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Effect of 5-Oxo-2-Pyrrolidinecarboxylic Acid (PCA) as a New Topically Applied Agent for Dry Eye Syndrome Treatment

The aim of the study was the evaluation of the suitability of 5-oxo-2-pyrrolidinecarboxylic acid (PCA), also in combination with hyaluronic acid (HA), as artificial tears for treatment of dry eye syndrome (DES). Different aqueous formulations containing 0.10% w/w of PCA were used to determine: (i) e...

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Autores principales: Tampucci, Silvia, Monti, Daniela, Burgalassi, Susi, Terreni, Eleonora, Zucchetti, Erica, Baldacci, Filippo, Chetoni, Patrizia
Formato: Online Artículo Texto
Lenguaje:English
Publicado: MDPI 2018
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6161197/
https://www.ncbi.nlm.nih.gov/pubmed/30149648
http://dx.doi.org/10.3390/pharmaceutics10030137
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author Tampucci, Silvia
Monti, Daniela
Burgalassi, Susi
Terreni, Eleonora
Zucchetti, Erica
Baldacci, Filippo
Chetoni, Patrizia
author_facet Tampucci, Silvia
Monti, Daniela
Burgalassi, Susi
Terreni, Eleonora
Zucchetti, Erica
Baldacci, Filippo
Chetoni, Patrizia
author_sort Tampucci, Silvia
collection PubMed
description The aim of the study was the evaluation of the suitability of 5-oxo-2-pyrrolidinecarboxylic acid (PCA), also in combination with hyaluronic acid (HA), as artificial tears for treatment of dry eye syndrome (DES). Different aqueous formulations containing 0.10% w/w of PCA were used to determine: (i) ex vivo permeation profile of PCA in isolated rabbit corneas; (ii) in vivo residence time of PCA in the precorneal area of rabbits; and (iii) in vivo ability of PCA to counteract the reduction of tear production in an experimental model of DES induced in rabbits. The pharmacokinetic profile of PCA in tear fluid was characterized by high concentrations immediately after application, followed by a rapid decrease, with half-life values of 17.16 and 22.27 min for solutions containing PCA alone and in combination with HA, respectively, when 100 µL of solutions were instilled. The addition of HA almost doubled the PCA bioavailability minimizing the ex vivo apparent corneal permeability of PCA. A positive Shirmer Test Score (STS) was observed for PCA compared to contralateral eyes at all days of treatment for PCA/HA formulation. PCA provides protection from desiccation probably for its osmoprotective activity and high water–binding capability, and this behaviour was enhanced by HA.
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spelling pubmed-61611972018-10-01 Effect of 5-Oxo-2-Pyrrolidinecarboxylic Acid (PCA) as a New Topically Applied Agent for Dry Eye Syndrome Treatment Tampucci, Silvia Monti, Daniela Burgalassi, Susi Terreni, Eleonora Zucchetti, Erica Baldacci, Filippo Chetoni, Patrizia Pharmaceutics Article The aim of the study was the evaluation of the suitability of 5-oxo-2-pyrrolidinecarboxylic acid (PCA), also in combination with hyaluronic acid (HA), as artificial tears for treatment of dry eye syndrome (DES). Different aqueous formulations containing 0.10% w/w of PCA were used to determine: (i) ex vivo permeation profile of PCA in isolated rabbit corneas; (ii) in vivo residence time of PCA in the precorneal area of rabbits; and (iii) in vivo ability of PCA to counteract the reduction of tear production in an experimental model of DES induced in rabbits. The pharmacokinetic profile of PCA in tear fluid was characterized by high concentrations immediately after application, followed by a rapid decrease, with half-life values of 17.16 and 22.27 min for solutions containing PCA alone and in combination with HA, respectively, when 100 µL of solutions were instilled. The addition of HA almost doubled the PCA bioavailability minimizing the ex vivo apparent corneal permeability of PCA. A positive Shirmer Test Score (STS) was observed for PCA compared to contralateral eyes at all days of treatment for PCA/HA formulation. PCA provides protection from desiccation probably for its osmoprotective activity and high water–binding capability, and this behaviour was enhanced by HA. MDPI 2018-08-25 /pmc/articles/PMC6161197/ /pubmed/30149648 http://dx.doi.org/10.3390/pharmaceutics10030137 Text en © 2018 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
Tampucci, Silvia
Monti, Daniela
Burgalassi, Susi
Terreni, Eleonora
Zucchetti, Erica
Baldacci, Filippo
Chetoni, Patrizia
Effect of 5-Oxo-2-Pyrrolidinecarboxylic Acid (PCA) as a New Topically Applied Agent for Dry Eye Syndrome Treatment
title Effect of 5-Oxo-2-Pyrrolidinecarboxylic Acid (PCA) as a New Topically Applied Agent for Dry Eye Syndrome Treatment
title_full Effect of 5-Oxo-2-Pyrrolidinecarboxylic Acid (PCA) as a New Topically Applied Agent for Dry Eye Syndrome Treatment
title_fullStr Effect of 5-Oxo-2-Pyrrolidinecarboxylic Acid (PCA) as a New Topically Applied Agent for Dry Eye Syndrome Treatment
title_full_unstemmed Effect of 5-Oxo-2-Pyrrolidinecarboxylic Acid (PCA) as a New Topically Applied Agent for Dry Eye Syndrome Treatment
title_short Effect of 5-Oxo-2-Pyrrolidinecarboxylic Acid (PCA) as a New Topically Applied Agent for Dry Eye Syndrome Treatment
title_sort effect of 5-oxo-2-pyrrolidinecarboxylic acid (pca) as a new topically applied agent for dry eye syndrome treatment
topic Article
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6161197/
https://www.ncbi.nlm.nih.gov/pubmed/30149648
http://dx.doi.org/10.3390/pharmaceutics10030137
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