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Ocular kinetics and safety of intravitreally injected angiotensin converting enzyme inhibitor lisinopril

BACKGROUND AND OBJECTIVES: The study investigated the intravitreal safety and vitreous disposition of lisinopril, an angiotensin converting enzyme inhibitor in rabbits for its projected use in retinopathy. METHODS: For the safety study, following the baseline ERG recording and fundus photography, 40...

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Autores principales: Nath, Madhu, Halder, Nabanita, Chandra, Parijat, Singh, Sundararajan Baskar, Deorari, Ashok Kumar, Kumar, Atul, Velpandian, Thirumurthy
Formato: Online Artículo Texto
Lenguaje:English
Publicado: BioMed Central 2018
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6234689/
https://www.ncbi.nlm.nih.gov/pubmed/30460043
http://dx.doi.org/10.1186/s40942-018-0146-7
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author Nath, Madhu
Halder, Nabanita
Chandra, Parijat
Singh, Sundararajan Baskar
Deorari, Ashok Kumar
Kumar, Atul
Velpandian, Thirumurthy
author_facet Nath, Madhu
Halder, Nabanita
Chandra, Parijat
Singh, Sundararajan Baskar
Deorari, Ashok Kumar
Kumar, Atul
Velpandian, Thirumurthy
author_sort Nath, Madhu
collection PubMed
description BACKGROUND AND OBJECTIVES: The study investigated the intravitreal safety and vitreous disposition of lisinopril, an angiotensin converting enzyme inhibitor in rabbits for its projected use in retinopathy. METHODS: For the safety study, following the baseline ERG recording and fundus photography, 40 µg/50 µl of lisinopril sterile injection was injected unilaterally in the rabbit eyes (n = 4), where other eye served as a control. The electroretinogram and fundus images were obtained at 24, 48, 72 and 168 h following the intravitreal injection. For pharmacokinetics evaluation of the lisinopril, one eye of each rabbit (n = 4) received an intravitreal injection of lisinopril (40 µg/50 µl). The concentration of lisinopril in the ocular tissues, humours, plasma, lung, kidney and liver were measured through ESI-LC-MS/MS. RESULTS: Upon the electroretinography studies, no significant difference was observed in the ERG pattern in the lisinopril injected eye when compared to the baseline of the respective animals till the 7th day of the study. In the fundus imaging, no morphological changes were observed in the retina of the animal. The concentration of the lisinopril was found to be above to the IC50 in the retina-choroid till 36 h. The concentration found in the plasma and body tissues were many folds less than the IC50 of the lisinopril. CONCLUSIONS: Intravitreal injection of 40 µg/50 µl of lisinopril found to be safe in the rabbit eye as evidenced by the electroretinography and fundus imaging studies. The average half-life of lisinopril is 12.6 h and the above-mentioned dose able to sustain its IC50 value till the 36 h.
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spelling pubmed-62346892018-11-20 Ocular kinetics and safety of intravitreally injected angiotensin converting enzyme inhibitor lisinopril Nath, Madhu Halder, Nabanita Chandra, Parijat Singh, Sundararajan Baskar Deorari, Ashok Kumar Kumar, Atul Velpandian, Thirumurthy Int J Retina Vitreous Original Article BACKGROUND AND OBJECTIVES: The study investigated the intravitreal safety and vitreous disposition of lisinopril, an angiotensin converting enzyme inhibitor in rabbits for its projected use in retinopathy. METHODS: For the safety study, following the baseline ERG recording and fundus photography, 40 µg/50 µl of lisinopril sterile injection was injected unilaterally in the rabbit eyes (n = 4), where other eye served as a control. The electroretinogram and fundus images were obtained at 24, 48, 72 and 168 h following the intravitreal injection. For pharmacokinetics evaluation of the lisinopril, one eye of each rabbit (n = 4) received an intravitreal injection of lisinopril (40 µg/50 µl). The concentration of lisinopril in the ocular tissues, humours, plasma, lung, kidney and liver were measured through ESI-LC-MS/MS. RESULTS: Upon the electroretinography studies, no significant difference was observed in the ERG pattern in the lisinopril injected eye when compared to the baseline of the respective animals till the 7th day of the study. In the fundus imaging, no morphological changes were observed in the retina of the animal. The concentration of the lisinopril was found to be above to the IC50 in the retina-choroid till 36 h. The concentration found in the plasma and body tissues were many folds less than the IC50 of the lisinopril. CONCLUSIONS: Intravitreal injection of 40 µg/50 µl of lisinopril found to be safe in the rabbit eye as evidenced by the electroretinography and fundus imaging studies. The average half-life of lisinopril is 12.6 h and the above-mentioned dose able to sustain its IC50 value till the 36 h. BioMed Central 2018-11-14 /pmc/articles/PMC6234689/ /pubmed/30460043 http://dx.doi.org/10.1186/s40942-018-0146-7 Text en © The Author(s) 2018 Open AccessThis article is distributed under the terms of the Creative Commons Attribution 4.0 International License (http://creativecommons.org/licenses/by/4.0/), which permits unrestricted use, distribution, and reproduction in any medium, provided you give appropriate credit to the original author(s) and the source, provide a link to the Creative Commons license, and indicate if changes were made. The Creative Commons Public Domain Dedication waiver (http://creativecommons.org/publicdomain/zero/1.0/) applies to the data made available in this article, unless otherwise stated.
spellingShingle Original Article
Nath, Madhu
Halder, Nabanita
Chandra, Parijat
Singh, Sundararajan Baskar
Deorari, Ashok Kumar
Kumar, Atul
Velpandian, Thirumurthy
Ocular kinetics and safety of intravitreally injected angiotensin converting enzyme inhibitor lisinopril
title Ocular kinetics and safety of intravitreally injected angiotensin converting enzyme inhibitor lisinopril
title_full Ocular kinetics and safety of intravitreally injected angiotensin converting enzyme inhibitor lisinopril
title_fullStr Ocular kinetics and safety of intravitreally injected angiotensin converting enzyme inhibitor lisinopril
title_full_unstemmed Ocular kinetics and safety of intravitreally injected angiotensin converting enzyme inhibitor lisinopril
title_short Ocular kinetics and safety of intravitreally injected angiotensin converting enzyme inhibitor lisinopril
title_sort ocular kinetics and safety of intravitreally injected angiotensin converting enzyme inhibitor lisinopril
topic Original Article
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6234689/
https://www.ncbi.nlm.nih.gov/pubmed/30460043
http://dx.doi.org/10.1186/s40942-018-0146-7
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