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

Mária Budai-Szucs, Gabriella Horvát, Barnabás Áron Szilágyi, Benjámin Gyarmati, A. Szilágyi, Szilvia Berkó, P. Szabó-Révész, Giuseppina Sandri, Maria Cristina Bonferoni, Carla Caramella, Judit Soós, Andrea Facskó, Erzsébet Csányi

Research output: Contribution to journalArticle

3 Citations (Scopus)

Abstract

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.

Original languageEnglish
Article number2647264
JournalJournal of Ophthalmology
Volume2016
DOIs
Publication statusPublished - 2016

Fingerprint

Excipients
Ophthalmic Solutions
Polymers
Eye Diseases
Mucins
Sulfhydryl Compounds
Corneal Epithelium
Vision Disorders
Mucus
Tears
Disulfides
Antioxidants
Quality of Life
Lubricant Eye Drops
Proteins
Therapeutics

ASJC Scopus subject areas

  • Ophthalmology

Cite this

Budai-Szucs, M., Horvát, G., Szilágyi, B. Á., Gyarmati, B., Szilágyi, A., Berkó, S., ... Csányi, E. (2016). Cationic Thiolated Poly(aspartamide) Polymer as a Potential Excipient for Artificial Tear Formulations. Journal of Ophthalmology, 2016, [2647264]. https://doi.org/10.1155/2016/2647264

Cationic Thiolated Poly(aspartamide) Polymer as a Potential Excipient for Artificial Tear Formulations. / Budai-Szucs, Mária; Horvát, Gabriella; Szilágyi, Barnabás Áron; Gyarmati, Benjámin; Szilágyi, A.; Berkó, Szilvia; Szabó-Révész, P.; Sandri, Giuseppina; Bonferoni, Maria Cristina; Caramella, Carla; Soós, Judit; Facskó, Andrea; Csányi, Erzsébet.

In: Journal of Ophthalmology, Vol. 2016, 2647264, 2016.

Research output: Contribution to journalArticle

Budai-Szucs, M, Horvát, G, Szilágyi, BÁ, Gyarmati, B, Szilágyi, A, Berkó, S, Szabó-Révész, P, Sandri, G, Bonferoni, MC, Caramella, C, Soós, J, Facskó, A & Csányi, E 2016, 'Cationic Thiolated Poly(aspartamide) Polymer as a Potential Excipient for Artificial Tear Formulations', Journal of Ophthalmology, vol. 2016, 2647264. https://doi.org/10.1155/2016/2647264
Budai-Szucs, Mária ; Horvát, Gabriella ; Szilágyi, Barnabás Áron ; Gyarmati, Benjámin ; Szilágyi, A. ; Berkó, Szilvia ; Szabó-Révész, P. ; Sandri, Giuseppina ; Bonferoni, Maria Cristina ; Caramella, Carla ; Soós, Judit ; Facskó, Andrea ; Csányi, Erzsébet. / Cationic Thiolated Poly(aspartamide) Polymer as a Potential Excipient for Artificial Tear Formulations. In: Journal of Ophthalmology. 2016 ; Vol. 2016.
@article{237ba4c19e304e409762db60d40ec5d1,
title = "Cationic Thiolated Poly(aspartamide) Polymer as a Potential Excipient for Artificial Tear Formulations",
abstract = "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.",
author = "M{\'a}ria Budai-Szucs and Gabriella Horv{\'a}t and Szil{\'a}gyi, {Barnab{\'a}s {\'A}ron} and Benj{\'a}min Gyarmati and A. Szil{\'a}gyi and Szilvia Berk{\'o} and P. Szab{\'o}-R{\'e}v{\'e}sz and Giuseppina Sandri and Bonferoni, {Maria Cristina} and Carla Caramella and Judit So{\'o}s and Andrea Facsk{\'o} and Erzs{\'e}bet Cs{\'a}nyi",
year = "2016",
doi = "10.1155/2016/2647264",
language = "English",
volume = "2016",
journal = "Journal of Ophthalmology",
issn = "2090-004X",
publisher = "Hindawi Publishing Corporation",

}

TY - JOUR

T1 - Cationic Thiolated Poly(aspartamide) Polymer as a Potential Excipient for Artificial Tear Formulations

AU - Budai-Szucs, Mária

AU - Horvát, Gabriella

AU - Szilágyi, Barnabás Áron

AU - Gyarmati, Benjámin

AU - Szilágyi, A.

AU - Berkó, Szilvia

AU - Szabó-Révész, P.

AU - Sandri, Giuseppina

AU - Bonferoni, Maria Cristina

AU - Caramella, Carla

AU - Soós, Judit

AU - Facskó, Andrea

AU - Csányi, Erzsébet

PY - 2016

Y1 - 2016

N2 - 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.

AB - 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.

UR - http://www.scopus.com/inward/record.url?scp=84975159027&partnerID=8YFLogxK

UR - http://www.scopus.com/inward/citedby.url?scp=84975159027&partnerID=8YFLogxK

U2 - 10.1155/2016/2647264

DO - 10.1155/2016/2647264

M3 - Article

AN - SCOPUS:84975159027

VL - 2016

JO - Journal of Ophthalmology

JF - Journal of Ophthalmology

SN - 2090-004X

M1 - 2647264

ER -