J Ocul Pharmacol Ther [JOURNAL]
Sun
200 papers
Ocular Pharmacokinetics and Biodistribution of Perfluorohexyloctane after Topical Administration to Rabbits.
Krösser S, Grillenberger R, Eickhoff K … +3 more , Korward J, Cavet ME, Mah FS
J Ocul Pharmacol Ther · 2025 Sep · PMID 40533097 · Publisher ↗
Perfluorohexyloctane ophthalmical solution (PFHO) forms an anti-evaporative layer at the air-tear interface and is indicated for treatment of the signs and symptoms of dry eye disease (DED). This study evaluated the ocul...
Perfluorohexyloctane ophthalmical solution (PFHO) forms an anti-evaporative layer at the air-tear interface and is indicated for treatment of the signs and symptoms of dry eye disease (DED). This study evaluated the ocular pharmacokinetics and biodistribution of PFHO in rabbits. Radiolabeled PFHO was administered to female Dutch Belted rabbits as single (35 µL to each eye) or multiple (twice daily for 5 days) topical ocular doses. Animals were euthanized at designated timepoints. Tears (antemortem), ocular tissues, and blood were collected for pharmacokinetic analysis; heads and carcasses were collected for autoradiographic analysis. Concentrations were measured using liquid scintillation counting. After multiple doses, maximum concentration (C) and area under the concentration-time curve were highest in tears (2330 µg/g, 3720 µg•h/g) and Meibomian glands (222 µg/g, 1440 µg•h/g), followed by other anterior tissues (cornea, 27.6 µg/g, 463 µg•h/g; palpebral conjunctiva, 14.0 µg/g, 136 µg•h/g). PFHO was measurable in tears for 8 h and in Meibomian glands for ≥24 h. Distribution to the posterior ocular segment was minimal, and plasma concentrations were low (single-dose C, 0.97 µg/g; multiple-dose C, 3.2 µg/g). In non-ocular tissues, PFHO was confined primarily to nasal tissues and gastrointestinal tract contents; exposure to other systemic tissues was negligible. Exposure of PFHO was highest in tears, consistent with its anti-evaporative mode of action, followed by the Meibomian glands. PFHO exposure was very low in posterior ocular tissues and negligible in systemic circulation, consistent with the clinical safety profile.
Clinical Trials of Aflibercept Biosimilars: A Review.
Lee H, Sharma A, Woo SJ
J Ocul Pharmacol Ther · 2025 Sep · PMID 40526023 · Publisher ↗
Anti-vascular endothelial growth factor (VEGF) biologics have revolutionized the management of VEGF-driven retinal diseases, significantly improving visual outcomes for patients. Following the patent expiration of ranibi...
Anti-vascular endothelial growth factor (VEGF) biologics have revolutionized the management of VEGF-driven retinal diseases, significantly improving visual outcomes for patients. Following the patent expiration of ranibizumab, multiple anti-VEGF biosimilars have been developed, with the first approved for ophthalmic use entering the market in 2022. More recently, the expiration of aflibercept market exclusivity in 2024 has led to the rapid development of aflibercept biosimilars-some already approved and others pending regulatory decisions. By offering clinically equivalent and cost-effective alternatives to reference biologics, biosimilars can lessen financial burdens and improve treatment adherence. Understanding the study designs of biosimilars can mitigate negative perceptions of biosimilars and promote their active implementation. In this review, we provide a comprehensive comparison of the designs of phase III clinical trials of aflibercept biosimilars, including recently published results.
Antineovascular Effects of Coenzyme Q10 and Vitamin E Combination in Corneal Neovascularization: A Pilot Study.
Özgür A, Özmen MC, Yalınbaş Yeter D … +1 more , İnan MA
J Ocul Pharmacol Ther · 2025 Sep · PMID 40495727 · Publisher ↗
To evaluate and compare the effects of subconjunctival injection of coenzyme Q10 (CoQ10) and vitamin E (Vit E) ophthalmic solution (Coqun®) with subconjunctival bevacizumab in a suture-induced corneal neovascularization...
To evaluate and compare the effects of subconjunctival injection of coenzyme Q10 (CoQ10) and vitamin E (Vit E) ophthalmic solution (Coqun®) with subconjunctival bevacizumab in a suture-induced corneal neovascularization (CoNV) rabbit model. CoNV was induced in the right eyes of 24 New Zealand rabbits using a 7.0 silk suture. One week after suturing, the rabbits were randomly divided into four groups and treated with a subconjunctival injection of either 0.1 mL balanced salt solution (control), bevacizumab (2.5 mg/0.1 mL), or two different doses of Coqun [(2 mg CoQ10 + 10 mg Vit E/0.2 mL) and (4 mg CoQ10 + 20 mg Vit E/0.4 mL)]. Photographs were taken on day 7 (pre-injection) and day 14 (7 days post-injection). On day 14, the regression area of CoNV was measured for analysis, and enucleation was performed for histopathological evaluation. The CoNV areas after treatment were smaller in all three treatment groups compared with the control group ( < 0.01). The mean percentage of CoNV regression was highest in the bevacizumab group (87.8% ± 3.2%), followed by the Coqun groups (69.5% ± 5.9% in the 0.2 mL dose, and 67.1% ± 9.3% in the 0.4 mL dose) No significant difference was observed between the two different doses of Coqun ( = 0.99). Subconjunctival administration of Coqun ophthalmic solution may offer a beneficial adjunct for the treatment of CoNV. Although it is not less effective than bevacizumab, its neuroprotective properties suggest potential value in cases where CoNV and glaucoma coexist. Further clinical studies are warranted to confirm these findings and to better define its therapeutic role.
Autologous Serum from Sjögren's Syndrome Patients Mitigates Ferroptosis in Hyperosmolarity-Induced Corneal Epitheliopathy.
Chu G, Wang J, Wang Z … +5 more , Cai X, Shi S, Qing Q, Zhong Y, Zhang Q
J Ocul Pharmacol Ther · 2025 Sep · PMID 40495717 · Publisher ↗
To investigate the role of autologous serum (AS) in alleviating hyperosmolarity-induced corneal epitheliopathy via the ferroptosis pathway. AS was extracted and prepared from patients with Sjögren's syndrome. An hypero...
To investigate the role of autologous serum (AS) in alleviating hyperosmolarity-induced corneal epitheliopathy via the ferroptosis pathway. AS was extracted and prepared from patients with Sjögren's syndrome. An hyperosmotic dry eye model was established by exposing HCE-T cells to 90 mM NaCl, followed by treatment with AS or ferroptosis inhibitors. Protein expression was analyzed using Western blotting. Intracellular Fe and reactive oxygen species (ROS) levels were determined by FerroOrange and 2',7'-Dichlorodihydrofluorescein diacetate (H2DCFDA) fluorescent probes, and cellular malondialdehyde and glutathione levels were measured using kits. Transmission electron microscopy was utilized to examine mitochondrial ultrastructure. Under hyperosmotic conditions, HCE-T cells exhibited increased lipid peroxidation and iron accumulation, accompanied by significant alterations in the expression of ferroptosis-related markers and characteristic changes in mitochondrial morphology, which indicated the induction of ferroptosis. Among the tested concentrations, 20% and 50% AS demonstrated notable therapeutic effects, significantly enhancing cell viability and migration, reducing ROS and Fe levels, and alleviating mitochondrial damage. Furthermore, AS effectively inhibited ferroptosis through the Xc/glutathione peroxidase 4 (GPX4) pathway. AS reduced lipid peroxidation levels in HCE-T cells under hyperosmolarity and inhibited ferroptosis through the Xc/GPX4 pathway.
Lower Levels of Endogenous Intraocular Interferon Beta in Patients with Primary Glaucoma.
Padmanabhan Nair A, Machiraju P, Tejwani S … +6 more , Dinakaran S, A V SD, Shetty N, Shetty R, Ghosh A, Sethu S
J Ocul Pharmacol Ther · 2025 Sep · PMID 40485295 · Publisher ↗
Glaucoma, a neurodegenerative condition of the optic nerve is driven by increased intraocular pressure (IOP) due to fibrotic changes of the trabecular meshwork (TM). Interferon beta (IFN-β), a pleiotropic cytokine is kno...
Glaucoma, a neurodegenerative condition of the optic nerve is driven by increased intraocular pressure (IOP) due to fibrotic changes of the trabecular meshwork (TM). Interferon beta (IFN-β), a pleiotropic cytokine is known for its neuroprotective and antifibrotic potential. Hence, we investigated the intraocular status of IFN-β in patients with primary glaucoma. Aqueous humor (AqH) from patients with primary glaucoma [107 eyes; primary open-angle glaucoma (POAG), 59 eyes; primary angle-closure glaucoma (PACG), 48 eyes] and controls (70 eyes) were collected during cataract surgery and/or trabeculectomy. TM from patients with POAG (20 eyes) and PACG (18 eyes) was collected during trabeculectomy. IFN-β in AqH was measured using bead-based Enzyme-Linked Immunosorbent Assay (ELISA), and messenger RNA (mRNA) expression of IFN-β in TM was measured by quantitative PCR. AqH-IFN-β levels were significantly ( < 0.05) lower in patients with glaucoma, particularly in patients with POAG compared with controls (area under the receiver operating characteristic curve = 0.723, < 0.001; odds ratio of 5.1, < 0.0001). AqH-IFN-β levels correlated positively with visual field index of both patients with POAG ( = 0.307; = 0.0321) and PACG ( = 0.518; P = 0.0007). Whereas, AqH-IFN-β levels correlated positively with retinal nerve fiber layer thickness in patients with POAG ( = 0.460; = 0.0042) only. TM-IFN-β mRNA expression was significantly lower in glaucoma patients with poor IOP control compared with those with good IOP control by IOP-lowering medications. Lower IFN-β in AqH and TM of patients with glaucoma and its association with clinical indices suggests its neuroprotective and antifibrotic role in glaucoma. The findings highlight the potential for IFN-β-based prognostication and therapy in the management of glaucoma.
Risk and Protective Factors for Ocular Surface Disease in Patients with Type 2 Diabetic Mellitus: A Retrospective Cohort Study.
Sun CC, Pan LY, Chen NN … +2 more , Kuo YK, Chen TH
J Ocul Pharmacol Ther · 2025 Aug · PMID 40485291 · Publisher ↗
Identify the risk and protective factors for ocular surface disease (OSD) in patients with type 2 diabetes mellitus (T2DM). This retrospective cohort study used the Chang Gung Research Database (2005-2020) for patients...
Identify the risk and protective factors for ocular surface disease (OSD) in patients with type 2 diabetes mellitus (T2DM). This retrospective cohort study used the Chang Gung Research Database (2005-2020) for patients with T2DM. A total of 161,001 patients were included, of which 915 had OSD and 160,086 did not. The OSD group was further divided into recurrent corneal erosion (RCE) ( = 92) and corneal ulcer ( = 371) groups after excluding those with overlapping diagnoses. The risk and protective factors were also analyzed. After age and gender matching, the OSD group had a considerably higher baseline and mean HbA1c and a higher incidence of dry eye disease (DED), diabetic neuropathy, retinopathy, and ocular procedures. After adjusting for gender, age, and diabetes mellitus (DM) duration, we found that DED, higher mean HbA1c, diabetic neuropathy, trans pars plana vitrectomy (TPPV) and cataract surgery were the contributing factors for OSD. Antihyperglycemic agents, especially sodium-glucose cotransporter-2 inhibitors and glucagon-like peptide-1 agonists, considerably protect against OSD. DED and TPPV were risk factors for corneal ulcers but not for RCE; however, DM medication had the same effect on corneal ulcers and RCE. Poor diabetic control, diabetic neuropathy, and ocular procedures are the risk factors for OSD. Antihyperglycemic agents, except metformin, can prevent OSD in patients with T2DM. Additionally, DED and TPPV are risk factors for corneal ulcers but not for RCE. A prospective randomized controlled trial is required to confirm our results.
Rose Bengal-Assisted Photodynamic Antimicrobial Therapy for Keratitis.
Roy A, Kompella UB
J Ocul Pharmacol Ther · 2025 Sep · PMID 40441703 · Full text
Rose bengal-assisted green light photodynamic antimicrobial therapy (RB-PDAT) is a new approach being evaluated for treating infectious keratitis. Preliminary clinical evidence suggests the broad-spectrum antimicrobial a...
Rose bengal-assisted green light photodynamic antimicrobial therapy (RB-PDAT) is a new approach being evaluated for treating infectious keratitis. Preliminary clinical evidence suggests the broad-spectrum antimicrobial activity of RB-PDAT. The therapy potentially exerts its activity by generating reactive oxygen species that inhibit microbial growth. Large clinical trials are underway to further establish a role for RB-PDAT in clinical medicine, especially recalcitrant fungal keratitis that is less responsive to conventional photodynamic therapy with riboflavin. A potential limitation of the therapy includes poor penetration of rose bengal dye into the cornea. This limitation is being addressed by several approaches, including lipophilic prodrugs, nanoparticles, and physical approaches for enhanced delivery, including iontophoresis and ultrasound.
Topical Cyclosporine and Steroid Treatments: A Comparative Approach to Membranous Punctal Stenosis.
Kholzoda S, Özkan G, Dericioğlu V … +1 more , Akkaya Turhan S
J Ocul Pharmacol Ther · 2025 Sep · PMID 40372950 · Publisher ↗
To compare the efficacy of topical cyclosporine A (CsA) and steroid treatment in the membranous punctal stenosis (PS). Forty-eight patients with membranous PS were divided into 2 groups: 23 eyes of 13 patients received...
To compare the efficacy of topical cyclosporine A (CsA) and steroid treatment in the membranous punctal stenosis (PS). Forty-eight patients with membranous PS were divided into 2 groups: 23 eyes of 13 patients received topical CsA for 6 months as Group CsA and 25 eyes of 14 patients received topical steroid for 3 months as Group S. Examinations were performed before and at 1, 3, 6, and 9 months after treatment. Clinical evaluations involved the Munk score and the fluorescein dye disappearance test (FDDT). Anterior segment optical coherence tomography was employed to measure tear meniscus height (TMH), tear meniscus area (TMA), and outer punctum diameter (OPD). TMH was also examined with biomicroscopy (TMH-Bio). A questionnaire was administered to assess patient satisfaction. Munk score and FDDT grade decreased in both groups at all follow-ups compared with the pre-treatment. TMH-Bio was lower in the Group CsA at all follow-up visits compared with baseline ( < 0.001). TMA and TMH decreased in the Group CsA compared with pre-treatment at 6 months after treatment, whereas there were no changes in the Group S. OPD was larger at 9 months in both groups compared with baseline. The patients' satisfaction was higher in Group CsA at the 6th month compared with Group S. CsA has demonstrated the potential to be a more effective treatment option for the management of PS, with additional advantages compared with topical steroid, such as higher patient satisfaction and favorable functional outcomes.
Steroid-Induced Ocular Hypertension in Children: A Review on Risk Factors.
Lacau S, Marin A, Bitrian E
J Ocul Pharmacol Ther · 2025 Aug · PMID 40359125 · Publisher ↗
Steroid-induced ocular hypertension is poorly understood in children, despite its frequent occurrence. Significant knowledge voids exist in steroid responsiveness, especially in the pediatric population. Therefore, highl...
Steroid-induced ocular hypertension is poorly understood in children, despite its frequent occurrence. Significant knowledge voids exist in steroid responsiveness, especially in the pediatric population. Therefore, highlighting the most critical risk factors in pediatric patients can help ophthalmologists identify who is at increased risk of developing a high steroid response. A manual search was conducted in PubMed and Google Scholar in search of relevant articles on the steroid-induced glaucoma subtopic. Key risk factors for high steroid response include glaucoma family history, previous glaucoma diagnosis, young age, steroid type, administration route, and diseases such as vernal keratoconjunctivitis (VKC) and uveitis. Clinically, it presents similarly to primary glaucoma, except for steroid usage history. Steroid cessation or reduction can normalize intraocular pressure (IOP) levels; however, in some cases, pressure-lowering drugs are necessary for treatment. Topical ocular steroids are frequently used by pediatricians and ophthalmologists alike. Understanding the importance of risk factors allows for a timely diagnosis of steroid response and adequate treatment before glaucomatous vision loss can occur.
Real-World Safety Profile of Cenegermin Per FDA Adverse Event Reporting System.
Choudhry HS, Pei M, Mothy D … +2 more , Scarfuto J, Mian SI
J Ocul Pharmacol Ther · 2025 Aug · PMID 40329904 · Publisher ↗
To characterize the safety profile of cenegermin through an analysis of postmarket adverse events (AEs). The U.S. Food and Drug Administration adverse event reporting system was queried for AEs associated with cenegermi...
To characterize the safety profile of cenegermin through an analysis of postmarket adverse events (AEs). The U.S. Food and Drug Administration adverse event reporting system was queried for AEs associated with cenegermin use between 2019 and 2023. Demographic information was collected. Reporting odds ratio (ROR) and proportional reporting ratio (PRR) were used to determine adverse reactions that were significantly more likely to be caused by cenegermin use compared with other ophthalmical topicals. Most AEs occurred in females (65.16%). The most common AEs were eye pain (46.94%), irritation (14.46%), and ocular hyperemia (9.8%). Of 34 eye disorders that were found to be associated with cenegermin use, the ones with the highest odds ratios were periorbital pain [ROR: 25.34, confidence interval (CI): 20.70-31.01, PRR: 16.45], eyelid pain (ROR: 22.96, CI: 19.39-27.19, PRR: 15.50), and eye pain (ROR: 20.02, CI: 18.77-21.35, PRR: 16.08). Patients taking cenegermin were significantly more likely to develop eye disorders (ROR: 2.21, CI: 2.12-2.31, PRR: 1.46), but were not more likely to develop disorders of other system organ classes. In terms of patient outcomes, patients taking cenegermin were at higher risk for hospitalization (ROR: 16.39, CI: 12.84-20.94, PRR: 12.17) and surgery (ROR: 9.57, CI: 6.14-14.93, PRR: 8.01). Postmarket surveillance of cenegermin demonstrates that eye pain and irritation are the most common AEs. Involvement of other organ systems is highly unlikely. Patients using topical cengermin should be counseled accordingly.
Corneal Complications: Drug-Induced Deposits and Food and Drug Administration Adverse Event Reporting System Data Insights-A Retrospective Study.
Aftab OM, Khan H, Aftab B … +2 more , Haque W, Daoud YJ
J Ocul Pharmacol Ther · 2025 Aug · PMID 40322910 · Publisher ↗
The aim of this study was to identify and quantify the occurrence of corneal deposits caused by medications, utilizing data from the Food and Drug Administration Adverse Event Reporting System (FAERS). We conducted a re...
The aim of this study was to identify and quantify the occurrence of corneal deposits caused by medications, utilizing data from the Food and Drug Administration Adverse Event Reporting System (FAERS). We conducted a retrospective analysis of the national FAERS database, focusing on instances of drug-induced corneal deposits reported between 2004 and the third quarter of 2023. Our methodology included applying the proportional reporting ratio, reporting odds ratio, empirical Bayes geometric mean, and information component in our disproportionality analysis. A signal was considered present if all four of these disproportionality metrics showed positive results. Over the span of 20 years, our research identified 383 adverse event reports linked to corneal deposits associated with 349 different medications. The most common age-group of these reports involved patients over 65 years of age (32.4%), with equal distribution between male (40.0%) and female (42.8%) patients. Thirty-one medications showed a positive signal. Notably, drugs such as amiodarone (68 reports), prednisolone (60 reports), and timolol (54 reports) were most frequently mentioned. Cyclopentolate and chloramphenicol demonstrated robust statistical relevance in association with corneal deposits. Positive signals for drug-induced corneal deposits included both well-known medications such as amiodarone and lesser-studied medications such as prednisolone and timolol. Clinician awareness of these findings alongside further investigation is needed.
Endoplasmic Reticulum Stress as a Regulator of High Glucose-Induced Epithelial-Mesenchymal Transition in Human Lens Epithelial Cells.
Li H, Yang J
J Ocul Pharmacol Ther · 2025 Aug · PMID 40322907 · Publisher ↗
Diabetic patients have been proven to have higher incidence of subcapsular cataract, and the subcapsular cataract formation has a closed link with epithelial-to-mesenchymal transition (EMT). EMT in numerous tissues can b...
Diabetic patients have been proven to have higher incidence of subcapsular cataract, and the subcapsular cataract formation has a closed link with epithelial-to-mesenchymal transition (EMT). EMT in numerous tissues can be regulated by the endoplasmic reticulum stress response (ER stress). In this study, we aim to explore the role of ER stress high glucose (HG)-induced EMT of human lens epithelial cells (HLECs). The human lens epithelial cell line SRA01/04 was treated under HG conditions, and 4-phenylbutyrate (PBA) or tauroursodeoxycholic acid (TUDCA) was used for 24 h to restore endoplasmic reticulum (ER) homeostasis under HG condition. The long axis and the aspect ratio of the cells were analyzed with ImageJ software to evaluate the morphology of the cells. Western blot analysis and immunofluorescence staining were applied to measure ER stress makers: glucose-regulated protein 78 (GRP78), phosphorylation of eukaryotic initiation factor-2α (P-eIf2α), activating transcription factor 6 (ATF6), phospho-inositol-requiring enzyme1 (P-IRE1α), and the EMT makers: fibronectin, vimentin, alpha-smooth muscle actin (α-SMA), and N-cadherin. Additionally, wound-healing assays were performed to evaluate the cell migration ability. Under HG, the morphology of HLECs became elongated, accompanied by a significantly increased cellular aspect ratio. Both the expression of ER stress markers (GRP78, P-eIF2α, ATF6, and P-IRE1α) and the EMT markers (fibronectin, vimentin, αSMA, and N-cadherin) increased. Conversely, the expression of E-cadherin, a marker of epithelial cells, decreased, and wound-healing assays indicated enhanced cell migration ability. All of these alterations were inhibited by PBA or TUDCA treatment. ER stress regulates HG-induced EMT in lens epithelial cells.
Comparative Efficacy of Current Topical Treatments for Dry Eye Disease: A Review of Pivotal Clinical Trials Evaluating Corneal Staining Outcomes.
Fahmy A, Ahmed M, Pflugfelder S … +2 more , Serikbaeva A, Tsao FW
J Ocul Pharmacol Ther · 2025 Aug · PMID 40293775 · Publisher ↗
Dry eye disease (DED) is a multifactorial disorder characterized by disruption of tear film homeostasis, resulting in ocular surface inflammation and damage. Although several Food and Drug Administration-approved topical...
Dry eye disease (DED) is a multifactorial disorder characterized by disruption of tear film homeostasis, resulting in ocular surface inflammation and damage. Although several Food and Drug Administration-approved topical treatments are available, direct comparisons of their efficacy and safety are complicated by variability in study designs and corneal staining grading scales. This review systematically evaluates and compares the efficacy and safety of topical therapies approved in the United States, focusing on anti-inflammatory and semi-fluorinated alkane (SFA)-based therapies. A systematic literature review identified 12 randomized controlled trials involving a total of 6,984 patients with varying severity of DED eligible for inclusion, with 8 providing data suitable for quantitative meta-analysis and 5 for exploratory regression analysis. Meta-analysis indicated that cyclosporine 0.1%/SFA showed the most significant early improvement (within ≤4 weeks) in total corneal fluorescein staining, outperforming other treatments. Exploratory regression analysis further supported these findings, demonstrating that cyclosporine 0.1%/SFA had the fastest and most consistent reduction in corneal staining, with the steepest improvement slope and strong predictability ( = 0.871). Safety analyses highlighted improved local tolerability for SFA-based therapies compared with traditional anti-inflammatory treatments, notably lower instillation site discomfort for both cyclosporine 0.1%/SFA (2.5%-9.9%) and perfluorohexyloctane (≤1%) vs. other cyclosporine formulations. SFA-based therapies, especially cyclosporine 0.1%/SFA, demostrated robust efficacy in improving signs of DED with superior tolerability profiles compared to traditional anti-inflammatory treatments. These findings support the role in effectively managing ocular surface inflammation and optimizing treatment strategies in DED.
Eyes on New Product Development.
Novack GD
J Ocul Pharmacol Ther · 2025 Jun · PMID 40293772 · Publisher ↗
Abstract loading — click title to view on PubMed.
Beneficial Effect of Rebamipide Eye Drops on Blue Light-Induced Oxidative Damage in the Ocular Surface.
Liu J, Jiang E, Kim H … +3 more , Moon J, Yoon HJ, Yoon KC
J Ocul Pharmacol Ther · 2025 Aug · PMID 40293740 · Publisher ↗
We evaluated the capacity of rebamipide (REB) to alleviate corneal epithelial damage induced via blue light (BL) exposure. Eight-week-old C57BL/6 mice were exposed to BL (410 nm, 100 J) twice daily for 10 days. The mice...
We evaluated the capacity of rebamipide (REB) to alleviate corneal epithelial damage induced via blue light (BL) exposure. Eight-week-old C57BL/6 mice were exposed to BL (410 nm, 100 J) twice daily for 10 days. The mice were randomly divided into 5 groups: 1 untreated and 4 groups receiving BL exposure ± different topical treatments: BL exposure alone, carboxymethylcellulose, 5% -acetylcysteine, and REB. Reactive oxygen species (ROS) levels were assessed, and -associated X protein ( was analyzed. Apoptotic cells were detected, inflammatory cytokine levels [tumor necrosis factor-alpha (TNF-α) and interleukin-6 (IL-6)] were measured using enzyme-linked immunosorbent assay (ELISA), and histopathological changes in the cornea were evaluated using hematoxylin and eosin (H&E) staining. The REB group demonstrated significantly lower BL exposure-induced ROS levels ( < 0.01) and expression ( < 0.01) than the BL group. The number of Terminal deoxynucleotidyl transferase dUTP nick end labeling (TUNEL) positive cells were lower in the REB group than in the BL group ( < 0.01). Furthermore, ELISA analysis revealed significantly reduced TNF-α and IL-6 levels in the REB group relative to BL group levels ( < 0.01). Hematoxylin and eosin staining showed preservation of corneal epithelial thickness. Rebamipide alleviated BL-induced oxidative damage to ocular surfaces by reducing ROS levels, inhibiting apoptosis, and suppressing inflammatory cytokine expression.
Myopia Progression Study Comparing Low-Dose (0.01%) Atropine Eye Drops with a Control Group.
Sanchez-Tocino H, Villanueva Gomez A, Saldaña Burgos R … +2 more , Hata Viveiros MM, Galindo-Ferreiro A
J Ocul Pharmacol Ther · 2025 Jun · PMID 40250999 · Publisher ↗
To evaluate myopia progression in children treated with 0.01% atropine eye drops compared with controls. Two longitudinal cohorts of myopic children (atropine and control) were observed in different time periods. All ch...
To evaluate myopia progression in children treated with 0.01% atropine eye drops compared with controls. Two longitudinal cohorts of myopic children (atropine and control) were observed in different time periods. All children had an increase in myopia of greater than -0.50 diopters (D) or axial length (AL) growth of >0.20 mm in the previous year. Patients were examined at baseline and every 6 months for 18 months. The primary outcomes were the annual progression rate of spherical equivalent refractive error (SER) and AL. Response to treatment was categorized as insufficient, moderate, or good. Progression according to age was also evaluated. Statistical significance was defined as < 0.05. The study included 243 myopic children [127 (44.7%) female; mean age, 10.19 ± 2.29 years]. The atropine group comprised 158 (65%) children. At 18 months, the mean (95% confidence interval) change in SER was -0.85 D (-1.00, -0.69) in the control group and -0.73 D (-0.85, -0.61) in atropine ( = 0.295). The mean increase in AL was 0.41 mm (0.32, 0.50) in the control group and 0.33 mm (0.28, 0.39) in the atropine ( = 0.160). Children aged <9 years had the lowest percentage of success [3/21 (27.8%)] in the atropine group and the highest percentage of failure (63.2%) ( = 0.03). Atropine drops at 0.01% did not slow myopia progression. Increasing the concentration or combining with optical treatments may be necessary, particularly for children aged <9 years, who showed the greatest progression but also had the highest potential for myopia control.
Tacrolimus 0.1% Ophthalmic Suspension: Corneal and Intraocular Penetration Study.
Quirke M, Lamoureux F, Arnoult C … +5 more , Gress G, Ganem A, Charpentier T, Muraine M, Gueudry J
J Ocul Pharmacol Ther · 2025 Jun · PMID 40248843 · Publisher ↗
Topical tacrolimus is currently used in ocular surface pathologies as a corticosteroid-sparing immunosuppressive agent. It could also help prevent endothelial corneal graft rejection and inflammatory diseases; however, i...
Topical tacrolimus is currently used in ocular surface pathologies as a corticosteroid-sparing immunosuppressive agent. It could also help prevent endothelial corneal graft rejection and inflammatory diseases; however, its hydrophobic nature and high molecular weight theoretically limit its intraocular penetration. The aim of this study is to investigate the corneal and intraocular penetration of a 0.1% tacrolimus ophthalmic suspension. Sixteen rabbits were randomly spread into four groups defined by the delay between the last tacrolimus instillation and corneal sampling (2, 6, 11, and 24 h). Three rabbits per group received bilateral instillations of tacrolimus twice daily for 5 days, the 4th subject in each group serving as negative controls. The 5th day, conjunctiva, corneal epithelium, anterior stroma, posterior stroma, corneal endothelium, iris, choroid/retina, aqueous humor, and plasma samples were collected. Tacrolimus concentrations were determined using high-performance liquid chromatography coupled with tandem mass spectrometry. Maximum mean concentration was reached after 2 h in the epithelium, anterior and posterior stroma, and endothelium: 12794 (±2656), 436 (±178), 341 (±179), and 4125 (±1673) ng/g, respectively. The descending rank order of exposure over 24 h was: corneal epithelium; corneal endothelium; conjunctiva; anterior stroma; posterior stroma; iris; and chorioretina with 158.0; 39.99; 4.620; 4.134; 3.350; 0.384; 0.270 ng.h/mg, respectively. Tacrolimus concentrations measured in the corneal tissues are significantly higher than that described as lower limit of efficacy in solid organ transplantation. Topical 0.1% tacrolimus could therefore become an alternative to corticosteroids for endothelial graft rejection prevention and endothelial inflammatory pathologies management.
Biodistribution of Reconstituted High-Density Lipoprotein Nanoparticles for Targeted Delivery to Retinal Ganglion Cells.
Petty RM, Rangan RS, Curry S … +5 more , Brooks CD, Sabnis N, Clark AF, Lacko AG, Krishnamoorthy RR
J Ocul Pharmacol Ther · 2025 Jun · PMID 40248840 · Full text
Nanoparticle-based drug delivery systems offer a promising approach for overcoming the challenges of ocular drug delivery. Our study evaluated the biodistribution and potential targeting of reconstituted high-density lip...
Nanoparticle-based drug delivery systems offer a promising approach for overcoming the challenges of ocular drug delivery. Our study evaluated the biodistribution and potential targeting of reconstituted high-density lipoprotein nanoparticles (rHDL NPs) loaded with near-infrared dye IR780 to retinal ganglion cells (RGCs) and optic nerve head astrocytes (ONHAs) as a model for neuroprotective drug delivery in glaucoma. A stable rHDL-payload complex was formulated using IR780, phosphatidylcholine, and apolipoprotein A-I (Apo A-I) by using a novel preparation method. Fluorescent rHDL (rHDL-IR780) was assessed for cellular uptake in primary human ONHAs , whereas scavenger receptor class B1 (SR-B1) expression was confirmed by Western blot. Receptor-mediated uptake was examined by SR-B1 receptor blocking. biodistribution was evaluated by intravitreal injection of rHDL into postmortem human donor eyes. Spectroscopic analysis confirmed IR780 encapsulation in rHDL NPs. Blocking SR-B1 receptors significantly reduced IR780 uptake by ONHAs, supporting an SR-B1-mediated delivery mechanism, in addition to confirming SR-B1 expression in human retinal lysates. In experiments, 4 h postinjection, IR780 localized in the retinal nerve fiber and ganglion cell layers. By 24 h, IR780 penetrated deeper retinal layers, achieving RGC uptake. Our findings demonstrate that rHDL NPs facilitate targeted delivery to retinal tissues through an Apo A-I/SR-B1 pathway, overcoming ocular barriers to reach RGCs. This study supports the potential of rHDL NPs as a platform for neuroprotective drug delivery to treat glaucoma, enhancing both pharmacokinetics and targeted cellular uptake.
Topical Losartan in the Management of Corneal Scarring Fibrosis: Update on Dosage, Efficacy, and Potential Epithelial Toxicity.
Dutra BAL, Wilson SE
J Ocul Pharmacol Ther · 2025 Jun · PMID 40238717 · Publisher ↗
Losartan is an angiotensin II receptor blocker (ARB) that also inhibits transforming growth factor (TGF)-beta signaling by blocking the activation of extracellular signal-regulated kinase (ERK) in the noncanonical TGF-be...
Losartan is an angiotensin II receptor blocker (ARB) that also inhibits transforming growth factor (TGF)-beta signaling by blocking the activation of extracellular signal-regulated kinase (ERK) in the noncanonical TGF-beta signaling pathway. Rabbit studies demonstrated the efficacy of topical losartan in reducing fibrotic scarring following a variety of corneal injuries, such as descemetorhexis, alkali burns, and photorefractive keratectomy (PRK). Several human case reports have subsequently shown the efficacy of topical losartan in treating scarring fibrosis resulting from surgical complications and infections. Since rabbit studies have also found concentration-dependent corneal epithelial toxicity associated with topical losartan, a lower concentration of 0.2 mg/mL administered 6 times daily is recommended in corneas with epithelial defects until epithelial closure is achieved before using standard 0.8 mg/mL losartan 6 times a day for the duration of treatment. For eyes with intact epithelium, a dose of 0.8 mg/mL 6 times daily is recommended throughout the treatment period. Doses of topical losartan above 0.8 mg/mL should be avoided due to dosage-related increases in persistent epithelial defects. Clinical studies are needed to further assess questions such as which corneal fibrotic disorders are most likely to respond to topical losartan treatment and whether a lower frequency of application leads to greater treatment failure.
Durability of Treatment with a Thermomechanical Device in Meibomian Gland Dysfunction: An Observational Extension Study.
Sadri E, Verachtert A, Parkhurst GD … +4 more , Echegoyen J, Klein I, Agmon Gerstein Y, Berdy GJ
J Ocul Pharmacol Ther · 2025 Jun · PMID 40238710 · Publisher ↗
To evaluate the durability of thermomechanical device treatment effect in patients with meibomian gland dysfunction (MGD) at 6 months post-treatment. This was an extension of an initial 3-month, prospective, controlled,...
To evaluate the durability of thermomechanical device treatment effect in patients with meibomian gland dysfunction (MGD) at 6 months post-treatment. This was an extension of an initial 3-month, prospective, controlled, randomized, masked, multicenter pivotal study, in which subjects with MGD were randomized to thermomechanical device treatment (3 sessions, 2 weeks apart) or a single control treatment. The extension study was a single-arm, observational study in the same 5 sites of the pivotal study. A subset of subjects from the thermomechanical device group with an increase in tear break-up time (TBUT) of 2.5 s or greater in at least 1 eye at 1- or 3-month follow-up and able to attend the 6-month follow-up were included. Effectiveness endpoints included changes in TBUT, Meibomian gland score (MGS), and Ocular Surface Disease Index (OSDI) from baseline to 6 months. Device-related adverse events (AEs) were also assessed. At 6 months post-treatment, 21 subjects (42 eyes) demonstrated significant improvements from baseline in mean TBUT (5.2 ± 3.8 s; < 0.001), mean MGS (18.2 ± 10.9; < 0.0001), and mean OSDI (-24.3 ± 26.5; = 0.0004). Improvements in corneal staining scores were also observed. No ocular AEs were reported. The findings of the extension study demonstrate that the clinical benefit of the thermomechanical device, evaluated by TBUT, MGS, and OSDI, can be maintained out to 6 months and that the device is safe and effective in improving the signs and symptoms of evaporative dry eye disease in MGD.
About
- Frequency
- Sun
- Papers found
- 200
- RSS feed
- Subscribe