Journal of ocular pharmacology and therapeutics : the official journal of the Association for Ocular Pharmacology and Therapeutics最新文献

{"title":"Evolution of vitreomacular traction following the use of the dexamethasone intravitreal implant (Ozurdex) in the treatment of macular edema secondary to central retinal vein occlusion.","authors":"Sophie J Bakri,&nbsp;Ahmed F Omar","doi":"10.1089/jop.2011.0184","DOIUrl":"https://doi.org/10.1089/jop.2011.0184","url":null,"abstract":"<p><strong>Purpose: </strong>To report a case of worsening of vitreomacular traction (VMT) after the dexamethasone intravitreal implant (Ozurdex; Allergan, Inc., Irvine, CA) for the treatment of macular edema secondary to central retinal vein occlusion (CRVO).</p><p><strong>Case: </strong>A 71-year-old man who presented with macular edema secondary to CRVO was treated by intravitreal injections of bevacizumab followed by Ozurdex.</p><p><strong>Results: </strong>VMT developed during the course of treatment and became more evident when macular edema resolved after treatment with Ozurdex.</p><p><strong>Conclusion: </strong>VMT may become apparent and worsen after resolution of macular edema treated with intravitreal Ozurdex.</p>","PeriodicalId":520681,"journal":{"name":"Journal of ocular pharmacology and therapeutics : the official journal of the Association for Ocular Pharmacology and Therapeutics","volume":" ","pages":"547-9"},"PeriodicalIF":2.3,"publicationDate":"2012-10-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://sci-hub-pdf.com/10.1089/jop.2011.0184","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"40185572","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Preparation, characterization, and in vivo evaluation of triamcinolone acetonide microspheres after intravitreal administration.","authors":"Siamak Zarei-Ghanavati,&nbsp;Bizhan Malaekeh-Nikouei,&nbsp;Reza Pourmazar,&nbsp;Sajad Seyedi","doi":"10.1089/jop.2011.0215","DOIUrl":"https://doi.org/10.1089/jop.2011.0215","url":null,"abstract":"<p><strong>Purpose: </strong>The aim of this study was to evaluate the intraocular pressure (IOP) increasing effect and bioavailability of triamcinolone acetonide (TA) microspheres, as a novel drug delivery system, after intravitreal administration.</p><p><strong>Methods: </strong>Microspheres loaded by TA were prepared by the solvent evaporation method. After encapsulation, the final microspherical formulation was tested in an animal model. The left eyes of rabbits received microspherical TA and the right eyes were injected with conventional TA suspension. The drug concentration in the vitreous samples at days 7, 14, 28, and 56 after the injection was determined by high-performance liquid chromatography. The IOP was also checked at the same days with the Schiotz tonometer.</p><p><strong>Results: </strong>There was no statistically significant (P>0.05) difference between mean concentration of TA in the vitreous of right and left eyes at the different sampling times except day 56. Mean IOP of eyes that received microspherical TA was increased less than that of the eyes injected with TA suspension, and the difference was statistically significant (P<0.05) for each measurement day. TA was detectable in both eyes after 8 weeks. Both TA microsphere and suspension showed the sustained release profile.</p><p><strong>Conclusion: </strong>The results of this study showed less IOP increasing effect of triamcinolone microspheres in comparison with suspension form.</p>","PeriodicalId":520681,"journal":{"name":"Journal of ocular pharmacology and therapeutics : the official journal of the Association for Ocular Pharmacology and Therapeutics","volume":" ","pages":"502-6"},"PeriodicalIF":2.3,"publicationDate":"2012-10-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://sci-hub-pdf.com/10.1089/jop.2011.0215","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"40186434","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Posology, efficacy, and safety of epidermal growth factor eye drops in 305 patients: logistic regression and group-wise odds of published data.","authors":"José Manuel Lou-Bonafonte,&nbsp;Elena Bonafonte-Marquez,&nbsp;Sergio Bonafonte-Royo,&nbsp;Pedro A Martínez-Carpio","doi":"10.1089/jop.2011.0236","DOIUrl":"https://doi.org/10.1089/jop.2011.0236","url":null,"abstract":"<p><p>The aim of this article is to investigate clinical research on indications, posology, efficacy, and safety of epidermal growth factor (EGF) eye drops in the treatment of some human corneal disorders. Methods used include systematic search and selection of series of cases and clinical trials in Medline database up to January 2012, kappa index (K) to validate retrieval information, cumulative Mantel-Haenszel-stratified meta-analysis, 2×2 contingency table of randomized EGF-vehicle-controlled treated groups, and statistical program SPSSv12. Our results indicate that EGF eye drops appear to be a very effective treatment of acute heterogeneous corneal diseases, without significant adverse effects, with a 86.8% clinical efficacy reported by authors, a 98% (P<0.05) probabilistic expected efficacy, and 51.3 (17.4-148.7 confidence interval 95%; P<0.05) odds ratio EGF/vehicle. However, clinical trials are scarce, with low sample sizes and serious inconsistencies in EGF posology. EGF eye drops (50-1,000 ng, 2-3 times/day) could be a useful treatment for promoting postoperative refractive surgery, reversing cases of keratopathy secondary to systematic EGF receptor inhibitors, diabetic keratopathy, and other corneal and conjunctival disorders.</p>","PeriodicalId":520681,"journal":{"name":"Journal of ocular pharmacology and therapeutics : the official journal of the Association for Ocular Pharmacology and Therapeutics","volume":" ","pages":"467-72"},"PeriodicalIF":2.3,"publicationDate":"2012-10-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://sci-hub-pdf.com/10.1089/jop.2011.0236","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"40186435","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Subcutaneous nadroparin calcium in the treatment of recent onset retinal vein occlusion: a pilot study.","authors":"Antonio Pinna,&nbsp;Piera Simula,&nbsp;Angelo Zinellu","doi":"10.1089/jop.2012.0012","DOIUrl":"https://doi.org/10.1089/jop.2012.0012","url":null,"abstract":"<p><strong>Purpose: </strong>Optimal management of retinal vein occlusion (RVO) is still a matter of debate. The purpose of this pilot study was to investigate whether nadroparin calcium may play some role in the treatment of recent onset (≤3 weeks' duration) RVO.</p><p><strong>Methods: </strong>Twenty-four RVO patients were treated with subcutaneous nadroparin calcium (200 I.U./kg/day) for 6 weeks. Best corrected visual acuity (BCVA) and macular thickness in the affected eye were measured at baseline, and after 3 and 6 months. Twenty-four RVO patients treated with oral pentoxifylline, matched for age, gender, RVO type, eye involvement, and BCVA at presentation, randomly selected from the RVO register, were used as controls.</p><p><strong>Results: </strong>Median BCVAs at baseline, month 3, and month 6 were 20/70 (range: 20/1,000-20/20), 20/40 (range: 20/100-20/20), and 20/30 (range: 20/200-20/20) in cases and 20/70 (range: 20/1,000-20/20), 20/60 (range: 20/320-20/25), and 20/60 (range: 20/500-20/20) in controls. Differences between groups were statistically significant at months 3 (P=0.025) and 6 (P=0.024). In the study group, the mean macular thickness was 510±207 μm at baseline, 384±198 μm after 3 months, and 313±170 μm after 6 months. Differences between baseline and months 3 and 6 were statistically significant (P=0.004 and P<0.001).</p><p><strong>Conclusions: </strong>Results suggest that nadroparin calcium might become a potential candidate for the treatment of RVO. Larger trials are necessary to confirm these preliminary findings.</p>","PeriodicalId":520681,"journal":{"name":"Journal of ocular pharmacology and therapeutics : the official journal of the Association for Ocular Pharmacology and Therapeutics","volume":" ","pages":"448-54"},"PeriodicalIF":2.3,"publicationDate":"2012-10-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://sci-hub-pdf.com/10.1089/jop.2012.0012","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"40170496","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"A comparison of azithromycin and tobramycin eye drops on epithelial wound healing and tolerance after penetrating keratoplasty.","authors":"Julie Blavin,&nbsp;Arnaud Sauer,&nbsp;Maher Saleh,&nbsp;David Gaucher,&nbsp;Claude Speeg-Schatz,&nbsp;Tristan Bourcier","doi":"10.1089/jop.2011.0171","DOIUrl":"https://doi.org/10.1089/jop.2011.0171","url":null,"abstract":"<p><strong>Purpose: </strong>After keratoplasty, antibiotic eye drops are used to prevent ocular infection until the recipient corneal epithelium has healed. We compared the effects of azithromycin, a new macrolide, with the effect of the standard antibiotics, tobramycin, on the (i) prevention of infection, (ii) epithelial healing, and (iii) ocular tolerance after penetrating keratoplasty.</p><p><strong>Methods: </strong>In this prospective, single-center, randomized study, patients undergoing penetrating keratoplasty received postoperative topical dexamethasone and either azithromycin (n=23; Azyter(®); one drop twice daily for 3 days) or tobramycin (n=23; Tobrex(®); 1 drop 4 times daily until complete re-epithelialization). Daily slit-lamp examination with fluorescein was performed, and photographs were taken to digitally assess the re-epithelialized surface area. Daily questionnaires assessed ocular comfort and pain.</p><p><strong>Results: </strong>There were no cases of infection in either group. The re-epithelialized area of the corneal graft increased at a similar rate in each group, with no difference between the groups on any day. The mean±SD days until complete re-epithelialization did not differ between tobramycin (4.14±1.17) and azithromycin (4.13±1.82) (P=0.89). Superficial punctate keratitis scores were similar for tobramycin (1.39) and azithromycin (1.34). Pain and discomfort scores improved each day after surgery with no differences between the groups on any day.</p><p><strong>Conclusion: </strong>Postkeratoplasty epithelial healing and ocular tolerance were not significantly different between the azithromycin- and tobramycin-treatment groups. Our results support the use of azithromycin as an alternative to tobramycin after corneal surgery such as keratoplasty.</p>","PeriodicalId":520681,"journal":{"name":"Journal of ocular pharmacology and therapeutics : the official journal of the Association for Ocular Pharmacology and Therapeutics","volume":" ","pages":"428-32"},"PeriodicalIF":2.3,"publicationDate":"2012-08-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://sci-hub-pdf.com/10.1089/jop.2011.0171","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"40167170","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"The 12-month outcome of three consecutive monthly intravitreal injections of ranibizumab for myopic choroidal neovascularization.","authors":"Tsung-Tien Wu,&nbsp;Ya-Hsin Kung","doi":"10.1089/jop.2011.0106","DOIUrl":"https://doi.org/10.1089/jop.2011.0106","url":null,"abstract":"<p><strong>Purpose: </strong>The aim of this study was to evaluate the 12-month outcomes, efficacy, and safety of three consecutive monthly intravitreal ranibizumab injections for myopic choroidal neovascularization (CNV).</p><p><strong>Methods: </strong>We retrospectively reviewed the medical records of 25 consecutive eyes that received a loading dose of three consecutive monthly intravitreal injections of ranibizumab for myopic CNV between February, 2008, and March, 2010, with a follow-up of 12 months. Eyes with persistent or recurrent CNV after 3 months received additional ranibizumab injections as needed. Patients' demographic data, best corrected visual acuity (BCVA), CNV findings on fluorescent angiography (FAG), central macular thickness (CMT) on optical coherence tomography (OCT), total number of treatments, and complications were recorded.</p><p><strong>Results: </strong>Mean baseline BCVA was 0.73 logarithm of the minimum angle of resolution (logMAR) (standard deviation [SD] 0.63), and improved significantly to 0.42 logMAR (SD 0.43) at 1 month, 0.38 logMAR (SD 0.47) at 2 months, 0.34 logMAR (SD 0.43) at 3 months, and 0.34 logMAR (SD 0.40) at 12 months (all P<0.001, Wilcoxon signed-rank test). The average number of injections was 3.44 (SD 0.92). At 12 months, mean improvement was 2.88 lines (SD 2.35), and 20 eyes (80%) showed a gain of at least one line after treatment. At 3 months, OCT showed significant reduction in CMT (P=0.012, two-tailed t-test), and FAG showed significant reduction of mean CNV size from 0.3 (SD 0.16) to 0.19 (SD 0.12) disc area (P=0.007, two-tailed t-test). No angiographic leakage was evident at 3 months in 21 eyes (84%); four eyes (16%) required additional injections for persistent leakage. Two eyes (8%) had recurrent CNV during follow-up and required retreatment. No complications were noted after treatment.</p><p><strong>Conclusions: </strong>An initial loading dose of three ranibizumab injections is safe and effective in treating myopic CNV, with visual improvement maintained over 12 months.</p>","PeriodicalId":520681,"journal":{"name":"Journal of ocular pharmacology and therapeutics : the official journal of the Association for Ocular Pharmacology and Therapeutics","volume":" ","pages":"129-33"},"PeriodicalIF":2.3,"publicationDate":"2012-04-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://sci-hub-pdf.com/10.1089/jop.2011.0106","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"40139439","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Improvement of acetazolamide ocular permeation using ascorbyl laurate nanostructures as drug delivery system.","authors":"Luis I Tártara,&nbsp;Daniela A Quinteros,&nbsp;Verónica Saino,&nbsp;Daniel A Allemandi,&nbsp;Santiago D Palma","doi":"10.1089/jop.2011.0104","DOIUrl":"https://doi.org/10.1089/jop.2011.0104","url":null,"abstract":"<p><strong>Purpose: </strong>To evaluate the performance of 6-O-Lauryl-l-ascorbic acid nanostructures (coagels) as vehicles for acetazolamide (AZM) in ophthalmic administration by in vitro and in vivo experimental tests.</p><p><strong>Methods: </strong>The systems of coagel + AZM were evaluated in terms of their in vitro release (dialysis membrane), permeability (isolated cornea), pharmacological effectiveness [intraocular pressure (IOP)-reduction in normotensive rabbits], and potential irritant effects.</p><p><strong>Results: </strong>The results concerning AZM permeation were better when vehiculized in coagels compared with ringer solution, which was evident from the AZM steady-state flux and P(app) values (J=1.43 μg/min and P(app)=3.04 cm.s(1)). As a consequence of this increase in permeation, the coagel-AZMs were more effective in lowering the IOP, according to the results obtained from the in vivo assays. Coagels loaded with 0.4% (W/W) of AZM showed a higher hypotensive effect in rabbits compared with the commercial formulation AZOPT(®) (brinzolamide 1%), mainly due to the prolonged effect of the former. In all cases, the intensity of irritation was time dependent. The sodium lauryl sulphate solution (2%) used as a positive control produced serious injury 30 min postadministration. This effect caused irritation, which decreased slowly and even at 180 min, the discomfort was still considerable. However, in the case of coagels, a mild-to-moderate effect was observed.</p><p><strong>Conclusions: </strong>The incorporation of AZM in coagels seems to improve the ocular bioavailability of this drug. Coagel-AZM 0.4% showed a higher hypotensive effect, with a mild-to-moderate irritant effect. These systems could be administrated in human beings, although more detailed studies still need to be carried out.</p>","PeriodicalId":520681,"journal":{"name":"Journal of ocular pharmacology and therapeutics : the official journal of the Association for Ocular Pharmacology and Therapeutics","volume":" ","pages":"102-9"},"PeriodicalIF":2.3,"publicationDate":"2012-04-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://sci-hub-pdf.com/10.1089/jop.2011.0104","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"40133912","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"The effects and underlying mechanisms of S-allyl l-cysteine treatment of the retina after ischemia/reperfusion.","authors":"Yan-Qing Chen,&nbsp;Wynn H T Pan,&nbsp;Jorn-Hon Liu,&nbsp;Mi-Mi Chen,&nbsp;Chi-Ming Liu,&nbsp;Ming-Yang Yeh,&nbsp;Shen-Kou Tsai,&nbsp;Mason Shing Young,&nbsp;Xiu-Mei Zhang,&nbsp;Hsiao-Ming Chao","doi":"10.1089/jop.2011.0099","DOIUrl":"https://doi.org/10.1089/jop.2011.0099","url":null,"abstract":"<p><strong>Purpose: </strong>Retinal ischemia-associated ocular disorders are vision-threatening. The aim of the present study was to examine whether S-allyl l-cysteine (SAC) is able to protect against retina ischemia/reperfusion injury.</p><p><strong>Methods: </strong>In vivo, retinal ischemia in the rat was induced by raising intraocular pressure (IOP) to 120 mmHg for 60 min. In vitro, an ischemic-like insult, namely oxidative stress, was established by incubating retinal ganglion cell-5 (RGC-5) with 500 μM H(2)O(2) for 24 h. The mechanisms involved in these processes were evaluated by electrophysiology, immunohistochemistry, and molecular biological approaches.</p><p><strong>Results: </strong>The retinal changes caused by the high IOP were characterized by a decrease in electroretinogram b-wave amplitudes, a loss of choline acetyltransferase immunolabeling amacrine cell bodies/neuronal processes, and an upregulation of the mRNA levels of hypoxia-inducible factor-1α (HIF-1α), vascular endothelium growth factor (VEGF), and matrix metalloproteinase-9 (MMP-9). The increased protein levels of HIF-1α, VEGF, and MMP-9 were also seen in RGC-5 cells subjected to defined oxidative stress. Of clinical importance, the ischemic/ischemic-like detrimental effects were concentration-dependently (least effect at 25 μM) and/or significantly (50 and/or 100 μM) blunted when SAC was applied 15 min before retinal ischemia or ischemic-like insult, respectively.</p><p><strong>Conclusion: </strong>SAC would seem to protect against retinal ischemia by acting as an antioxidant and inhibiting the upregulation of HIF-1α, VEGF, and MMP-9.</p>","PeriodicalId":520681,"journal":{"name":"Journal of ocular pharmacology and therapeutics : the official journal of the Association for Ocular Pharmacology and Therapeutics","volume":" ","pages":"110-7"},"PeriodicalIF":2.3,"publicationDate":"2012-04-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://sci-hub-pdf.com/10.1089/jop.2011.0099","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"40128939","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Functional and anatomic response of the retina and the choroid to intravitreal bevacizumab for macular edema.","authors":"Raimondo Forte,&nbsp;Gilda Cennamo,&nbsp;Maria Angelica Breve,&nbsp;Elisabetta Chiariello Vecchio,&nbsp;Giuseppe de Crecchio","doi":"10.1089/jop.2010.0181","DOIUrl":"https://doi.org/10.1089/jop.2010.0181","url":null,"abstract":"<p><strong>Purpose: </strong>This study evaluated the rate of change of best corrected visual acuity (BCVA), central retinal sensitivity, and retinal and choroidal thickness in patients with macular edema after intravitreal bevacizumab.</p><p><strong>Methods: </strong>This was a prospective, nonrandomized, interventional study. Thirty-four consecutive eyes (34 patients) with macular edema were included in the study. Choroidal neovascularization was present in 21 cases, stage 1 retinal angiomatous proliferation in 6 cases, branch retinal vein occlusion in 4 cases, and diabetic edema in 3 cases. Evaluation of BCVA (Early Treatment Diabetic Retinopathy Study [ETDRS] logarithm of the minimum angle of resolution [LogMAR]), central retinochoroidal thickness (RCT) at standardized A-scan, combined optical coherence tomography/microperimetric assessment of central retinal thickness (RT), central scotoma, and fixation behavior was performed during 12 months after treatment. Choroidal thickness was considered as the difference between RCT and RT. All patients received two initial intravitreal bevacizumab injections (1.25 mg/0.05 mL) at a 1-month interval.</p><p><strong>Results: </strong>BCVA and RT during follow-up were significantly better than at baseline. BCVA was improved of 0.32±0.3 LogMAR (P<0.001) at month 1, 0.18±0.4 LogMAR (P=0.05) at month 6, and 0.14±0.2 (P=0.09) at month 12. RT was reduced by 172.9±192.8 μm (P<0.001) at month 1, 157.7±134.2 μm (P=0.003) at month 6, and 164.3±122.3 (P=0.002) at month 12. Mean retinal sensitivity significantly increased during the first month; it decreased afterward, but an improvement if compared with baseline was present at each visit during follow-up. In 23.5% of cases, a choroidal thinning was present during follow-up, and in this group visual acuity at baseline and final visual improvement were significantly greater if compared with patients showing a choroidal thickening.</p><p><strong>Conclusion: </strong>Intravitreal bevacizumab for macular edema determines significant functional and anatomic improvement at the 12-month follow-up. Visual acuity at baseline and following treatment could be influenced by the choroidal involvement.</p>","PeriodicalId":520681,"journal":{"name":"Journal of ocular pharmacology and therapeutics : the official journal of the Association for Ocular Pharmacology and Therapeutics","volume":" ","pages":"69-75"},"PeriodicalIF":2.3,"publicationDate":"2012-02-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://sci-hub-pdf.com/10.1089/jop.2010.0181","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"40135118","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Ocular pharmacokinetics profile of different indomethacin topical formulations.","authors":"Claudio Bucolo,&nbsp;Barbara Melilli,&nbsp;Cateno Piazza,&nbsp;Monia Zurria,&nbsp;Filippo Drago","doi":"10.1089/jop.2011.0120","DOIUrl":"https://doi.org/10.1089/jop.2011.0120","url":null,"abstract":"<p><strong>Purpose: </strong>This study evaluated the ocular pharmacokinetics of indomethacin following topical administration of two different formulations present in the market.</p><p><strong>Methods: </strong>Rabbits received a multiple topical instillation (30 μL) of indomethacin ophthalmic suspension containing hydroxypropylmethylcellulose (IND-HPMC; Indom™ Alfa-Intes) or indomethacin ophthalmic solution with hydroxypropyl-β-cyclodextrin (IND-CD; Indocollirio™ Bausch & Lomb). Aqueous humor, vitreous humor, and retina were collected from animals at fixed time intervals after dosing. Indomethacin ocular levels were measured by liquid chromatography mass spectrometry (LC-MS/MS), and the pharmacokinetic parameters--peak drug concentration (C(max)), time to peak value (T(max)), and area under the concentration-time curve between 0 and 240 min (AUC(0-240))--were determined. All of the animals were treated according to the Association for Research in Vision and Ophthalmology (ARVO) Statement for the Use of Animals in Ophthalmic and Vision Research.</p><p><strong>Results: </strong>Peak concentrations of indomethacin in aqueous and vitreous were achieved within 30 min and 60 min after a single instillation of IND-HPMC and IND-CD, respectively. Retinal T(max) was 30 min and 120 min in the IND-HPMC-treated group and the IND-CD-treated group, respectively. Higher levels of indomethacin were found in retina after IND-HPMC administration compared to IND-CD (AUC(0-240) 272.9 ng/g per min vs. AUC(0-240) 73.5 ng/g/min, respectively; P<0.01). Also in the aqueous and vitreous, the drug levels were statistically higher (P<0.01) in the IND-HPMC group in comparison with the IND-CD group (AUC(0-240) 2039 ng/mL per min vs. AUC(0-240) 427.3 ng/mL per min, AUC(0-240) 53.8 ng/mL per min vs. AUC(0-240) 12.5 ng/mL per min, respectively). The highest drug levels in the ocular tissues were found following IND-HPMC administration compared with IND-CD (retina: C(max) 73.7±6.4 ng/g vs. 25.5±1.73 ng/g; aqueous: C(max) 952±6.8 ng/mL vs. 163±4.1 ng/mL; vitreous C(max) 31±3.5 ng/mL vs. 6.37±3.6 ng/mL).</p><p><strong>Conclusions: </strong>IND-HPMC treatment demonstrates a nonclinical ocular pharmacokinetic profile of indomethacin characterized by higher concentrations of drug in ocular tissues (4.7-, 4.3- and 3.7-fold higher in aqueous, vitreous, and retina, respectively) compared to the ND-CD-treated group. Taken together, these data seem to indicate that IND-HPMC formulation has good ocular distribution reaching relevant indomethacin levels in the back of the eye, and suggest that this formulation may be very useful for clinicians to manage retinal conditions.</p>","PeriodicalId":520681,"journal":{"name":"Journal of ocular pharmacology and therapeutics : the official journal of the Association for Ocular Pharmacology and Therapeutics","volume":" ","pages":"571-6"},"PeriodicalIF":2.3,"publicationDate":"2011-12-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://sci-hub-pdf.com/10.1089/jop.2011.0120","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"40133896","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}