Cyclosporine A micellar delivery system for dry eyes

Han Kang,1,2 Kwang-Ho Cha,1 Wonkyung Cho,1 Junsung Park,1 Hee Jun Park,1 Bo Kyung Sun,1,2 Sang-Min Hyun,1,2 Sung-Joo Hwang1,2 1Yonsei Institute of Pharmaceutical Sciences, 2College of Pharmacy, Yonsei University, Incheon, South Korea Background: The objectives of this study were to develop stable...

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Autores principales:	Kang H, Cha KH, Cho W, Park J, Park HJ, Sun BK, Hyun SM, Hwang SJ
Formato:	article
Lenguaje:	EN
Publicado:	Dove Medical Press 2016
Materias:	cyclosporin A Cremophor EL micelle solution dry eyes Restasis® Medicine (General) R5-920
Acceso en línea:	https://doaj.org/article/d7de07ff24ba46eeba1b00f86a514f56
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spelling	oai:doaj.org-article:d7de07ff24ba46eeba1b00f86a514f562021-12-02T08:07:35ZCyclosporine A micellar delivery system for dry eyes1178-2013https://doaj.org/article/d7de07ff24ba46eeba1b00f86a514f562016-06-01T00:00:00Zhttps://www.dovepress.com/cyclosporine-a-micellar-delivery-system-for-dry-eyes-peer-reviewed-article-IJNhttps://doaj.org/toc/1178-2013Han Kang,1,2 Kwang-Ho Cha,1 Wonkyung Cho,1 Junsung Park,1 Hee Jun Park,1 Bo Kyung Sun,1,2 Sang-Min Hyun,1,2 Sung-Joo Hwang1,2 1Yonsei Institute of Pharmaceutical Sciences, 2College of Pharmacy, Yonsei University, Incheon, South Korea Background: The objectives of this study were to develop stable cyclosporine A (CsA) ophthalmic micelle solutions for dry-eye syndrome and evaluate their physicochemical properties and therapeutic efficacy. Materials and methods: CsA-micelle solutions (MS-CsA) were created by a simple method with Cremophor EL, ethanol, and phosphate buffer. We investigated the particle size, pH, and osmolarity. In addition, long-term physical and chemical stability for MS-CsA was observed. To confirm the therapeutic efficacy, tear production in dry eye-induced rabbits was evaluated using the Schirmer tear test (STT). When compared to a commercial product, Restasis, MS-CsA demonstrated improvement in goblet-cell density and conjunctival epithelial morphology, as demonstrated in histological hematoxylin and eosin staining. Results: MS-CsA had a smaller particle size (average diameter 14–18 nm) and a narrow size distribution. Physicochemical parameters, such as particle size, pH, osmolarity, and remaining CsA concentration were all within the expected range of 60 days. STT scores significantly improved in MS-CsA treated groups (P<0.05) in comparison to those of the Restasis-treated group. The number of goblet cells for rabbit conjunctivas after the administration of MS-CsA was 94.83±8.38, a significantly higher result than the 65.17±11.51 seen with Restasis. The conjunctival epithelial morphology of dry eye-induced rabbits thinned with loss of goblet cells. However, after 5 days of treatment with drug formulations, rabbit conjunctivas recovered epithelia and showed a relative increase in the number of goblet cells. Conclusion: The results of this study indicate the potential use of a novel MS for the ophthalmic delivery of CsA in treating dry eyes. Keywords: cyclosporine A, Cremophor EL, micelle solution, dry eyes, RestasisKang HCha KHCho WPark JPark HJSun BKHyun SMHwang SJDove Medical Pressarticlecyclosporin ACremophor ELmicelle solutiondry eyesRestasis®Medicine (General)R5-920ENInternational Journal of Nanomedicine, Vol 2016, Iss default, Pp 2921-2933 (2016)
institution	DOAJ
collection	DOAJ
language	EN
topic	cyclosporin A Cremophor EL micelle solution dry eyes Restasis® Medicine (General) R5-920
spellingShingle	cyclosporin A Cremophor EL micelle solution dry eyes Restasis® Medicine (General) R5-920 Kang H Cha KH Cho W Park J Park HJ Sun BK Hyun SM Hwang SJ Cyclosporine A micellar delivery system for dry eyes
description	Han Kang,1,2 Kwang-Ho Cha,1 Wonkyung Cho,1 Junsung Park,1 Hee Jun Park,1 Bo Kyung Sun,1,2 Sang-Min Hyun,1,2 Sung-Joo Hwang1,2 1Yonsei Institute of Pharmaceutical Sciences, 2College of Pharmacy, Yonsei University, Incheon, South Korea Background: The objectives of this study were to develop stable cyclosporine A (CsA) ophthalmic micelle solutions for dry-eye syndrome and evaluate their physicochemical properties and therapeutic efficacy. Materials and methods: CsA-micelle solutions (MS-CsA) were created by a simple method with Cremophor EL, ethanol, and phosphate buffer. We investigated the particle size, pH, and osmolarity. In addition, long-term physical and chemical stability for MS-CsA was observed. To confirm the therapeutic efficacy, tear production in dry eye-induced rabbits was evaluated using the Schirmer tear test (STT). When compared to a commercial product, Restasis, MS-CsA demonstrated improvement in goblet-cell density and conjunctival epithelial morphology, as demonstrated in histological hematoxylin and eosin staining. Results: MS-CsA had a smaller particle size (average diameter 14–18 nm) and a narrow size distribution. Physicochemical parameters, such as particle size, pH, osmolarity, and remaining CsA concentration were all within the expected range of 60 days. STT scores significantly improved in MS-CsA treated groups (P<0.05) in comparison to those of the Restasis-treated group. The number of goblet cells for rabbit conjunctivas after the administration of MS-CsA was 94.83±8.38, a significantly higher result than the 65.17±11.51 seen with Restasis. The conjunctival epithelial morphology of dry eye-induced rabbits thinned with loss of goblet cells. However, after 5 days of treatment with drug formulations, rabbit conjunctivas recovered epithelia and showed a relative increase in the number of goblet cells. Conclusion: The results of this study indicate the potential use of a novel MS for the ophthalmic delivery of CsA in treating dry eyes. Keywords: cyclosporine A, Cremophor EL, micelle solution, dry eyes, Restasis
format	article
author	Kang H Cha KH Cho W Park J Park HJ Sun BK Hyun SM Hwang SJ
author_facet	Kang H Cha KH Cho W Park J Park HJ Sun BK Hyun SM Hwang SJ
author_sort	Kang H
title	Cyclosporine A micellar delivery system for dry eyes
title_short	Cyclosporine A micellar delivery system for dry eyes
title_full	Cyclosporine A micellar delivery system for dry eyes
title_fullStr	Cyclosporine A micellar delivery system for dry eyes
title_full_unstemmed	Cyclosporine A micellar delivery system for dry eyes
title_sort	cyclosporine a micellar delivery system for dry eyes
publisher	Dove Medical Press
publishDate	2016
url	https://doaj.org/article/d7de07ff24ba46eeba1b00f86a514f56
work_keys_str_mv	AT kangh cyclosporineamicellardeliverysystemfordryeyes AT chakh cyclosporineamicellardeliverysystemfordryeyes AT chow cyclosporineamicellardeliverysystemfordryeyes AT parkj cyclosporineamicellardeliverysystemfordryeyes AT parkhj cyclosporineamicellardeliverysystemfordryeyes AT sunbk cyclosporineamicellardeliverysystemfordryeyes AT hyunsm cyclosporineamicellardeliverysystemfordryeyes AT hwangsj cyclosporineamicellardeliverysystemfordryeyes
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Cyclosporine A micellar delivery system for dry eyes

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