Long-acting liposomal corneal anesthetics

Area of Science:

• Ophthalmology
• Nanotechnology
• Pharmacology

Background:

• Effective corneal pain management requires long-acting ocular anesthesia.
• Current anesthetic eye drops offer limited duration of action.
• Developing sustained-release formulations is crucial for improving patient outcomes.

Purpose of the Study:

• To develop and evaluate liposome-based eye drops for prolonged ocular anesthesia.
• To functionalize liposomes with succinyl-Concanavalin A (sConA-Lip) for enhanced corneal adhesion.
• To investigate the anesthetic efficacy and safety of sConA-Lip loaded with tetrodotoxin and dexmedetomidine (sConA-Lip/TD).

Main Methods:

• Liposomes were functionalized with sConA to improve corneal binding.
• sConA-Lip were loaded with tetrodotoxin and dexmedetomidine (TD).
• Anesthetic duration and efficacy were assessed after topical eye drop instillation in vivo and cytotoxicity was evaluated in vitro.

Main Results:

• A single sConA-Lip/TD eye drop provided 105 minutes of complete and 608 minutes of partial corneal analgesia.
• This duration was significantly longer than conventional proparacaine or non-functionalized liposomes.
• In vitro studies confirmed sConA-Lip/TD were non-cytotoxic to corneal cells.
• The formulation did not impede corneal wound healing.

Conclusions:

• sConA-Lip/TD eye drops represent a promising strategy for achieving very long-acting ocular anesthesia.
• This formulation offers a potential solution for managing acute surgical and non-surgical corneal pain.
• The sustained release and corneal adhesion properties may benefit treatment of various ocular surface diseases.