Open-Angle Glaucoma (OAG) is a progressive optic neuropathy and a major cause of irreversible blindness worldwide. Lowering Intraocular Pressure (IOP) remains the most effective approach for slowing disease progression. Latanoprostene bunod (LBN) ophthalmic solution 0.024% (Vyzulta®) is a nitric oxide (NO)-donating prostaglandin analogue developed to enhance aqueous humor drainage through two complementary pathways. Following topical administration, LBN is converted into latanoprost acid and a nitric oxide-releasing metabolite. Latanoprost acid increases uveoscleral outflow, whereas nitric oxide improves conventional outflow by relaxing the trabecular meshwork and Schlemm's canal. Clinical studies have shown that LBN provides significant reductions in IOP in patients with OAG and ocular hypertension. In the phase III APOLLO and LUNAR trials, LBN demonstrated efficacy comparable to, and in some analyses greater than, timolol 0.5%. Long-term data from the JUPITER study further confirmed sustained IOP reduction during 12 months of treatment. LBN is generally well tolerated, with conjunctival hyperemia, mild ocular irritation, and instillation-site discomfort being the most frequently reported adverse events. Beyond its clinical utility, several synthetic approaches have been reported for the preparation of LBN. These include esterification and alkylation strategies involving nitrooxyalkyl derivatives, as well as routes based on bromobutyl intermediates followed by nitrate substitution. Patent literature has further described process improvements aimed at enhancing purity, scalability, and manufacturing efficiency. Overall, current evidence supports LBN as an effective and well-tolerated therapeutic option for patients with OAG or ocular hypertension. Continued improvements in synthetic methodologies may facilitate cost-effective production and broader clinical accessibility.

Exit-site granuloma is a frequent and challenging complication in patients undergoing peritoneal dialysis, predisposing to exit-site infections. Recent evidence suggests a potential role for topical timolol in promoting regression of granulomatous tissue. We report two patients on continuous ambulatory peritoneal dialysis who developed exit-site granulomas. Both patients were treated with topical 0.5% timolol maleate ophthalmic solution applied locally to the exit site three times weekly as part of routine exit-site care. Clinical response was monitored using serial photographs. Complete resolution of the granuloma was achieved within 3 weeks in one patient and within 2 months in the other. Neither patient developed local or systemic adverse effects, and no exit-site infections occurred during treatment. Topical 0.5% timolol maleate may represent a safe, non-invasive, and effective treatment option for peritoneal dialysis exit-site granulomas. Larger studies are warranted to establish its efficacy in larger cohorts.

This study presents the development and validation of three selective chromatographic methods for the identification and quantification of related substances, including process-related impurities and degradation products, in combined ophthalmic formulations of dorzolamide hydrochloride (DH) and timolol maleate (TM). The methods were applied to ophthalmic solutions containing 2.0% DH and 0.5% TM (20 and 5 mg/mL, respectively) and were designed to comply with the requirements of the USP, B.P., and Ph. Eur. Both an in-house developed generic formulation and the reference listed drug formulations, COSOPT PF and COSOPT, were evaluated during method development and validation. The novelty of this work lies in the use of three complementary chromatographic approaches that significantly improve specificity, selectivity, and impurity profiling in complex ophthalmic matrices during the aqueous in-process of both phases (aqueous and polymer mixing phase). In addition, the study provides a comparative assessment between preservative-free and preserved formulations, supporting regulatory compliance, stability evaluation, and bioequivalence assessment of generic ophthalmic products.

Rosacea is a chronic skin condition with limited effective and well-tolerated treatment options. This study investigated the efficacy of 0.5% timolol maleate eye drops in treating facial rosacea lesions. A randomized, triple-blind, placebo-controlled clinical trial was conducted at Razi Hospital in Tehran, involving 42 participants diagnosed with erythematotelangiectatic rosacea (ETR). Participants were randomized to receive either 0.5% timolol maleate eye drops or a placebo (distilled water) administered once daily for 4 weeks. The participants were evaluated in three visits (at baseline, after 4 weeks of treatment, and 4 weeks after stopping treatment) using a Mexameter MX18 device (for lightness and erythema), Clinician Erythema Assessment Scale (CEA), Global Flushing Severity Score (GFSS), Patient Self-Assessment (PSA), and Visioface device (for ΔL and ΔE criteria). The primary outcome was the change in erythema severity, assessed by the Mexameter MX18 device. The timolol group significantly reduced Erythema Index (p < 0.001) and other secondary outcomes, including CEA, PSA, and GFSS. No significant adverse effects were reported. In addition, MANOVA revealed a significant time × group interaction across outcomes, indicating that the pattern of changes over time was significantly different between the intervention and placebo groups. This study provides preliminary evidence that 0.5% timolol eye drops could be an effective and well-tolerated treatment for facial rosacea. However, the small sample size and short follow-up duration limited our results.

Because of the variability in excretion of timolol into breastmilk and minimal reported experience during breastfeeding, other agents may be preferred, especially while nursing a newborn or preterm infant. Ophthalmic use of timolol by the mother should pose little risk to the breastfed infant, although some guidelines state that gel formulations are preferred over solutions.[1,2] To substantially diminish the amount of drug that reaches the breastmilk after using eye drops, place pressure over the tear duct by the corner of the eye for 1 minute or more, then remove the excess solution with an absorbent tissue.

Glaucoma remains a leading cause of irreversible blindness worldwide, yet conventional topical therapies are often hampered by poor patient adherence, and standard in-office applanation tonometry captures only static measurements, failing to capture the dynamic nature of intraocular pressure (IOP). Smart contact lenses have emerged as promising tools for home-based, real-time IOP monitoring and feedback-guided therapy; however, most rely on bulky or rigid electronics that impair comfort, safety, and visual performance. Here, we report a battery-free, all-polymer microfluidic theranostic smart contact lens (AP-TSCL) that enables autonomous IOP-responsive glaucoma therapy without bulky electronic components. The AP-TSCL integrates a noninvasive microfluidic IOP sensor with a multistage, pressure-gated drug delivery architecture. Embedded microchannels define distinct activation thresholds, enabling lens deformation under elevated IOP to drive staged release from multiple drug reservoirs. Across in vitro (artificial eye model), ex vivo (enucleated bovine eyes), and in vivo (rabbit ocular hypertension) studies, the device achieved tonometry-aligned IOP tracking, pressure-triggered delivery of timolol or brimonidine above preset thresholds, and IOP lowering comparable to conventional topical therapy. This preclinical evidence suggests that the fully integrated platform may overcome key limitations of existing technologies and offers a clinically translatable solution for personalized ocular care.

In situ gels have become a promising approach for ophthalmic drug delivery because they overcome the major limitations of conventional eye drops, such as rapid drainage of the drug, poor bioavailability, and poor patient compliance. These formulations are liquid before administration and undergo sol-gel transition in response to ocular stimuli such as temperature, pH, or tear ions, thus extending the time of precorneal residence and allowing controlled release. This review summarizes the existing progress in the design and use of ophthalmic in-situ gels, with a special focus on their mechanistic basis, formulation parameters, and clinical progress. Ion-activated gellan gum systems, such as the marketed gel-forming solution of timolol, have shown clinical viability, while pH- and thermosensitive systems have shown promising preclinical and early clinical results. Recent developments have involved the incorporation of polymers with nanoparticles, hybrid gel systems, and new excipients to improve stability, ocular penetration, and patient tolerability. This article offers a contemporary review of the therapeutic potential of ophthalmic in-situ gels and the ability of these gels to enhance the management of pathologies such as glaucoma, dry eye disease, and ocular infections by synthesizing evidence from preclinical and clinical research.

PurposeTo evaluate the efficacy and safety of tafluprost and timolol combination in open-angle glaucoma (OAG) and ocular hypertension (OHT).MethodsPubMed, Embase, Scopus, ClinicalTrials.gov and Cochrane Library databases were searched from their inception until March 28, 2025. Meta-analysis was conducted utilizing the 'metaprop' and 'metamean' packages in R Studio (version 4.4.3). We pooled proportion or incidence rate along with the respective 95% confidence interval (CI) and mean difference with 95% CI for continuous outcomes using a random effects model. The I2 test was employed to assess heterogeneity between the studies.ResultsThis meta-analysis included 15 studies involving 2066 patients. The pooled overall mean decrease in intraocular pressure (IOP) was -4.28 mmHg (95% CI: -6.21 to -2.34, I2 = 98.1%). Subgroup analysis indicated a more substantial IOP reduction in treatment-naïve individuals of -7.81 mmHg (95% CI: -10.73 to -4.90, I2 = 91.3%) when compared to the monotherapy switch group (-2.95 mmHg [95% CI: -5.09 to -0.81, I2 = 98.2%]). The incidence of any adverse event was 16% (95% CI: 6% to 37%, I2 = 96.2%), while incidence of serious adverse events was 2% (95% CI: 1% to 6%, I2 = 54.6%) and discontinuations were at 2% (95% CI: 1% to 5%, I2 = 52%).ConclusionThe fixed-dose combination of tafluprost and timolol notably decreases IOP, particularly in treatment-naïve patients, while exhibiting minimal systemic side effects and a satisfactory safety profile, thus endorsing its clinical application in the management of glaucoma and ocular hypertension.

Background and Objectives: This study evaluates the safety, tolerability, and efficacy of preservative-free Dorzolamide 2%-Timolol 0.5% (PF-DT), with a focus on improving the ocular microenvironment in a real-world transition setting. Materials and Methods: A prospective, multicenter, open-label study involving thirty patients with dry eye disease previously treated with BAK-DT was conducted. Participants were transitioned to PF-DT, and evaluated at weeks 4, 12, and 24. The primary endpoint was the Ocular Surface Disease Index (OSDI) score. Secondary outcomes included Break-Up Time (BUT), Schirmer test results, corneal staining, conjunctival hyperemia, intraocular pressure (IOP), and patient satisfaction. Results: Twenty-five patients completed the study. The OSDI improved from 21.5 to 12.5 (p < 0.001), with 60.0% of patients showing improvement and 52.0% achieving complete symptom resolution. Among eyes with corneal staining, 78.4% demonstrated a reduction of at least one grade, and 50.0% of those with conjunctival redness showed similar improvement. By week 24, 78.0% exhibited no corneal staining, and 50.0% had no conjunctival redness. BUT increased from 5.0 to 7.0 (p < 0.01), while IOP decreased by 1 mmHg (p < 0.01). Satisfaction regarding comfort (≥80%) and handling (≥50%) was high, with 88.0% preferring PF-DT. Conclusions: Transitioning to PF-DT improved ocular surface health while maintaining IOP control, supporting the benefits of preservative-free formulations in restoring microenvironment homeostasis and enhancing tolerability and patient satisfaction.