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Development of Sustained-Release Ophthalmic Formulation Based on Tranilast Solid Nanoparticles

Eye drops containing Tranilast (TL), N-(3,4-dimethoxycinnamoyl) anthramilic acid, are used as an anti-allergic conjunctivitis drug in the ophthalmic field. Traditional eye drops are very patient compliant, although the bioavailability (BA) of most eye drops is low since eye drops cannot be instilled...

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Autores principales: Minami, Misa, Seiriki, Ryotaro, Otake, Hiroko, Nakazawa, Yosuke, Kanai, Kazutaka, Tanino, Tadatoshi, Nagai, Noriaki
Formato: Online Artículo Texto
Lenguaje:English
Publicado: MDPI 2020
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC7178381/
https://www.ncbi.nlm.nih.gov/pubmed/32260210
http://dx.doi.org/10.3390/ma13071675
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author Minami, Misa
Seiriki, Ryotaro
Otake, Hiroko
Nakazawa, Yosuke
Kanai, Kazutaka
Tanino, Tadatoshi
Nagai, Noriaki
author_facet Minami, Misa
Seiriki, Ryotaro
Otake, Hiroko
Nakazawa, Yosuke
Kanai, Kazutaka
Tanino, Tadatoshi
Nagai, Noriaki
author_sort Minami, Misa
collection PubMed
description Eye drops containing Tranilast (TL), N-(3,4-dimethoxycinnamoyl) anthramilic acid, are used as an anti-allergic conjunctivitis drug in the ophthalmic field. Traditional eye drops are very patient compliant, although the bioavailability (BA) of most eye drops is low since eye drops cannot be instilled beyond the capacity of the conjunctival sac due to its limited volume. Thus, traditional eye drops have low BA and a short duration of the drug on the ocular surface, so solutions to these problems are highly anticipated. In this study, we designed a sustained-release drug-delivery system (DDS) for TL nanoparticles. TL nanoparticles were prepared by bead mill treatment, and the gel formulations containing TL nanoparticles (TL-NPs-Gel, particle size 50 nm–100 nm) were provided by carboxypolymethylene. The crystal structure of TL with and without bead mill treatment is the same, but the TL solubility in formulations containing nanoparticles was 5.3-fold higher compared with gel formulations containing TL microparticles (TL-MPs-Gel). The photo and thermal stabilities of TL-NPs-Gel are also higher than those of dissolved TL. Moreover, when TL-NPs-Gel is applied to the upper eyelid skin (outside), the TL is released as nanoparticles, and delivered to the lacrimal fluid through the meibomian glands. In addition, the TL release profile for TL-NPs-Gel was sustained over 180 min after the treatment. These findings can be used to develop a sustained-release DDS in the ophthalmic field.
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spelling pubmed-71783812020-04-28 Development of Sustained-Release Ophthalmic Formulation Based on Tranilast Solid Nanoparticles Minami, Misa Seiriki, Ryotaro Otake, Hiroko Nakazawa, Yosuke Kanai, Kazutaka Tanino, Tadatoshi Nagai, Noriaki Materials (Basel) Article Eye drops containing Tranilast (TL), N-(3,4-dimethoxycinnamoyl) anthramilic acid, are used as an anti-allergic conjunctivitis drug in the ophthalmic field. Traditional eye drops are very patient compliant, although the bioavailability (BA) of most eye drops is low since eye drops cannot be instilled beyond the capacity of the conjunctival sac due to its limited volume. Thus, traditional eye drops have low BA and a short duration of the drug on the ocular surface, so solutions to these problems are highly anticipated. In this study, we designed a sustained-release drug-delivery system (DDS) for TL nanoparticles. TL nanoparticles were prepared by bead mill treatment, and the gel formulations containing TL nanoparticles (TL-NPs-Gel, particle size 50 nm–100 nm) were provided by carboxypolymethylene. The crystal structure of TL with and without bead mill treatment is the same, but the TL solubility in formulations containing nanoparticles was 5.3-fold higher compared with gel formulations containing TL microparticles (TL-MPs-Gel). The photo and thermal stabilities of TL-NPs-Gel are also higher than those of dissolved TL. Moreover, when TL-NPs-Gel is applied to the upper eyelid skin (outside), the TL is released as nanoparticles, and delivered to the lacrimal fluid through the meibomian glands. In addition, the TL release profile for TL-NPs-Gel was sustained over 180 min after the treatment. These findings can be used to develop a sustained-release DDS in the ophthalmic field. MDPI 2020-04-03 /pmc/articles/PMC7178381/ /pubmed/32260210 http://dx.doi.org/10.3390/ma13071675 Text en © 2020 by the authors. Licensee MDPI, Basel, Switzerland. This article is an open access article distributed under the terms and conditions of the Creative Commons Attribution (CC BY) license (http://creativecommons.org/licenses/by/4.0/).
spellingShingle Article
Minami, Misa
Seiriki, Ryotaro
Otake, Hiroko
Nakazawa, Yosuke
Kanai, Kazutaka
Tanino, Tadatoshi
Nagai, Noriaki
Development of Sustained-Release Ophthalmic Formulation Based on Tranilast Solid Nanoparticles
title Development of Sustained-Release Ophthalmic Formulation Based on Tranilast Solid Nanoparticles
title_full Development of Sustained-Release Ophthalmic Formulation Based on Tranilast Solid Nanoparticles
title_fullStr Development of Sustained-Release Ophthalmic Formulation Based on Tranilast Solid Nanoparticles
title_full_unstemmed Development of Sustained-Release Ophthalmic Formulation Based on Tranilast Solid Nanoparticles
title_short Development of Sustained-Release Ophthalmic Formulation Based on Tranilast Solid Nanoparticles
title_sort development of sustained-release ophthalmic formulation based on tranilast solid nanoparticles
topic Article
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC7178381/
https://www.ncbi.nlm.nih.gov/pubmed/32260210
http://dx.doi.org/10.3390/ma13071675
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