Pharmacokinetics and Efficacy of Topically Applied Nonsteroidal Anti-Inflammatory Drugs in Retinochoroidal Tissues in Rabbits

Kida, Tetsuo; Kozai, Seiko; Takahashi, Hiroaki; Isaka, Mitsuyoshi; Tokushige, Hideki; Sakamoto, Taiji

doi:10.1371/journal.pone.0096481

Cited by 32 publications

(47 citation statements)

References 40 publications

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“…It also increases the drug's potency against COX-1 and COX-2 compared with amfenac [9]. For instance, the half maximal inhibitory concentrations of bromfenac, amfenac and diclofenac were 5.56, 15.3 and 55.5 nM, respectively, for human-derived COX-1 and 7.45, 20.4 and 30.7 nM, respectively, for human-derived COX-2 [9].…”

Section: Introductionmentioning

confidence: 99%

“…Its mechanism of action is believed to result from its potent (in the nM range) inhibitory effect on cyclooxygenase (COX)-1 and -2 and, thus, on prostaglandin synthesis [7,9]. The presence of bromine in the bromfenac molecule increases the lipophilicity of bromfenac, with the drug being more lipophilic than amfenac (another NSAID) [partition coefficient (log P) of 2.23 vs. 1.23] [10].…”

Section: Introductionmentioning

confidence: 99%

“…The presence of bromine in the bromfenac molecule increases the lipophilicity of bromfenac, with the drug being more lipophilic than amfenac (another NSAID) [partition coefficient (log P) of 2.23 vs. 1.23] [10]. It also increases the drug's potency against COX-1 and COX-2 compared with amfenac [9]. For instance, the half maximal inhibitory concentrations of bromfenac, amfenac and diclofenac were 5.56, 15.3 and 55.5 nM, respectively, for human-derived COX-1 and 7.45, 20.4 and 30.7 nM, respectively, for human-derived COX-2 [9].…”

Section: Introductionmentioning

confidence: 99%

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Bromfenac Ophthalmic Solution 0.07 %: A Review of Its Use After Cataract Surgery

Hoy

2015

Clin Drug Investig

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The nonsteroidal anti-inflammatory drug bromfenac has recently been reformulated with a lower pH to facilitate a reduction in the concentration of bromfenac (to 0.07%) while ensuring an ocular bioavailability similar to that of the 0.09% formulation. Bromfenac ophthalmic solution 0.07% (hereafter referred to as bromfenac 0.07%) [Prolensa(®)] is a once-daily topical ophthalmic solution available in the USA and Canada for the treatment of postoperative inflammation and the reduction of ocular pain in patients who have undergone cataract surgery. In an integrated analysis of two multicentre, phase III studies, bromfenac 0.07% was significantly more effective than placebo in reducing ocular inflammation and pain. In these studies, bromfenac 0.07% was well tolerated, with significantly lower incidences of adverse events, and adverse events affecting the study eye than with placebo. The most common adverse events in the study eye (eye pain, anterior chamber inflammation, foreign body sensation, photophobia, conjunctival hyperaemia and corneal oedema) occurred in numerically fewer bromfenac 0.07% than placebo recipients. Thus, current evidence suggests once-daily bromfenac 0.07% extends the treatment options currently available for the management of postoperative inflammation and pain following cataract surgery.

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Section: Introductionmentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

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Bromfenac Ophthalmic Solution 0.07 %: A Review of Its Use After Cataract Surgery

Hoy

2015

Clin Drug Investig

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“…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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“…37 Bromfenac and nepafenac are NSAIDs that have excellent corneal and sclera penetration and have both been shown to reach the retina in therapeutic doses in animals, 38,39 although bromfenac would appear to be superior. 40 Recently, there has been interest in using bromfenac, ketorolac, and other NSAIDs as an adjunct to anti-VEGF drugs or intravitreal steroids 41 for macular edema from DME, RVO, 42 uveitis, 41 and also choroidal neovascularization (CNV), as there is evidence that COX plays an important role in promoting angiogenesis in CNV. 50 Nakano and others have demonstrated that steroid eye drops (difluprednate ophthalmic emulsion) can be effective in reducing retinal thickness in eyes with DME, in eyes that have been vitrectomized, 51 and in eyes prior to vitrectomy.…”

Section: Nonsteroidal Anti-inflammatory Drugsmentioning

confidence: 99%

Recent Advances in Topical Therapeutics for Vitreoretinal Diseases

Gibson¹,

McGinnigle

2015

US Ophthalmic Review

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Amongst other attributes, the ideal drug for retinal disorders should be easy to administer, safe, have a long duration of action, and be costeffective. Needless to say, to date, no such drug exists as far as we are aware, but how close does topical delivery come to meeting these aspirations? Compared with intravitreal drug delivery, topical delivery has some obvious advantages and disadvantages and these are summarized in Table 1.Maurice wrote a seminal review of this subject in 2002, in which he was particularly interested in the passage of drugs delivered by eye AbstractEye drops are convenient for patients, but achieving therapeutic doses and maintaining sustained drug release without frequent re-application to treat diseases of the retina has been largely unsuccessful. Topical administration of drugs is hindered by the anatomy, physiology, and biochemistry of the eye and its highly effective defence mechanisms. Advances in nanotechnology have led to the experimental use of topical permeation-enhancing liposomes, emulsions, and microspheres to enhance absorption and penetration of drugs across membranes; allow controlled release of the drug; and to target drugs at distinct tissues to allow sufficient local bioavailability. In the near future it is hoped that improved technologies may provide means of sustained topical drug delivery for retinal therapy, with improved side-effect profiles and reduced cost compared with currently available clinical treatments.

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Pharmacokinetics and Efficacy of Topically Applied Nonsteroidal Anti-Inflammatory Drugs in Retinochoroidal Tissues in Rabbits

Cited by 32 publications

References 40 publications

Bromfenac Ophthalmic Solution 0.07 %: A Review of Its Use After Cataract Surgery

Bromfenac Ophthalmic Solution 0.07 %: A Review of Its Use After Cataract Surgery

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

Recent Advances in Topical Therapeutics for Vitreoretinal Diseases

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