Hyaluronan-based Sustained Delivery of the Antibiotic Besifloxacin to the Eye

Shirley Luo


Corneal ulcers, an ocular emergency and can be a cause of blindness globally if not effectively treated, require topical antibiotics delivered via a very inconvenient hourly, round-the-clock, multiple-day administration regimen to prevent corneal vision loss. These eye drops must be compounded off-label, are difficult to reliably administer, and can suffer from low availability of therapeutic agent due to tears and blinking. This study focuses on the development of a topical hyaluronic acid (HA)-based biodegradable film designed to deliver Besifloxacin on a sustained-released (SR) basis to overcome today’s dosing challenges. Prototype films of cross-linked, thiolated carboxymethylated HA (CMHA-S) containing Besifloxacin were produced and evaluated for in vitro drug release. Films were fabricated in silicone molds using 16 mg/mL CMHA-S and poly(ethyleneglycol) diacrylate (PEGDA), as a cross-linker. The polymerized gel was dried at 37°C overnight to create thin films. Various amounts of Besifloxacin (up to 150 μg/film) were formulated into the polymer solution prior to cross-linking. The release rate was monitored in phosphate buffered saline (PBS) by measuring UV absorption at 293 nm. Released amounts were calculated from the Besifloxacin standard solution. Results show that Besifloxacin can be continuously released from films for up to 9 days (on Day 9, approximately 1 μg was released from 150 μg loading). In vitro efficacy tests on the released Besifloxacin are currently in progress. In conclusion, Jade Therapeutics’ Besifloxacin-loaded films represent a promising alternative to hourly antibiotic eye drops, and have the potential to move forward into in vivo studies and ultimately become a clinically useful product. Furthermore, this polymer-based system can be expanded to deliver other antimicrobials to treat additional indications such as ophthalmic fungal or viral infections.


Corneal Ulcers; Delivery; Hyaluronan; Besifloxacin

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