Cationic Thiolated Poly(aspartamide) Polymer as a Potential Excipient for Artificial Tear Formulations

Dry eye disease is a relatively common ocular problem, which causes eye discomfort and visual disorders leading to a decrease in the quality of life. The aim of this study was to find a possible excipient for eye drop formulations, which is able to stabilize the tear film. A cationic thiolated polya...

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Main Authors: Mária Budai-Szűcs, Gabriella Horvát, Barnabás Áron Szilágyi, Benjámin Gyarmati, András Szilágyi, Szilvia Berkó, Piroska Szabó-Révész, Giuseppina Sandri, Maria Cristina Bonferoni, Carla Caramella, Judit Soós, Andrea Facskó, Erzsébet Csányi
Format: Article
Language:English
Published: Wiley 2016-01-01
Series:Journal of Ophthalmology
Online Access:http://dx.doi.org/10.1155/2016/2647264
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author Mária Budai-Szűcs
Gabriella Horvát
Barnabás Áron Szilágyi
Benjámin Gyarmati
András Szilágyi
Szilvia Berkó
Piroska Szabó-Révész
Giuseppina Sandri
Maria Cristina Bonferoni
Carla Caramella
Judit Soós
Andrea Facskó
Erzsébet Csányi
author_facet Mária Budai-Szűcs
Gabriella Horvát
Barnabás Áron Szilágyi
Benjámin Gyarmati
András Szilágyi
Szilvia Berkó
Piroska Szabó-Révész
Giuseppina Sandri
Maria Cristina Bonferoni
Carla Caramella
Judit Soós
Andrea Facskó
Erzsébet Csányi
author_sort Mária Budai-Szűcs
collection DOAJ
description Dry eye disease is a relatively common ocular problem, which causes eye discomfort and visual disorders leading to a decrease in the quality of life. The aim of this study was to find a possible excipient for eye drop formulations, which is able to stabilize the tear film. A cationic thiolated polyaspartamide polymer, poly[(N-mercaptoethylaspartamide)-co-(N-(N′,N′-dimethylaminoethyl)aspartamide)] (ThioPASP-DME), was used as a potential vehicle. Besides satisfying the basic requirements, the chemical structure of ThioPASP-DME is similar to those of ocular mucins as it is a protein-like polymer bearing a considerable number of thiol groups. The solution of the polymer is therefore able to mimic the physiological properties of the mucins and it can interact with the mucus layer via disulphide bond formation. The resultant mucoadhesion provides a prolonged residence time and ensures protective effect for the corneal/conjunctival epithelium. ThioPASP-DME also has an antioxidant effect due to the presence of the thiol groups. The applicability of ThioPASP-DME as a potential excipient in eye drops was determined by means of ocular compatibility tests and through examinations of the interactions with the mucosal surface. The results indicate that ThioPASP-DME can serve as a potential eye drop excipient for the therapy of dry eye disease.
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spelling doaj-art-465eecd59bf749c090ce7bec5e65b4492025-08-20T03:36:12ZengWileyJournal of Ophthalmology2090-004X2090-00582016-01-01201610.1155/2016/26472642647264Cationic Thiolated Poly(aspartamide) Polymer as a Potential Excipient for Artificial Tear FormulationsMária Budai-Szűcs0Gabriella Horvát1Barnabás Áron Szilágyi2Benjámin Gyarmati3András Szilágyi4Szilvia Berkó5Piroska Szabó-Révész6Giuseppina Sandri7Maria Cristina Bonferoni8Carla Caramella9Judit Soós10Andrea Facskó11Erzsébet Csányi12Department of Pharmaceutical Technology, Faculty of Pharmacy, University of Szeged, Eötvös utca 6, Szeged 6720, HungaryDepartment of Pharmaceutical Technology, Faculty of Pharmacy, University of Szeged, Eötvös utca 6, Szeged 6720, HungarySoft Matters Group, Department of Physical Chemistry and Materials Science, Budapest University of Technology and Economics, Budafoki út 8, Budapest 1111, HungarySoft Matters Group, Department of Physical Chemistry and Materials Science, Budapest University of Technology and Economics, Budafoki út 8, Budapest 1111, HungarySoft Matters Group, Department of Physical Chemistry and Materials Science, Budapest University of Technology and Economics, Budafoki út 8, Budapest 1111, HungaryDepartment of Pharmaceutical Technology, Faculty of Pharmacy, University of Szeged, Eötvös utca 6, Szeged 6720, HungaryDepartment of Pharmaceutical Technology, Faculty of Pharmacy, University of Szeged, Eötvös utca 6, Szeged 6720, HungaryDepartment of Drug Sciences, Faculty of Pharmacy, University of Pavia, Viale Taramelli 12, 27100 Pavia, ItalyDepartment of Drug Sciences, Faculty of Pharmacy, University of Pavia, Viale Taramelli 12, 27100 Pavia, ItalyDepartment of Drug Sciences, Faculty of Pharmacy, University of Pavia, Viale Taramelli 12, 27100 Pavia, ItalyDepartment of Ophthalmology, Faculty of Medicine, University of Szeged, Korányi fasor 10-11, Szeged 6720, HungaryDepartment of Ophthalmology, Faculty of Medicine, University of Szeged, Korányi fasor 10-11, Szeged 6720, HungaryDepartment of Pharmaceutical Technology, Faculty of Pharmacy, University of Szeged, Eötvös utca 6, Szeged 6720, HungaryDry eye disease is a relatively common ocular problem, which causes eye discomfort and visual disorders leading to a decrease in the quality of life. The aim of this study was to find a possible excipient for eye drop formulations, which is able to stabilize the tear film. A cationic thiolated polyaspartamide polymer, poly[(N-mercaptoethylaspartamide)-co-(N-(N′,N′-dimethylaminoethyl)aspartamide)] (ThioPASP-DME), was used as a potential vehicle. Besides satisfying the basic requirements, the chemical structure of ThioPASP-DME is similar to those of ocular mucins as it is a protein-like polymer bearing a considerable number of thiol groups. The solution of the polymer is therefore able to mimic the physiological properties of the mucins and it can interact with the mucus layer via disulphide bond formation. The resultant mucoadhesion provides a prolonged residence time and ensures protective effect for the corneal/conjunctival epithelium. ThioPASP-DME also has an antioxidant effect due to the presence of the thiol groups. The applicability of ThioPASP-DME as a potential excipient in eye drops was determined by means of ocular compatibility tests and through examinations of the interactions with the mucosal surface. The results indicate that ThioPASP-DME can serve as a potential eye drop excipient for the therapy of dry eye disease.http://dx.doi.org/10.1155/2016/2647264
spellingShingle Mária Budai-Szűcs
Gabriella Horvát
Barnabás Áron Szilágyi
Benjámin Gyarmati
András Szilágyi
Szilvia Berkó
Piroska Szabó-Révész
Giuseppina Sandri
Maria Cristina Bonferoni
Carla Caramella
Judit Soós
Andrea Facskó
Erzsébet Csányi
Cationic Thiolated Poly(aspartamide) Polymer as a Potential Excipient for Artificial Tear Formulations
Journal of Ophthalmology
title Cationic Thiolated Poly(aspartamide) Polymer as a Potential Excipient for Artificial Tear Formulations
title_full Cationic Thiolated Poly(aspartamide) Polymer as a Potential Excipient for Artificial Tear Formulations
title_fullStr Cationic Thiolated Poly(aspartamide) Polymer as a Potential Excipient for Artificial Tear Formulations
title_full_unstemmed Cationic Thiolated Poly(aspartamide) Polymer as a Potential Excipient for Artificial Tear Formulations
title_short Cationic Thiolated Poly(aspartamide) Polymer as a Potential Excipient for Artificial Tear Formulations
title_sort cationic thiolated poly aspartamide polymer as a potential excipient for artificial tear formulations
url http://dx.doi.org/10.1155/2016/2647264
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