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Nanomedicines for Ocular NSAIDs: State-of-the-Art Update of the Safety on Drug Delivery
Published in Lajos P. Balogh, Nano-Enabled Medical Applications, 2020
Joana R. Campos, Joana Araújo, Elisabet Gonzalez-Mira, Maria A. Egea, Elena Sanchez-Lopez, Marta Espina, Selma B. Souto, Maria L. Garcia, Eliana B. Souto
NSAIDs are effective drugs compared to placebos for the relief of anterior chamber inflammation [34]. The goals of topical prophylactic NSAIDs treatment include the prevention of intraoperative miosis [35], management of postoperative inflammation, prevention or treatment of CME [36] and reduction of ocular pain [37]. There are four NSAIDs currently approved by the U.S. Food and Drug Administration (FDA) for the treatment of post operative inflammation after cataract surgery [38], namely kerotolac, bromfenac, diclofenac, and nepafenac. This latter is the only prodrug NSAID and thus requires conversion to its more active state, amfenac, through intraocular enzymatic hydrolysis [39]. A study compared aqueous humour concentrations of these four NSAIDs after administration in patients having cataract surgery and the cyclooxigenase-1 (COX-1) and COX-2 inhibitory activity was also determined, via in vitro measurement of PG inhibition to rank order the potency of the molecules, showing nepafenac significantly greater ocular bioavailability than the others and amfenac greater potency at COX-2 inhibition [38]. Furthermore, diclofenac, nepafenac, ketorolac, and bromfenac have relatively greater significant effects than other topical NSAIDs. NSAIDs were first approved by the FDA to prevent surgically induced miosis [40]. Newer NSAIDs are being investigated for their ability to reduce the incidence of CME after cataract surgery. CME is a major complication after cataract surgery and remains the primary cause of surgical visual disorders [41]. Whether NSAIDs can effectively prevent the development of CME is still controversial. Recent comprehensive analyses investigated the ability of NSAIDs to reduce the incidence of CME after cataract surgery, but a positive effect was not observed [40]. Although ambiguity surrounds NSAIDs regarding CME prevention, NSAIDs play an important role in cataract surgery.
Ocular nonsteroidal inflammatory drugs: where do we stand today?
Published in Cutaneous and Ocular Toxicology, 2020
S. A. Kandarakis, P. Petrou, E. Papakonstantinou, D. Spiropoulos, A. Rapanou, I. Georgalas
Several studies have focussed on investigating the local pharmacokinetics of ophthalmic NSAIDs, showing that dosing and frequency of administration differs significantly. After a single topical application, peak aqueous drug levels are detectable for: diclofenac 0.1% (82 ng/mL; 2.4 h peak), furbiprofen 0.03% (60 ng/mL; 2.0 h peak), nepafenac 0.1% (205.3 ng/mL; peak 30 min), amfenac (70.1 ng/mL), ketorolac 0.4% (57.5 ng/mL; 60 min), and bromfenac 0.09% (25.9 ng/mL)18,19. On the other hand, there is a paucity in literature, regarding the vitreous levels of NSAIDs after topical administration, constituting uncertain their ability to suppress prostaglandin synthesis in the retina/choroid. A single study measured vitreous drug levels in patients who received ketorolac 0.4% four times daily, bromfenac 0.09% two times daily, or nepafenac 0.1% three times daily for three days before vitrectomy surgery. Vitreous levels of ketorolac, bromfenac, and amfenac were reported as 2.8 ng/mL, 0.96 ng/mL, and 2.0 ng/mL, respectively, but only ketorolac resulted in significantly lower vitreous PGE2 levels compared to placebo20.
Retinal Vascular Caliber Changes After Topical Nepafenac Treatment for Diabetic Macular Edema
Published in Current Eye Research, 2018
Ferhat Evliyaoğlu, Çetin Akpolat, Muhammed Mustafa Kurt, Osman Çekiç, Mustafa Nuri Elçioğlu
In animal studies, there are some indications that topical nepafenac can penetrate sufficiently into the posterior segment to have a direct effect on the retinal vasculature.21,22Nepafenac is a prodrug that converts to amfenac, after which it reaches its highest concentration in the choroid and retina. Unlike other conventional NSAIDs, nepafenac also inhibits prostaglandin formation in the vitreous, which increases its effect on the retina.23 NSAIDs are known to reduce vascular hyperpermeability associated with tissue inflammation, and increased inflammatory markers have been found in diabetic retinopathy.24
Design, fabrication, and characterization of graft co-polymer assisted ocular insert: a state of art in reducing post-operative pain
Published in Drug Development and Industrial Pharmacy, 2020
Prakash N. Kendre, Pooja D. Kadam, Shirish P. Jain, Somnath K. Vibhute, Ajinkya K. Pote
Nepafenac is a non-steroidal anti-inflammatory prodrug (NSAID) that is usually sold as prescription eye drops. It is used to treat the pain and inflammation associated with cataract surgery [30]. It has several advantages over other ophthalmic NSAIDs. First, it has a unique prodrug structure. Prodrugs are the inactive forms of drugs that get converted into active forms after metabolic conversion in the body [29]. Nepafenac rapidly penetrates the cornea. After nepafenac penetrates the cornea, it is deaminated by intraocular hydrolases to amfenac [(2-amino-3-benzoyl phenyl) acetate], a potent inhibitor of COX-1 and COX-2 [31].