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 language | English |
|---|---|
| Article number | 2647264 |
| Journal | Journal of Ophthalmology |
| Volume | 2016 |
| DOIs | |
| Publication status | Published - 2016 |
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ASJC Scopus subject areas
- Ophthalmology
Cite this
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 journal › Article
}
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 -