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Travoprost Liquid Nanocrystals: An Innovative Armamentarium for Effective Glaucoma Therapy

To date, the ophthalmic application of liquid crystalline nanostructures (LCNs) has not been thoroughly reconnoitered, yet they have been extensively used. LCNs are primarily made up of glyceryl monooleate (GMO) or phytantriol as a lipid, a stabilizing agent, and a penetration enhancer (PE). For opt...

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Autores principales: El-Gendy, Mohamed A., Mansour, Mai, El-Assal, Mona I. A., Ishak, Rania A. H., Mortada, Nahed D.
Formato: Online Artículo Texto
Lenguaje:English
Publicado: MDPI 2023
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC10056037/
https://www.ncbi.nlm.nih.gov/pubmed/36986814
http://dx.doi.org/10.3390/pharmaceutics15030954
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author El-Gendy, Mohamed A.
Mansour, Mai
El-Assal, Mona I. A.
Ishak, Rania A. H.
Mortada, Nahed D.
author_facet El-Gendy, Mohamed A.
Mansour, Mai
El-Assal, Mona I. A.
Ishak, Rania A. H.
Mortada, Nahed D.
author_sort El-Gendy, Mohamed A.
collection PubMed
description To date, the ophthalmic application of liquid crystalline nanostructures (LCNs) has not been thoroughly reconnoitered, yet they have been extensively used. LCNs are primarily made up of glyceryl monooleate (GMO) or phytantriol as a lipid, a stabilizing agent, and a penetration enhancer (PE). For optimization, the D-optimal design was exploited. A characterization using TEM and XRPD was conducted. Optimized LCNs were loaded with the anti-glaucoma drug Travoprost (TRAVO). Ex vivo permeation across the cornea, in vivo pharmacokinetics, and pharmacodynamic studies were performed along with ocular tolerability examinations. Optimized LCNs are constituted of GMO, Tween(®) 80 as a stabilizer, and either oleic acid or Captex(®) 8000 as PE at 25 mg each. TRAVO-LNCs, F-1-L and F-3-L, showed particle sizes of 216.20 ± 6.12 and 129.40 ± 11.73 nm, with EE% of 85.30 ± 4.29 and 82.54 ± 7.65%, respectively, revealing the highest drug permeation parameters. The bioavailability of both attained 106.1% and 322.82%, respectively, relative to the market product TRAVATAN(®). They exhibited respective intraocular pressure reductions lasting for 48 and 72 h, compared to 36 h for TRAVATAN(®). All LCNs exhibited no evidence of ocular injury in comparison to the control eye. The findings revealed the competence of TRAVO-tailored LCNs in glaucoma treatment and suggested the potential application of a novel platform in ocular delivery.
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spelling pubmed-100560372023-03-30 Travoprost Liquid Nanocrystals: An Innovative Armamentarium for Effective Glaucoma Therapy El-Gendy, Mohamed A. Mansour, Mai El-Assal, Mona I. A. Ishak, Rania A. H. Mortada, Nahed D. Pharmaceutics Article To date, the ophthalmic application of liquid crystalline nanostructures (LCNs) has not been thoroughly reconnoitered, yet they have been extensively used. LCNs are primarily made up of glyceryl monooleate (GMO) or phytantriol as a lipid, a stabilizing agent, and a penetration enhancer (PE). For optimization, the D-optimal design was exploited. A characterization using TEM and XRPD was conducted. Optimized LCNs were loaded with the anti-glaucoma drug Travoprost (TRAVO). Ex vivo permeation across the cornea, in vivo pharmacokinetics, and pharmacodynamic studies were performed along with ocular tolerability examinations. Optimized LCNs are constituted of GMO, Tween(®) 80 as a stabilizer, and either oleic acid or Captex(®) 8000 as PE at 25 mg each. TRAVO-LNCs, F-1-L and F-3-L, showed particle sizes of 216.20 ± 6.12 and 129.40 ± 11.73 nm, with EE% of 85.30 ± 4.29 and 82.54 ± 7.65%, respectively, revealing the highest drug permeation parameters. The bioavailability of both attained 106.1% and 322.82%, respectively, relative to the market product TRAVATAN(®). They exhibited respective intraocular pressure reductions lasting for 48 and 72 h, compared to 36 h for TRAVATAN(®). All LCNs exhibited no evidence of ocular injury in comparison to the control eye. The findings revealed the competence of TRAVO-tailored LCNs in glaucoma treatment and suggested the potential application of a novel platform in ocular delivery. MDPI 2023-03-15 /pmc/articles/PMC10056037/ /pubmed/36986814 http://dx.doi.org/10.3390/pharmaceutics15030954 Text en © 2023 by the authors. https://creativecommons.org/licenses/by/4.0/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 (https://creativecommons.org/licenses/by/4.0/).
spellingShingle Article
El-Gendy, Mohamed A.
Mansour, Mai
El-Assal, Mona I. A.
Ishak, Rania A. H.
Mortada, Nahed D.
Travoprost Liquid Nanocrystals: An Innovative Armamentarium for Effective Glaucoma Therapy
title Travoprost Liquid Nanocrystals: An Innovative Armamentarium for Effective Glaucoma Therapy
title_full Travoprost Liquid Nanocrystals: An Innovative Armamentarium for Effective Glaucoma Therapy
title_fullStr Travoprost Liquid Nanocrystals: An Innovative Armamentarium for Effective Glaucoma Therapy
title_full_unstemmed Travoprost Liquid Nanocrystals: An Innovative Armamentarium for Effective Glaucoma Therapy
title_short Travoprost Liquid Nanocrystals: An Innovative Armamentarium for Effective Glaucoma Therapy
title_sort travoprost liquid nanocrystals: an innovative armamentarium for effective glaucoma therapy
topic Article
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC10056037/
https://www.ncbi.nlm.nih.gov/pubmed/36986814
http://dx.doi.org/10.3390/pharmaceutics15030954
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