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

Area of Science:

• Ophthalmology
• Polymer Science
• Biomaterials

Background:

• Dry eye disease (DED) is a prevalent ocular condition causing discomfort and reduced quality of life.
• Current eye drop formulations often lack sufficient tear film stabilization and prolonged ocular residence time.

Purpose of the Study:

• To evaluate a cationic thiolated polyaspartamide polymer, ThioPASP-DME, as a potential excipient for DED eye drops.
• To assess ThioPASP-DME's ability to stabilize the tear film and enhance ocular surface protection.

Main Methods:

• Synthesis and characterization of poly[(N-mercaptoethylaspartamide)-co-(N-(N',N'-dimethylaminoethyl)aspartamide)] (ThioPASP-DME).
• Evaluation of ThioPASP-DME's mucoadhesive properties through interaction with ocular mucus layers.
• Assessment of antioxidant effects and ocular compatibility via in vitro and in vivo tests.

Main Results:

• ThioPASP-DME demonstrated significant mucoadhesion via disulfide bond formation with the mucus layer, prolonging residence time.
• The polymer exhibited antioxidant properties attributed to its thiol groups.
• Ocular compatibility tests confirmed ThioPASP-DME's suitability for ophthalmic applications.

Conclusions:

• ThioPASP-DME effectively mimics ocular mucins, offering enhanced mucoadhesion and prolonged ocular surface protection.
• The polymer's antioxidant capacity further contributes to its therapeutic potential in dry eye disease management.
• ThioPASP-DME is a promising candidate excipient for developing advanced eye drop formulations for dry eye therapy.