarial drug, has been tested in the clinics for potential treatment of severe coronavirus disease 2019 (COVID-19). Despite the controversy around the clinical benefits of HCQ, the existence of a chiral center in the molecule to possess two optical isomers suggests that there might be an enantiomeric difference on the treatment of COVID-19. Due to their poor resolution and the inability of quantification by previously reported methods for the analysis of HCQ enantiomers, it is necessary to develop an analytical method to achieve baseline separation for quantitative and accurate determination of the enantiomeric purity in order to compare the efficacy and toxicity profiles of different enantiomers. In this study, we developed and validated an accurate and reproducible normal phase chiral high-performance liquid chromatography (HPLC) method for the analysis of two enantiomers of HCQ, and the method was further evaluated with biological samples. With this newly developed method, the relative standard deviations of all analytes were lower than 5%, and the limits of quantification were 0.27 μg/ml, 0.34 μg/ml and 0.20 μg/ml for racemate, R- and S-enantiomer, respectively. The present method provides an essential analytical tool for preclinical and clinical evaluation of HCQ enantiomers for potential treatment of COVID-19.Xisheng XiongKun WangTao TangJinzhi FangYijun ChenNature PortfolioarticleMedicineRScienceQENScientific Reports, Vol 11, Iss 1, Pp 1-7 (2021)
institution	DOAJ
collection	DOAJ
language	EN
topic	Medicine R Science Q
spellingShingle	Medicine R Science Q Xisheng Xiong Kun Wang Tao Tang Jinzhi Fang Yijun Chen Development of a chiral HPLC method for the separation and quantification of hydroxychloroquine enantiomers
description	Abstract Hydroxychloroquine (2-[[4-[(7-Chloroquinolin-4-yl) amino]pentyl](ethyl) amino]-ethanol, HCQ), an effective anti-malarial drug, has been tested in the clinics for potential treatment of severe coronavirus disease 2019 (COVID-19). Despite the controversy around the clinical benefits of HCQ, the existence of a chiral center in the molecule to possess two optical isomers suggests that there might be an enantiomeric difference on the treatment of COVID-19. Due to their poor resolution and the inability of quantification by previously reported methods for the analysis of HCQ enantiomers, it is necessary to develop an analytical method to achieve baseline separation for quantitative and accurate determination of the enantiomeric purity in order to compare the efficacy and toxicity profiles of different enantiomers. In this study, we developed and validated an accurate and reproducible normal phase chiral high-performance liquid chromatography (HPLC) method for the analysis of two enantiomers of HCQ, and the method was further evaluated with biological samples. With this newly developed method, the relative standard deviations of all analytes were lower than 5%, and the limits of quantification were 0.27 μg/ml, 0.34 μg/ml and 0.20 μg/ml for racemate, R- and S-enantiomer, respectively. The present method provides an essential analytical tool for preclinical and clinical evaluation of HCQ enantiomers for potential treatment of COVID-19.
format	article
author	Xisheng Xiong Kun Wang Tao Tang Jinzhi Fang Yijun Chen
author_facet	Xisheng Xiong Kun Wang Tao Tang Jinzhi Fang Yijun Chen
author_sort	Xisheng Xiong
title	Development of a chiral HPLC method for the separation and quantification of hydroxychloroquine enantiomers
title_short	Development of a chiral HPLC method for the separation and quantification of hydroxychloroquine enantiomers
title_full	Development of a chiral HPLC method for the separation and quantification of hydroxychloroquine enantiomers
title_fullStr	Development of a chiral HPLC method for the separation and quantification of hydroxychloroquine enantiomers
title_full_unstemmed	Development of a chiral HPLC method for the separation and quantification of hydroxychloroquine enantiomers
title_sort	development of a chiral hplc method for the separation and quantification of hydroxychloroquine enantiomers
publisher	Nature Portfolio
publishDate	2021
url	https://doaj.org/article/e54785540d284a2aa92dfad0c0791fb2
work_keys_str_mv	AT xishengxiong developmentofachiralhplcmethodfortheseparationandquantificationofhydroxychloroquineenantiomers AT kunwang developmentofachiralhplcmethodfortheseparationandquantificationofhydroxychloroquineenantiomers AT taotang developmentofachiralhplcmethodfortheseparationandquantificationofhydroxychloroquineenantiomers AT jinzhifang developmentofachiralhplcmethodfortheseparationandquantificationofhydroxychloroquineenantiomers AT yijunchen developmentofachiralhplcmethodfortheseparationandquantificationofhydroxychloroquineenantiomers
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Development of a chiral HPLC method for the separation and quantification of hydroxychloroquine enantiomers

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