Safety comparison of additives in antiglaucoma prostaglandin (PG) analog ophthalmic formulations

Masamichi Fukuda, Shinsuke Shibata, Naoko Shibata, Kenta Hagihara, Hiromoto Yaguchi, Hiromi Osada, Nobuo Takahashi, Eri Kubo, Hiroshi SasakiDepartment of Ophthalmology, Kanazawa Medical University, Uchinada, JapanPurpose: To investigate the safety of five types of antiglaucoma prostaglandin analog o...

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Autores principales:	Fukuda M, Shibata S, Shibata N, Hagihara K, Yaguchi H, Osada H, Takahashi N, Kubo E, Sasaki H
Formato:	article
Lenguaje:	EN
Publicado:	Dove Medical Press 2013
Materias:	Ophthalmology RE1-994
Acceso en línea:	https://doaj.org/article/3855b2f9298c4cd7a0932b2ee13b91da
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spelling	oai:doaj.org-article:3855b2f9298c4cd7a0932b2ee13b91da2021-12-02T04:13:06ZSafety comparison of additives in antiglaucoma prostaglandin (PG) analog ophthalmic formulations1177-54671177-5483https://doaj.org/article/3855b2f9298c4cd7a0932b2ee13b91da2013-03-01T00:00:00Zhttp://www.dovepress.com/safety-comparison-of-additives-in-antiglaucoma-prostaglandin-pg-analog-a12450https://doaj.org/toc/1177-5467https://doaj.org/toc/1177-5483Masamichi Fukuda, Shinsuke Shibata, Naoko Shibata, Kenta Hagihara, Hiromoto Yaguchi, Hiromi Osada, Nobuo Takahashi, Eri Kubo, Hiroshi SasakiDepartment of Ophthalmology, Kanazawa Medical University, Uchinada, JapanPurpose: To investigate the safety of five types of antiglaucoma prostaglandin analog ophthalmic formulations, and to clarify their differences in accordance with contained additives (preservatives and surface-active agents).Methods: The following five types of ophthalmic solutions and three types of additives were investigated: latanoprost (Xalatan&reg;; latanoprost), tafluprost (Tapros&reg;; tafluprost), bimatoprost (Lumigan&reg;; bimatoprost), travoprost (Travatan&reg;; travoprost), travoprost (Travatan Z&reg;; travoprost-Z), benzalkonium chloride (BAK), polyoxyethylene hardening castor oil 40 (HCO-40), and polysorbate 80 (P-80). These experimental solutions were exposed to the cultured cells of a rabbit-derived corneal cell line for a certain time, and the exposure time causing 50% cell damage (CD50), indicated by the ratio of viable cells to total cells was calculated (in vitro). In addition, corneal resistance (CR) was measured and CR ratio (post-treatment CR/pretreatment CR &times; 100) was calculated (in vivo).Results: CD50 of each ophthalmic solution was the longest with tafluprost, followed by travoprost-Z, bimatoprost, travoprost, and latanoprost. CD50 of 0.005%, 0.01%, and 0.02% BAK was 14.5 minutes, 8.1 minutes, and 4.0 minutes, respectively. The number of viable cells decreased to 60%, 8 minutes after exposure with HCO-40, and 30 minutes after being exposed to P-80. The CR ratio was 81.0% with travoprost and 82.0% with latanoprost, indicating a significant posttreatment reduction of CR (P &lt; 0.05). The CR ratio did not decrease after treatment with tafluprost, travoprost-Z, or bimatoprost. The CR ratio of 0.005%, 0.01%, and 0.02% BAK was 105.0%, 90.5%, and 68.7%, respectively, and that of HCO-40 and P-80 was 108.7% and 114.2%, respectively.Conclusion: BAK, HCO-40, and P-80 were thought to be involved in corneal injuries caused by each ophthalmic solution. Corneal injuries due to surface action were observed when using HCO-40 and P-80. When HCO-40 was combined with BAK, it induced micellar BAK and reduced corneal injuries by BAK.Keywords: corneal resistance measuring device, additives, prostaglandin analogs, surface-active agents, corneal epithelial injuryFukuda MShibata SShibata NHagihara KYaguchi HOsada HTakahashi NKubo ESasaki HDove Medical PressarticleOphthalmologyRE1-994ENClinical Ophthalmology, Vol 2013, Iss default, Pp 515-520 (2013)
institution	DOAJ
collection	DOAJ
language	EN
topic	Ophthalmology RE1-994
spellingShingle	Ophthalmology RE1-994 Fukuda M Shibata S Shibata N Hagihara K Yaguchi H Osada H Takahashi N Kubo E Sasaki H Safety comparison of additives in antiglaucoma prostaglandin (PG) analog ophthalmic formulations
description	Masamichi Fukuda, Shinsuke Shibata, Naoko Shibata, Kenta Hagihara, Hiromoto Yaguchi, Hiromi Osada, Nobuo Takahashi, Eri Kubo, Hiroshi SasakiDepartment of Ophthalmology, Kanazawa Medical University, Uchinada, JapanPurpose: To investigate the safety of five types of antiglaucoma prostaglandin analog ophthalmic formulations, and to clarify their differences in accordance with contained additives (preservatives and surface-active agents).Methods: The following five types of ophthalmic solutions and three types of additives were investigated: latanoprost (Xalatan&reg;; latanoprost), tafluprost (Tapros&reg;; tafluprost), bimatoprost (Lumigan&reg;; bimatoprost), travoprost (Travatan&reg;; travoprost), travoprost (Travatan Z&reg;; travoprost-Z), benzalkonium chloride (BAK), polyoxyethylene hardening castor oil 40 (HCO-40), and polysorbate 80 (P-80). These experimental solutions were exposed to the cultured cells of a rabbit-derived corneal cell line for a certain time, and the exposure time causing 50% cell damage (CD50), indicated by the ratio of viable cells to total cells was calculated (in vitro). In addition, corneal resistance (CR) was measured and CR ratio (post-treatment CR/pretreatment CR &times; 100) was calculated (in vivo).Results: CD50 of each ophthalmic solution was the longest with tafluprost, followed by travoprost-Z, bimatoprost, travoprost, and latanoprost. CD50 of 0.005%, 0.01%, and 0.02% BAK was 14.5 minutes, 8.1 minutes, and 4.0 minutes, respectively. The number of viable cells decreased to 60%, 8 minutes after exposure with HCO-40, and 30 minutes after being exposed to P-80. The CR ratio was 81.0% with travoprost and 82.0% with latanoprost, indicating a significant posttreatment reduction of CR (P &lt; 0.05). The CR ratio did not decrease after treatment with tafluprost, travoprost-Z, or bimatoprost. The CR ratio of 0.005%, 0.01%, and 0.02% BAK was 105.0%, 90.5%, and 68.7%, respectively, and that of HCO-40 and P-80 was 108.7% and 114.2%, respectively.Conclusion: BAK, HCO-40, and P-80 were thought to be involved in corneal injuries caused by each ophthalmic solution. Corneal injuries due to surface action were observed when using HCO-40 and P-80. When HCO-40 was combined with BAK, it induced micellar BAK and reduced corneal injuries by BAK.Keywords: corneal resistance measuring device, additives, prostaglandin analogs, surface-active agents, corneal epithelial injury
format	article
author	Fukuda M Shibata S Shibata N Hagihara K Yaguchi H Osada H Takahashi N Kubo E Sasaki H
author_facet	Fukuda M Shibata S Shibata N Hagihara K Yaguchi H Osada H Takahashi N Kubo E Sasaki H
author_sort	Fukuda M
title	Safety comparison of additives in antiglaucoma prostaglandin (PG) analog ophthalmic formulations
title_short	Safety comparison of additives in antiglaucoma prostaglandin (PG) analog ophthalmic formulations
title_full	Safety comparison of additives in antiglaucoma prostaglandin (PG) analog ophthalmic formulations
title_fullStr	Safety comparison of additives in antiglaucoma prostaglandin (PG) analog ophthalmic formulations
title_full_unstemmed	Safety comparison of additives in antiglaucoma prostaglandin (PG) analog ophthalmic formulations
title_sort	safety comparison of additives in antiglaucoma prostaglandin (pg) analog ophthalmic formulations
publisher	Dove Medical Press
publishDate	2013
url	https://doaj.org/article/3855b2f9298c4cd7a0932b2ee13b91da
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Safety comparison of additives in antiglaucoma prostaglandin (PG) analog ophthalmic formulations

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