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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doaj-abac2bb8aeb14a82943d69ec673951312020-11-24T21:17:10ZengMDPI AGPharmaceutics1999-49232018-08-0110313710.3390/pharmaceutics10030137pharmaceutics10030137Effect of 5-Oxo-2-Pyrrolidinecarboxylic Acid (PCA) as a New Topically Applied Agent for Dry Eye Syndrome TreatmentSilvia Tampucci0Daniela Monti1Susi Burgalassi2Eleonora Terreni3Erica Zucchetti4Filippo Baldacci5Patrizia Chetoni6Department of Pharmacy, University of Pisa, 56126 Pisa, ItalyDepartment of Pharmacy, University of Pisa, 56126 Pisa, ItalyDepartment of Pharmacy, University of Pisa, 56126 Pisa, ItalyDepartment of Pharmacy, University of Pisa, 56126 Pisa, ItalyDepartment of Pharmacy, University of Pisa, 56126 Pisa, ItalyLaboratori Baldacci S.p.A., 56100 Pisa, ItalyDepartment of Pharmacy, University of Pisa, 56126 Pisa, ItalyThe 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.http://www.mdpi.com/1999-4923/10/3/137dry eyehyaluronic acidosmoprotectant5-oxo-2-pyrrolidinecarboxylic acid (PCA)rabbitstear fluid |
collection |
DOAJ |
language |
English |
format |
Article |
sources |
DOAJ |
author |
Silvia Tampucci Daniela Monti Susi Burgalassi Eleonora Terreni Erica Zucchetti Filippo Baldacci Patrizia Chetoni |
spellingShingle |
Silvia Tampucci Daniela Monti Susi Burgalassi Eleonora Terreni Erica Zucchetti Filippo Baldacci Patrizia Chetoni Effect of 5-Oxo-2-Pyrrolidinecarboxylic Acid (PCA) as a New Topically Applied Agent for Dry Eye Syndrome Treatment Pharmaceutics dry eye hyaluronic acid osmoprotectant 5-oxo-2-pyrrolidinecarboxylic acid (PCA) rabbits tear fluid |
author_facet |
Silvia Tampucci Daniela Monti Susi Burgalassi Eleonora Terreni Erica Zucchetti Filippo Baldacci Patrizia Chetoni |
author_sort |
Silvia Tampucci |
title |
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_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_sort |
effect of 5-oxo-2-pyrrolidinecarboxylic acid (pca) as a new topically applied agent for dry eye syndrome treatment |
publisher |
MDPI AG |
series |
Pharmaceutics |
issn |
1999-4923 |
publishDate |
2018-08-01 |
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. |
topic |
dry eye hyaluronic acid osmoprotectant 5-oxo-2-pyrrolidinecarboxylic acid (PCA) rabbits tear fluid |
url |
http://www.mdpi.com/1999-4923/10/3/137 |
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