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Cyclosporine Amicellar delivery system for dry eyes
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 Cr...
Autores principales: | , , , , , , , |
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Formato: | Online Artículo Texto |
Lenguaje: | English |
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Dove Medical Press
2016
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Materias: | |
Acceso en línea: | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC4922772/ https://www.ncbi.nlm.nih.gov/pubmed/27382280 http://dx.doi.org/10.2147/IJN.S107569 |
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author | Kang, Han Cha, Kwang-Ho Cho, Wonkyung Park, Junsung Park, Hee Jun Sun, Bo Kyung Hyun, Sang-Min Hwang, Sung-Joo |
author_facet | Kang, Han Cha, Kwang-Ho Cho, Wonkyung Park, Junsung Park, Hee Jun Sun, Bo Kyung Hyun, Sang-Min Hwang, Sung-Joo |
author_sort | Kang, Han |
collection | PubMed |
description | 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. |
format | Online Article Text |
id | pubmed-4922772 |
institution | National Center for Biotechnology Information |
language | English |
publishDate | 2016 |
publisher | Dove Medical Press |
record_format | MEDLINE/PubMed |
spelling | pubmed-49227722016-07-05 Cyclosporine Amicellar delivery system for dry eyes Kang, Han Cha, Kwang-Ho Cho, Wonkyung Park, Junsung Park, Hee Jun Sun, Bo Kyung Hyun, Sang-Min Hwang, Sung-Joo Int J Nanomedicine Original Research 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. Dove Medical Press 2016-06-21 /pmc/articles/PMC4922772/ /pubmed/27382280 http://dx.doi.org/10.2147/IJN.S107569 Text en © 2016 Kang et al. This work is published and licensed by Dove Medical Press Limited The full terms of this license are available at https://www.dovepress.com/terms.php and incorporate the Creative Commons Attribution – Non Commercial (unported, v3.0) License (http://creativecommons.org/licenses/by-nc/3.0/). By accessing the work you hereby accept the Terms. Non-commercial uses of the work are permitted without any further permission from Dove Medical Press Limited, provided the work is properly attributed. |
spellingShingle | Original Research Kang, Han Cha, Kwang-Ho Cho, Wonkyung Park, Junsung Park, Hee Jun Sun, Bo Kyung Hyun, Sang-Min Hwang, Sung-Joo Cyclosporine Amicellar delivery system for dry eyes |
title | Cyclosporine Amicellar delivery system for dry eyes |
title_full | Cyclosporine Amicellar delivery system for dry eyes |
title_fullStr | Cyclosporine Amicellar delivery system for dry eyes |
title_full_unstemmed | Cyclosporine Amicellar delivery system for dry eyes |
title_short | Cyclosporine Amicellar delivery system for dry eyes |
title_sort | cyclosporine amicellar delivery system for dry eyes |
topic | Original Research |
url | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC4922772/ https://www.ncbi.nlm.nih.gov/pubmed/27382280 http://dx.doi.org/10.2147/IJN.S107569 |
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