Sun Pharma makes a novel NSAID by combining a known medicine with a new delivery vehicle.

The retention time of eye drops for adequate penetration into the eye has always been an issue, as frequent dosing leads to preservative toxicity and patient noncompliance. Some physicians suggest that DuraSite (InSite Vision) researchers might have found the answer to surface retention, and hence ocular surface penetration.

The combination of DuraSite with other ophthalmic medications, namely bromfenac ophthalmic solution, or BromSite, lets cataract surgeons offer their patients a topical nonsteroidal anti-inflammatory drug (NSAID) that is study proven to relieve pain effectively.

ABOUT DURASITE

DuraSite is a topical drug delivery vehicle that stabilizes small molecules in a polyacrylic acidic, muco-adhesive matrix that slowly releases the ocular pharmaceutical that is combined with it.¹ For example, this gel-forming drop has been used in combination with besifloxacin, known as Besivance (Bausch + Lomb)² and with azithromycin to create AzaSite (Akorn),³ both improving antibiotic delivery. The addition of DuraSite to an active ingredient increases the drug’s contact time with the ocular surface for several hours and allows for better distribution. In 2015, Sun Pharma acquired InSight Vision for the express purpose of using this delivery system for ophthalmic therapies.

ABOUT BROMSITE

BromSite (Sun Pharma) is the first drug to use the DuraSite delivery system in combination with 0.075% bromfenac ophthalmic solution to create a topical NSAID with better penetration.⁴ The FDA approved it in spring 2016 for the treatment of ocular pain and post-operative inflammation following cataract surgery.⁵ One drop is administered twice daily, one day prior to surgery, on the day of surgery and for 14 days postoperatively.⁶

Bromfenac blocks prostaglandin synthesis by inhibiting cyclooxygenase 1 and 2.⁶ In a study comparing the concentration of bromfenac in the aqueous humor when 0.09% was delivered topically without DuraSite versus 0.09% in DuraSite, a four-fold higher concentration of the bromfenac with DuraSite was found in the aqueous.⁷

PAIN MANAGEMENT

John French, MD, a specialist in corneal disease and small-incision cataract surgery in Southern Pines, NC, says other NSAIDs tend to sting and burn when instilled. He has found BromSite to be well tolerated by patients. Studies of ocular pain following cataract surgery showed that 78.9% of patients who received BromSite were pain free one-day postoperatively, while 55.3% who received DuraSite alone were pain free.⁶

While pain is not usually a major issue following cataract surgery, BromSite helps to resolve the mild discomfort and foreign body sensation.

For Jason P. Brinton, MD, a refractive surgeon in St. Louis, Mo., providing a comfortable patient experience is paramount. His patients are healthy adults in their 50s and 60s who increasingly opt for correction of presbyopia and ametropia with refractive lens exchange (RLE) rather than pursue LASIK with subsequent cataract surgery later in life. “When having RLE, our patients expect a comfortable experience from the day of surgery through full recovery,” he explains.

His off-label usage of BromSite includes one drop administered postoperatively in the recovery room immediately following LASIK and PRK for pain relief. Patients who receive PRK are also given an opportunity to take it for pain management twice daily for three days following surgery, if needed.

POST-OPERATIVE INFLAMMATION

With respect to treating post-operative inflammation, studies show that, of the patients who used BromSite as compared to the DuraSite vehicle alone, 47.6% had grade zero cells and 83.1% had grade zero flare at 15 days postoperatively compared to 20.6% zero cells and 44.7% zero flare with DuraSite only.⁶ Says Dr. French, “BromSite offers amazing penetration with increased comfort. There is definitely a perception of a quieter eye at one-day postop, with minimal cells and flare.” He also noted fewer complaints of light sensitivity than from patients using other NSAIDs.

PROS AND CONS

One main advantage of BromSite over other NSAIDS, in addition to its retention time, is the engineering design of the bottle itself. BromSite comes in an opaque polyethylene bottle with a clear tip. After inverting the bottle, patients flick the bottle firmly once before each use to move the drug to the bottle’s tip to administer. Says Dr. Brinton, “The BromSite bottle is convenient, easy to use, economical, has a high volume of liquid (5 mL) and, when you squeeze it, only one drop comes out. This leads to minimal waste and enough medication for the duration of treatment.”

Both Dr. French and Dr. Brinton suggest that the DuraSite gel formulation could help to lubricate the eyes by creating a more stable tear film, reducing ocular surface irritation and adding to post-surgical comfort. They speculate that patients using BromSite may not require the frequent dosing that artificial tears require, decreasing the number of eye drops needed overall. Although thicker solutions may result in viscosity blur, they have not found this to be an issue with BromSite when measuring post-operative acuities.

Adverse reactions to BromSite include anterior chamber inflammation, headache, vitreous floaters, iritis, eye pain and ocular hypertension. All NSAIDs may result in delayed healing, cross-sensitivity to acetylsalicylic acid and increased bleeding time. There is also a risk of corneal thinning, erosion or perforation with NSAID use.^6,8 OM

Both Dr. French and Dr. Brinton report no financial interests related to this article.

REFERENCES

1. DuraSite Compound Advantage. http://www.insitevision.com/durasite.html . Accessed Sept. 14, 2017.
2. Bausch + Lomb, Besivance. http://www.bausch.com/ecp/our-products/rx-pharmaceuticals/rx-pharmaceuticals/besivance-ecp . Accessed Sept. 13, 2017.
3. AzaSite. http://www.azasite.com/hcp/overview.html?hcpUser=yes. Accessed Nov. 6, 2017.
4. About BromSite. https://www.bromsite.com/ . Accessed Sept. 13, 2017.
5. BromSite (bromfenac) Ophthalmic Solution. https://www.accessdata.fda.gov/drugsatfda_docs/nda/2016/206911Orig1s000TOC.cfm . Accessed Sept. 14, 2017.
6. NDA 206911, ISV-303 (0.075% bromfenac) 1.14.2.3 Final Labeling Text. https://www.accessdata.fda.gov/drugsatfda_docs/label/2016/206911s000lbl.pdf .
7. Bowman LM, Si EC, Hosseini K. Effect of DuraSite on the Topical Delivery of Bromfenac to the Ocular Tissues. Invest Ophthalmol Vis Sci. 2010;51:5298.
8. Burling-Phillips L. Topical NSAIDs: Best Practices for Safe Use. AAO EyeNet Magazine. July 2013. https://www.aao.org/eyenet/article/topical-nsaids-best-practices-safe-use .