The Influence of Topical Perioperative Nepafenac on Retinal Vasculature Following Phacoemulsification Using Optical Coherence Tomography Angiography: A Randomized Clinical Trial.

PURPOSE: To investigate topical nepafenac drops (TND) effect on retinal vasculature following uneventful phacoemulsification. METHODS: 54 eyes were randomly assigned to G1: TND 3 days preoperatively and 1 month postoperatively; G2: TND for 1 month postoperatively; and G3 no TND (control). BCVA, macular OCTA were compared baseline, 1 week and 1 month. RESULTS: No statistically significant differences found between 3 groups in OCTA parameters during study visits. However, at 1 month (compared to baseline) there were a statistically significant increase in superficial capillary plexus (SCP) capillary vessel density (CVD) in G2 (p=0.036); increase in central foveal thickness (CFT) in G2 (p=0.011) and G3 (control) (p=0.001); and reduced number of patients with SCP disorganization in G2 (p=0.04). There were no significant correlation/association between most of OCTA parameters and final BCVA. CONCLUSION: TND use perioperative did not show any effect on retinal OCTA microvasculature and might affect macular edema by other mechanisms.

In Vitro Drug Release Testing Method For Nepafenac Ophthalmic Suspension.

In vitro release test (IVRT) method is important to monitor batch-to-batch quality variations during pharmaceutical manufacturing and also to show the pharmaceutical equivalence of a generic product with the innovator. To fulfil regulatory requirements for approval of a generic ophthalmic suspension product, in vitro release study is required. No compendial or non-compendial method is available for IVRT of nepafenac ophthalmic suspension. Current research is aimed to screen various approaches using different conventional and non-conventional instruments to suggest the most suitable technique appropriate for nepafenac ophthalmic suspension followed by optimization of method parameters and validation. The trials used the paddle apparatus (USP Type-2) with dialysis sacs, the flow-through cell apparatus (USP Type-4), the rotating bottle apparatus, and the Franz diffusion cell apparatus. With the USP Type-4 apparatus drug release was found to be ∼ 83% in the simulated tear fluid (STF) of pH 7.4 in 120 min that increased to ∼ 97% upon the addition of surfactant sodium lauryl sulfate (SLS). With USP Type-2 and Franz diffusion cell apparatus, the drug release was either slow or not reaching close to the complete release. Whereas, in the case of the rotating bottle apparatus, a burst release profile was observed. The estimation of the drug release was done by the HPLC method and all the method validation parameters like specificity, accuracy, linearity, and precision were found to be within acceptance criteria.

Comparison of the efficacy of Diclofenac 0.1% and Nepafenac 0.1% on anterior chamber cells in patients undergoing cataract surgery: A prospective clinical practice trial.

Objectives: To compare the efficacy of topical Nepafenac 0.1 % and Diclofenac 0.1% eye drops in reducing the aqueous cells in the anterior chamber in an un-eventful post cataract surgery. Methods: This prospective, clinical trial was conducted at an Eye OPD of Qazi Hussain Ahmad Medical Complex, Nowshera from January till December 2021. Ophthalmic assessment included Visual acuity (VA), slit-lamp examination, Intraocular pressure (IOP), Central macular thickness (CMT) by Optical coherence tomography (OCT) and anterior chamber-aqueous cells measurement pre-operatively and at day 1st, 2nd, 4th and 8th week post-operatively. Patients were randomly allocated to topical diclofenac 0.1% (TD) four times a day and nepafenac 0.1% (TN) three times a day for four weeks each along with topical steroids and antibiotics. Results: Seventy patients (70) were randomly distributed into two treatment arms of 35 each. In both the arms VA improved which achieved a level of statistical significance post-operatively, however statistically insignificant difference was observed between the groups at 8th week follow up visit (p= 0.62). However, IOP and CMT values didn't achieve statistical significance between the arms pre and post operatively. In TN arm, level of AC-cells at 2nd and 4th week post-operatively were significantly lower (10.54 ± 4.05 and 08.20 ± 4.44) than TD arm (11.28 ± 5.04 and 09. 66 ± 5.50) with statistically significant difference (p < 0.05). Conclusions: Topical Nepafenac 0.1% was more effective in suppressing the anterior chamber inflammation as compared to diclofenac during the early few post-operative weeks.

Cyclodextrin-enabled nepafenac eye drops with improved absorption open a new therapeutic window.

Nepafenac is a highly effective NSAID used for treating postoperative ocular inflammation and pain after cataract surgery and its advantage over conventional topical NSAIDs has been proved many times. However, Nevanac® is a suspension eye drop, which clearly lacks patient compliance causing irritation, blurred vision, foreign body sensation along with problematic dosage due to its sticky, inhomogeneous consistence. In this study, nepafenac containing eye drops were prepared using hydroxypropyl-ß-cyclodextrin to ensure complete dissolution of nepafenac, sodium hyaluronate to provide mucoadhesion and adequate viscosity and a preservative-free officinal formula, Oculogutta Carbomerae containing carbomer (just like Nevanac®), therefore providing a similar base for the new formulations. According to an experimental design, 11 formulations were tested in vitro including two reference formulations by measuring their viscosity, mucoadhesion, drug release and corneal permeability. Finally, two formulations were found promising and investigated further on porcine eyes ex vivo and corneal distribution of nepafenac was determined by RAMAN mapping. The results showed that one formulation possessed better bioavailability ex vivo than Nevanac® 0.1 % suspension, while the other formulation containing only 60 % of the original dose were ex vivo equivalent with Nevanac® opening the way to nepafenac-containing eye drops with better patient compliance in the future.

OCT imaging of macular cysts and treatment response with nepafenac in mucopolysaccharidosis type 1.

PURPOSE: Mucopolysaccharidosis Type I (MPS I) is an autosomal recessive lysosomal storage disorder characterized by a defect in the enzyme alpha-L-iduronidase. Glycosaminoglycan accumulation causes ocular involvement such as corneal clouding or pigmentary retinopathy. Here we report bilateral macular cysts in mucopolysaccharidosis type I (MPS I) that responds to nepafenac treatment. METHODS: Retrospective case report. RESULTS: A 27-year-old woman with MPS I (Scheie phenotype) was complaining of slightly blurred vision. She had been on alpha-L-iduronidase enzyme replacement therapy for ten years. Best-corrected visual acuity was 20/25 in both eyes. Biomicroscopy was normal. Dilated fundus examination revealed pigmentary retinopathy. Optical coherence tomography (OCT) detected macular cysts in inner and outer nuclear layers, with preservation of ellipsoid zone and IS/OS line. There was no dye leakage on fluorescein angiography. Macular cysts regressed partially after one month with topical nepafenac 0.1% four times a day. BCVA improved to 20/20 in both eyes. CONCLUSIONS: This is the first report of bilateral macular cysts that was demonstrated with OCT and treated with topical nepafenac in a patient with MPS I. Because the symptoms of our patient were mild, large-scaled cohort studies are required to ascertain the real prevalence of macular cysts in MPS I. It may also be beneficial to do more research on the possible benefits of nepafenac on the retinal manifestations of MPS.

Comparison of once daily dose of 0.3% nepafenac alone and three times dose of 0.1% nepafenac alone in pain and inflammation control after phacoemulsification.

PURPOSE: To compare the efficacy of a once-daily dose of 0.3% nepafenac and three times daily dose of 0.1% nepafenac in controlling pain and inflammation following phacoemulsification. METHODS: In this prospective randomized control single-blind study. patients who underwent uneventful phacoemulsification were divided into two groups. Group A received 0.1% nepafenac eye drops three times/day for 4 weeks and group B received 0.3% nepafenac eye drops once daily for 4 weeks following phacoemulsification. All the patients received moxifloxacin 0.5% eye drops four times/day for 2 weeks. None of the patients in any group received any form of corticosteroids. RESULTS: The mean age of the patients in group A was 63.55 ± 8.5 years, while in group B, it was 60.05 ± 7.76 years. There was no significant result in the preoperative baseline demographics and intraoperative parameters between both the groups. The results were statistically insignificant in terms of inflammatory markers between both groups on day 1. But, on day 7, group B showed better results in terms of lid edema, conjunctival congestion, and anterior chamber cells. The patients in group B also perceived significantly less pain on day 1 (P = 0.02) and day 7 (P < 0.001). The central macular thickness was also significantly lower in group B at day 30. (: P < .001) and day 90 (P < .001), respectively. CONCLUSION: Once-daily dose of higher concentrated nepafenac (0.3%) is equally effective and shows better results than 0.1% nepafenac for pain and inflammation control.

Topical 0.1% Nepafenac versus 0.09% Bromfenac Eye Drops for Inflammation after Laser Peripheral Iridotomy: A Randomized Controlled Trial.

PURPOSE: To assess the safety and efficacy of 0.1% nepafenac versus 0.09% bromfenac eye drops in controlling inflammation after neodymium yttrium-aluminum-garnet (YAG) laser peripheral iridotomy (LPI). DESIGN: Single-masked, single-center, randomized controlled trial. PARTICIPANTS: One hundred and sixty eyes of patients with primary angle-closure suspect (PACS) and primary angle closure (PAC) undergoing bilateral LPI. METHODS: Patients were randomized in a 1:1 ratio to receive 0.1% nepafenac thrice daily or 0.09% bromfenac eye drops twice daily for 2 weeks after neodymium YAG LPI. Assessment was performed by masked investigators at 2 weeks after LPI. A Glaucoma Symptom Scale (GSS) questionnaire was administered both at baseline and 2 weeks after LPI. Subjective comfort scores to the study medications were assessed on the basis of a Likert scale at 2 weeks after LPI. In patients with bilateral PACS or PAC, the right eye was analyzed, and in asymmetrical disease (i.e., when one eye had PACS and the other eye had PAC), the eye with PAC was analyzed. MAIN OUTCOME MEASURES: The primary outcome (end point) was uncontrolled inflammation, defined as symptomatic inflammation within 1 week after LPI, the presence of anterior chamber cells at 2 weeks, or rebound inflammation after medication discontinuation. The secondary outcome was patient-reported comfort levels with study medications based on the GSS and Likert scale. RESULTS: At 2 weeks after LPI, 7 patients (6 with PACS and 1 with PAC) in the nepafenac group and 2 patients with PACS in the bromfenac group achieved the primary end point, without a difference between the medication groups (P = 0.09). Post-LPI burning, smarting, and stinging was more common in the bromfenac group (P = 0.01), which also had a higher comfort score on the Likert scale (P = 0.004). The need for repeat LPI was comparable (10.0% in the nepafenac group vs. 15.4% in the bromfenac group; P = 0.22). A multivariate analysis revealed that a greater number of laser shots was associated with the need for repeat LPI (odds ratio, 1.05; 95% confidence interval, 1.00-1.10; P = 0.04). CONCLUSIONS: Topical 0.09% bromfenac is noninferior to 0.1% nepafenac in controlling inflammation after LPI in eyes with PACS and PAC. Nepafenac may be associated with higher patient-reported comfort.

A prospective randomized clinical trial comparing nepafenac, intravitreal triamcinolone and no adjuvant therapy for epiretinal membrane.

PURPOSE: To compare the efficacy of topical nepafenac 0.1% versus intravitreal triamcinolone acetonide (IVTA) at the conclusion of vitrectomy surgery versus no adjuvant therapy (NAT) in improving macular morphology post-operatively in patients undergoing vitrectomy for epiretinal membrane (ERM), as measured by optical coherence tomography (OCT) imaging and best-corrected visual acuity (BCVA). METHODS: Design: Prospective randomized clinical trial Setting: Multi-centre 80 patients scheduled to undergo vitrectomy surgery for idiopathic ERM were randomized to receive either IVTA (4 mg/0.1 cc) at the end of surgery, topical nepafenac sodium 0.1% TID for 1 month post-operation or no adjuvant treatment (NAT). Optical coherence tomography (OCT) imaging, best-corrected visual acuity and intraocular pressure (IOP) were measured before surgery, and 1 and 2 months post-operation. RESULTS: Although all three groups showed reduction in macular thickness post-operation, the NAT group showed the most improvement, with a reduction of 136.18 ± 29.84 µm at two months. There was no statistically significant difference in macular thickness between the groups at each time point, p = 0.158. The NAT group also had the best recovery in BCVA with an improvement of 0.207 logMAR (10.35 letters) at two months post-operation. There was no statistically significant difference in BCVA between the groups, p = 0.606. There was statistically significant difference in the IOP between the three groups, p = 0.04 only at 1-month visit. The IVTA group had the highest rise in average IOP at both 1 and 2 months post-operation (2.72 and 1.58 mmHg, respectively). CONCLUSION: Our study data suggest there was no advantage in the use of topical nepafenac or IVTA for post-vitrectomy ERM surgery.

Closure of Full-Thickness Macular Holes Associated with Macular Edema with Medical Therapy.

PURPOSE: The purpose of this study was to report the closure of macular hole without surgery in 7 cases using medical therapies. METHODS: The retrospective review of 7 cases of full-thickness macular holes, which closed after medical therapy without surgery. RESULTS: Seven eyes of 7 patients developed full-thickness macular holes, which initially closed on medical therapy without surgery. Six patients were kept on maintenance therapy; 1 recurred and 5 did not develop recurrence. One patient was taken off of maintenance therapy and later developed recurrent macular hole requiring macular hole surgery. CONCLUSIONS: Medical therapy to decrease macular edema may facilitate macular hole closure and should be considered, especially for small macular holes with significant edema. Reopening of macular holes may occur after stopping topical maintenance therapy for macular edema, which occurred at 10 weeks and 9 months after maintenance therapy was discontinued or markedly tapered.

Nepafenac in cataract surgery.

The role of topical non-steroidal anti-inflammatory drugs (NSAIDs) in routine cataract surgery has been established since decades. Topical NSAIDs have been shown to reduce postoperative ocular inflammation and pain, preserve intraoperative mydriasis, and reduce the risk of postoperative cystoid macular oedema, whilst carrying a very low side-effect profile. Nepafenac is one of the currently available topical NSAIDs. The studies have shown that is has a high ocular penetration, allowing for potentially better results than other NSAIDs. This review gathers the current literature on the role of nepafenac in cataract surgery aiming to help surgeons maximise the benefits of its use to achieve improved surgical outcomes.

Nepafenac for cystoid macular oedema secondary to paclitaxel.

Paclitaxel is used to treat a wide range of malignant tumours. This type of drug is known to cause ocular adverse effects, with cystoid macular oedema being a known, but rare complication, of this therapy. Although most cases resolve after discontinuation of the drug, several authors have attempted various treatments to accelerate resolution, or when paclitaxel therapy cannot be discontinued. A case is presented of a 62 year-old man who presented with decreased visual acuity due to bilateral cystoid macular oedema after administration of paclitaxel for oesophageal cancer. As part of the study, optical coherence tomography angiography (OCTA) was performed at the time of diagnosis, and later when the symptoms subsided. Nepafenac eye drops were prescribed as treatment.

Nepafenaco para edema macular cistoideo secundario a paclitaxel / Nepafenac for cystoid macular oedema secondary to paclitaxel

El paclitaxel es utilizado para tratar una amplia gama de tumores malignos. Se sabe que estos fármacos causan efectos adversos oculares, siendo el edema macular cistoide una complicación conocida pero rara de esta terapia. Aunque la mayoría de los casos se resuelven después de la interrupción del fármaco, varios autores han intentado diversos tratamientos para acelerar la resolución o cuando la terapia con paclitaxel no puede suspenderse. Presentamos un caso de un varón de 62 años que presentó disminución de la agudeza visual debido a edema macular cistoideo bilateral después de la administración de paclitaxel para cáncer de esófago; como parte del estudio se realizó angiografía por tomografía de coherencia óptica en el momento del diagnóstico y posteriormente cuando el cuadro remitió. Como tratamiento se prescribió colirio de nepafenaco (AU)

Paclitaxel is used to treat a wide range of malignant tumours. This type of drug is known to cause ocular adverse effects, with cystoid macular oedema being a known, but rare complication, of this therapy. Although most cases resolve after discontinuation of the drug, several authors have attempted various treatments to accelerate resolution, or when paclitaxel therapy cannot be discontinued. A case is presented of a 62 year-old man who presented with decreased visual acuity due to bilateral cystoid macular oedema after administration of paclitaxel for oesophageal cancer. As part of the study, optical coherence tomography angiography (OCTA) was performed at the time of diagnosis, and later when the symptoms subsided. Nepafenac eye drops were prescribed as treatment (AU)

Comparison between 0.1% Nepafenac and 1% Prednisolone Eye Drop in Postoperative Management Following Micro-incisional Cataract Surgery.

PURPOSE: To compare the efficacy of 0.1% nepafenac and 1% prednisolone acetate eye drop in postoperative inflammation control in micro-incisional cataract surgery. METHODS: We conducted a prospective, randomized, comparative, single-blind study. All the patients underwent temporal 2.2-mm micro-incisional cataract surgery. They were randomized into two groups (group A and B). Group A received 0.1% nepafenac eye drops 4 times/day for 4 weeks and group B received 1% prednisolone acetate eye drops in tapering doses for 4 weeks after surgery. Both the groups received moxifloxacin 0.5% eye drops 4 times/day for 2 weeks. Patients were examined on 1st, 7th, and 30th postoperative days and parameters of postoperative inflammation were evaluated and noted at each visit. RESULTS: A total of 200 patients were enrolled in the study. However, five patients lost to follow up, group A had 97 and group B had 98 patients respectively. Results were statistically insignificant in terms of the difference in lid edema, conjunctival congestion, corneal edema, anterior chamber cells and flare between the two groups with p-values >0.05 for each parameter at each visit. However, the difference in mean central macular thickness between the groups was significant (205.713 ± 17.14 vs. 220.984 ± 32.83 in group A and B, respectively, p ≤ 0.001) at 1 month. Also, the mean pain score was significantly lower (p = 0.018) in the nepafenac group at day 7 of surgery. CONCLUSIONS: Nepafenac is equally effective and non-inferior to prednisolone acetate in suppression and prevention of inflammation in postoperative period.

Efficacy of Nepafenac versus Flurbiprofen in Maintaining Intraoperative Mydriasis During Phacoemulsification: A Comparative Study.

PURPOSE: To compare the efficacy of topical nepafenac (0.1%) with flurbiprofen (0.03%) in maintaining intra-operative mydriasis during phacoemulsification surgery. PATIENTS AND METHODS: This study comprised of 160 patients, who were divided into two arms of 80 each (arms A and B) after randomisation. Pre-operatively, all patients received one drop of tropicamide 0.8% and phenylephrine 5% (combination), 4 times, at an interval of 15 minutes on the day of surgery. Thereafter, Nepafenac drop in arm A/Flurbiprofen drop in arm B was administered 4 times, at an interval of 15 minutes keeping a gap of 10 minutes between tropicamide-phenylephrine and any of the experimental drugs. Phacoemulsification was performed one hour after the administration of last drop. Both vertical and horizontal pupillary diameter were measured at three steps; immediately before the surgical incision (baseline), at the end of emulsification of nucleus (before irrigation and aspiration) and at the end of surgery (after stromal hydration). RESULTS: The difference in pupillary diameter between two groups, was statistically insignificant for vertical diameter (P = 0.08) and horizontal diameter (P = 0.28) at the start of surgery. On the other hand, pupillary diameter difference was statistically significant after emulsification of nucleus and at the end of surgery as well when both vertical (P < 0.05) and horizontal diameter (P < 0.05) were considered. The total reduction in pupillary diameter (both vertically and horizontally) was significantly less in the Nepafenac as compared to Flurbiprofen group (P < 0.05). Analysis of mean cumulative dissipated energy did not document any appreciable difference between the two groups. Phacoemulsification time analysis yielded statistically significant results (P = 0.004) between the Nepafenac and Flurbiprofen group. CONCLUSION: In the present study, topical Nepafenac (0.1%) proved to be more efficacious in maintaining intra-operative mydriasis during phacoemulsification surgery as compared to topical Flurbiprofen (0.03%).

Effect of nepafenac 0.1% on retinal thickness after cataract surgery in patients without risk factors for cystoid macular edema.

AIM: To evaluate the effect of topical preoperative nepafenac 0.1% treatment on postoperative macular edema using optical coherence tomography (OCT) after uncomplicated cataract surgery. METHODS: Ninety eyes of 90 patients without any risk factors were included in the study. The patients were assigned to three groups: group 1, treated with topical prednisolone acetate 1%; group 2, treated with topical nepafenac 0.1% in addition to prednisolone acetate (1%); and group 3, those who started receiving nepafenac 0.1% treatment 3d prior to surgery and continued the treatment postoperatively in addition to prednisolone acetate (1%). Central retinal thickness (CRT) and macular volume values were recorded using OCT at weeks 3 and 6. RESULTS: The increases in macular volume in the central 1 mm area after 3 and 6wk were significantly lower in patients who used prophylactic topical nepafenac preoperatively (group 3) compared with those in group 1 (P=0.028 and 0.008, respectively). No significant differences in the increase in macular volume and CRT were noted between groups 2 and 3 (P>0.05). In group 1, the increases in macular volume in the central 3 mm area at weeks 3 and 6 were significantly higher than that in group 2 and 3 (3rd week, P=0.004; 6th week, P=0.005). CONCLUSION: Nepafenac 0.1% treatment in addition to topical steroids after uncomplicated cataract surgery reduce the increase in macular volume in the early postoperative period.

Efficacy of Topical Nepafenac 0.3% in the Management of Postoperative Cystoid Macular Edema.

PURPOSE: To assess the effect of twice-daily nepafenac ophthalmic suspension 0.3% on postoperative cystoid-macular-edema (CME). PATIENTS AND METHODS: In this prospective, clinic-based, non-randomized case-series, 21 patients (21 eyes) were enrolled with either acute or chronic postoperative CME after cataract extraction. Patients were treated with twice-daily nepafenac 0.3% drops, and followed for at least a 4-month period. Best-corrected visual acuity (BCVA) and spectral-domain optical coherence tomography (SD-OCT)-derived central retinal thickness (CRT) were measured. RESULTS: From 21 patients, eight presented with acute postoperative CME and 13 with chronic CME. Mean follow-up was 4.82±1.24 months. No adverse events were reported during the study. Baseline BCVA was 0.49±0.36 logMAR and improved to 0.36±0.42 logMAR at the last follow-up visit (P<0.005). CRT decreased from 450.40±90.74 µm at baseline to 354.60±81.49 µm (P<0.05), following treatment. CONCLUSION: Our outcomes strongly suggest that administrating nepafenac 0.3% drops on a twice-daily regimen could be a promising alternative for the management of postoperative CME. Additional studies are necessary to further validate our results.

Design, fabrication, and characterization of graft co-polymer assisted ocular insert: a state of art in reducing post-operative pain.

PURPOSE: Targeted delivery of drugs at appropriate concentrations to ocular tissues is required to avoid wastage. Hence, advanced systems that maximize the release of poorly soluble drugs and deliver them at ocular sites must be designed. METHODS: In this study, Soluplus® (polyvinyl caprolactam-polyvinyl acetate-polyethylene glycol-graft copolymer) was selected as a solubilizer as well as film former for preparing ocular inserts and polyethylene glycol 400 (PEG-400) as a plasticizer. On the basis of an initial phase solubility study, the maximum concentration of Soluplus® possible was used for developing the inserts. An optimized formulation was obtained using a 32-factorial design. Two factors at three levels were used to design the ocular inserts. Soluplus® (X 1) and the plasticizer, PEG-400 (X 2), were set as the independent variables at various levels, and the Rel4h (drug release in 4 h, Y 1) and tensile strength (Y 2) were set as the dependent variables. A pre-formulation study was conducted to select suitable materials. RESULTS: Various physico-chemical parameters of the optimized formulation, including the tensile strength and folding endurance, were studied using FT-IR, DSC, XRD, and SEM. An in vitro dissolution study was conducted to determine the amount of drug released. There was no redness, swelling, or watering of the rabbit eye. CONCLUSION: It was concluded that the ocular inserts of the poorly soluble nepafenac developed using a graft-co-polymer enhanced the solubility and utilization of the drug for a prolonged period.

Degradation profile of nepafenac in aqueous solution and structural characterization of a novel degradation product.

The stability of the anti-inflammatory drug nepafenac was investigated in aqueous solutions containing hydroxypropyl-ß-cyclodextrin at three different values of pH and degradation products were identified. (2-Amino-3-benzoyl)-oxoacetic acid, previously not reported as nepafenac-related impurity, was isolated and structurally characterized by NMR and ESI-MS analyses. It was also shown that the formation of this α-ketoacid from nepafenac in alkaline water/organic cosolvent solution occurs through an aerobic oxidation of the key intermediate 7-benzoyl-1,3-dihydro-indol-2-one, which in some extent is protected from oxidation in the presence of the cyclodextrin additive.

In Vitro and Ex Vivo Evaluation of Nepafenac-Based Cyclodextrin Microparticles for Treatment of Eye Inflammation.

The aim of this study was to design and evaluate novel cyclodextrin (CD)-based aggregate formulations to efficiently deliver nepafenac topically to the eye structure, to treat inflammation and increase nepafenac levels in the posterior segment, thus attenuating the response of inflammatory mediators. The physicochemical properties of nine aggregate formulations containing nepafenac/γ-CD/hydroxypropyl-ß (HPß)-CD complexes as well as their rheological properties, mucoadhesion, ocular irritancy, corneal and scleral permeability, and anti-inflammatory activity were investigated in detail. The results were compared with a commercially marketed nepafenac suspension, Nevanac® 3 mg/mL. All formulations showed microparticles, neutral pH, and negative zeta potential (-6 to -27 mV). They were non-irritating and nontoxic and showed high permeation through bovine sclera. Formulations containing carboxymethyl cellulose (CMC) showed greater anti-inflammatory activity, even higher than the commercial formulation, Nevanac® 0.3%. The optimized formulations represent an opportunity for topical instillation of drugs to the posterior segment of the eye.