24-Hour Evaluation of the Ocular Distribution of <sup>14</sup>C-Labeled Bromfenac Following Topical Instillation into the Eyes of New Zealand White Rabbits

Baklayan, G. A.; Patterson, H.M.; Song, Clara K.; Gow, J.A.; McNamara, T.R.

doi:10.1089/jop.2007.0082

Cited by 48 publications

(43 citation statements)

References 10 publications

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“…In rabbits, bromfenac was detected in the retina, choroid, and sclera 24 hours after topical instillation; therefore, it could be used to treat inflammation in the posterior pole. 19 Yoshinaga et al 20 recently showed that bromfenac inhibits CNV by decreasing VEGF expression through the antioxidant protein heme oxygenase 1-dependent pathway in an experimental rat model. Clinically, Grant 8 suggested a synergistic effect of topical bromfenac on anti-VEGF treatment in a nonrandomized, retrospective, 6-month study; patients with topical bromfenac had a significant improvement in visual outcomes and a significant decrease in the number of ranibizumab injections.…”

Section: Discussionmentioning

confidence: 99%

Topical Bromfenac as an Adjunctive Treatment With Intravitreal Ranibizumab for Exudative Age-Related Macular Degeneration

Gomi

Sawa

Tsujikawa

et al. 2012

Retina

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Section: Discussionmentioning

confidence: 99%

Topical Bromfenac as an Adjunctive Treatment With Intravitreal Ranibizumab for Exudative Age-Related Macular Degeneration

Gomi

Sawa

Tsujikawa

et al. 2012

Retina

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“…[1][2][3][4][5][6] Therefore, NSAID treatment is preferred, and these compounds are being extensively studied in patients and animal models to assess their toxicity, pharmacokinetics, neuroprotective properties, and anti-inflammatory and antiedema effects, among others. 4,[7][8][9][10][11][12][13][14][15][16] One such NSAID, bromfenac, is an inhibitor of the cyclooxygenase (COX) enzymes COX1 and COX2, and is more selective for COX2 than for COX1. 17 In rabbits, topical bromfenac reaches the vitreous and retinochoriodal tissues, and after a single topical administration is detectable in the retinochoroid up to 24 hours.…”

mentioning

confidence: 99%

“…17 In rabbits, topical bromfenac reaches the vitreous and retinochoriodal tissues, and after a single topical administration is detectable in the retinochoroid up to 24 hours. 8,17,18 Kida et al 19 showed that compared to nepafenac and diclofenac, bromfenac concentration after topical application on rabbit eyes was continuously higher in the retinochoroidal tissues. Thus, bromfenac may have a better therapeutic effect than these two other NSAIDs in retinochoroidal inflammatory diseases.…”

mentioning

confidence: 99%

Topical Treatment With Bromfenac Reduces Retinal Gliosis and Inflammation After Optic Nerve Crush

Rovere

Nadal-Nicolás

Sobrado‐Calvo

et al. 2016

Invest. Ophthalmol. Vis. Sci.

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Citation: Rovere G, Nadal-Nicolás FM, Sobrado-Calvo P, et al. Topical treatment with bromfenac reduces retinal gliosis and inflammation after optic nerve crush. Invest Ophthalmol Vis Sci. 2016;57:6098-6106. DOI: 10.1167/iovs.16-20425 PURPOSE. To study the effect of topical administration of bromfenac, a nonsteroidal antiinflammatory drug (NSAID), on retinal gliosis and levels of prostaglandin E 2 (PGE 2 ) after complete optic nerve crush (ONC).METHODS. Adult albino rats were divided into the following groups (n ¼ 8 retinas/group): (1) intact, (2) intact and bromfenac treatment (twice a day during 7 days), (3) ONC (7 days), and (4) ONC (7 days) þ bromfenac treatment (twice a day during 7 days). Animals from groups 3 and 4 were imaged in vivo with spectral-domain optical coherence tomography (SD-OCT) before the procedure and 15 minutes, 3, 5, or 7 days later. Retinas from all groups were analyzed by immunodetection, Western blotting, or enzyme-linked immunoabsorbent assay (ELISA).RESULTS. Quantification of Brn3a (brain-specific homeobox/POU domain protein 3A)þ RGCs (retinal ganglion cells) in cross sections showed that bromfenac treatment does not accelerate ONC-induced degeneration. Cellular retinaldehyde binding protein 1 regulation indicated that bromfenac improves retinal homeostasis in injured retinas. Spectral-domain OCT showed that the thickness of the retina and the retinal nerve fiber layer at 7 days post ONC was significantly reduced in bromfenac-treated animals when compared to untreated animals. In agreement with these data, hypertrophy of astrocytes and Müller cells and expression of glial fibrillary acidic protein and vimentin were greatly diminished by bromfenac treatment. While no changes in cyclooxygenase (COX) enzyme COX1 and COX2 expression were observed, there was a significant increase of PGE 2 after ONC that was controlled by bromfenac treatment.CONCLUSIONS. Topical administration of bromfenac is an efficient and noninvasive treatment to control the retinal gliosis and release of proinflammatory mediators that follow a massive insult to the RGC population.

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“…Baklayan et al presented data from two separate but similar studies in which bromfenac and nepafenac were administered at three times the commercial dose in an animal model. 24 Bromfenac achieved measurable levels in all major ocular tissues that were detectable at 24 hours, but no significant levels of nepafenac/amfenac were detected in the aqueous humour and choroid after 12 hours and in the retina after six hours (see Figure 3). …”

Section: Penetration Of Ocular Tissuesmentioning

confidence: 98%

“…24,29 These early peak concentrations in aqueous humour remain above the concentration required to inhibit COX-2 by 50%…”

Section: Sustained Therapeutic Activitymentioning

confidence: 98%

New Look at Ocular Inflammation Control – Powerful and Fast-acting Twice-daily Bromfenac for a Novel Standard in the Treatment of Inflammation

Cho¹,

Mozayan²

2011

European Ophthalmic Review

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Inflammation in the eye arising from various factors -including allergy, infection, injury and surgery -can have serious consequences, and can continue long after the cause is removed, resulting in permanently damaged vision. The treatment of ophthalmic inflammation after surgery has traditionally consisted of topical corticosteroids, but adverse events such as delayed healing, rise in intraocular pressure and increased susceptibility to microbial infections have driven the search for alternative treatments. Non-steroidal anti-inflammatory drugs (NSAIDs) have been used as alternatives to steroid treatments but also have limitations and cause adverse events. Bromfenac has emerged as a potent and safe treatment for inflammation after cataract surgery. Its unique chemical structure makes it a highly lipophilic molecule that penetrates all major ocular tissues in a rapid and sustained manner. It is also a potent inhibitor of the enzyme cyclo-oxygenase-2, which is believed to be the primary mediator of ocular inflammation. These properties permit less frequent dosing (twice-daily [BID]) and greater patient tolerability. A body of efficacy and safety data support use of bromfenac in this indication and it compares favourably with other NSAIDs and steroids in limiting post-operative inflammation. NSAIDs and corticosteroids have different, potentially synergistic effects. However, benefits specific to NSAIDs include lowering prostaglandin E-induced intraocular pressure elevation, no increased risk of secondary infections and stabilisation of the blood-aqueous barrier. With increasing demand for ophthalmic surgery, bromfenac and other treatments are likely to be important components in the treatment of inflammatory conditions after cataract surgery, decreasing pain and contributing to favourable visual outcomes. KeywordsBromfenac, ophthalmic non-steroidal anti-inflammatory drugs, ocular inflammation, cystoid macular oedema, ocular pain Treatments for Ocular InflammationThe two main treatments for ocular inflammation are topical corticosteroids and non-steroidal anti-inflammatory drugs (NSAIDs).Corticosteroids interfere with the activity of phospholipase A 2 , thereby inhibiting the release of arachidonic acid metabolites, includingPGs.2 By contrast, NSAIDs non-specifically and irreversibly inhibit the synthesis of PGs by directly interfering with the activity of COX-1 and COX-2 (see Figure 1). 2 CorticosteroidsThe corticosteroids, which are considered the gold standard for the treatment of ocular inflammation, are associated with an increased incidence of adverse events that warrant their judicious use. Most NSAIDs are weakly acidic drugs that ionise at the pH of lacrimal fluid, thus limiting their permeability through the ionic cornea, which has an isoelectric point (pI) of 3.2. 6 Reducing the pH of the formulation increases the un-ionised fraction of the drug, enhancing permeation. Being acidic, NSAIDs are inherently irritant, and reducing the pH of the formulation further increases their irritation potentia...

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24-Hour Evaluation of the Ocular Distribution of ¹⁴C-Labeled Bromfenac Following Topical Instillation into the Eyes of New Zealand White Rabbits

Cited by 48 publications

References 10 publications

Topical Bromfenac as an Adjunctive Treatment With Intravitreal Ranibizumab for Exudative Age-Related Macular Degeneration

Topical Bromfenac as an Adjunctive Treatment With Intravitreal Ranibizumab for Exudative Age-Related Macular Degeneration

Topical Treatment With Bromfenac Reduces Retinal Gliosis and Inflammation After Optic Nerve Crush

New Look at Ocular Inflammation Control – Powerful and Fast-acting Twice-daily Bromfenac for a Novel Standard in the Treatment of Inflammation

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24-Hour Evaluation of the Ocular Distribution of 14C-Labeled Bromfenac Following Topical Instillation into the Eyes of New Zealand White Rabbits

Cited by 48 publications

References 10 publications

Topical Bromfenac as an Adjunctive Treatment With Intravitreal Ranibizumab for Exudative Age-Related Macular Degeneration

Topical Bromfenac as an Adjunctive Treatment With Intravitreal Ranibizumab for Exudative Age-Related Macular Degeneration

Topical Treatment With Bromfenac Reduces Retinal Gliosis and Inflammation After Optic Nerve Crush

New Look at Ocular Inflammation Control – Powerful and Fast-acting Twice-daily Bromfenac for a Novel Standard in the Treatment of Inflammation

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Product

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24-Hour Evaluation of the Ocular Distribution of ¹⁴C-Labeled Bromfenac Following Topical Instillation into the Eyes of New Zealand White Rabbits