loteprednol etabonate / Generic mfg. - LARVOL DELTA

Alembic Pharmaceuticals Ltd… said it has received final approval from the US health regulator for its generic version of Loteprednol Etabonate and Tobramycin ophthalmic suspension used for treatment of eye infection. (The Hindu Business Line) - "The approval granted by the US Food & Drug Administration (USFDA) for the Abbreviated New Drug Application (ANDA) Loteprednol Etabonate and Tobramycin Ophthalmic Suspension of strength 0.5 per cent/0.3 per cent (5 mL and 10 mL), Alembic Pharmaceuticals Ltd said in a regulatory filing...Alembic was granted a Competitive Generic Therapy (CGT) designation for this application. With this approval, Alembic is eligible for 180 days of CGT exclusivity upon commercialisation, it added."

ANDA • Infectious Disease • Ocular Inflammation

Different formulations of corticosteroid eye drops at different treatment times in the control of inflammation and prevention of cystoid macular edema after cataract surgery: randomized clinical trial. (PubMed, Arq Bras Oftalmol) - "Equivalent postoperative inflammation control can be achieved using different corticosteroid eye drop formulations at varying treatment durations following cataract surgery. Brazilian Registry of Clinical Trials (ReBEC): RBR-2frpntv."

Clinical • Journal • Cataract • Inflammation • Macular Degeneration • Macular Edema • Ocular Inflammation • Ophthalmology • Retinal Disorders • Uveitis

The Role of Loteprednol in Reducing Post-Intravitreal Injection Related Pain (clinicaltrials.gov) - P=N/A | N=64 | Completed | Sponsor: Virginia Polytechnic Institute and State University | Recruiting ➔ Completed

Trial completion • Age-related Macular Degeneration • Macular Degeneration • Ophthalmology • Pain • Retinal Disorders

Efficacy and Safety of Loteprednol Etabonate in Managing Pain and Inflammation After Cataract Surgery: A Systematic Review and Meta-analysis. (PubMed, Eye Contact Lens) - "Loteprednol etabonate demonstrates significant efficacy in alleviating pain and inflammation post-cataract surgery, with notable advantages in safety, including minimal impact on intraocular pressure and reduced adverse events."

Journal • Retrospective data • Cataract • Inflammation • Ocular Inflammation • Ophthalmology • Pain

Which topical ophthalmic drugs work best for Keratoconjunctivitis Sicca? A systematic review and meta-analysis. (PubMed, Naunyn Schmiedebergs Arch Pharmacol) - "The study concluded that cyclosporine therapy offers improvements in corneal fluorescein staining but does not significantly affect other common DED symptoms, such as OSDI, TBUT, and Schirmer test scores. Similarly, no significant improvements in DED symptoms were observed with loteprednol etabonate or diquafosol sodium. Further research is needed to explore the efficacy of these treatments in managing DED symptoms more comprehensively."

Journal • Retrospective data • Conjunctivitis • Dry Eye Disease • Ocular Infections • Ocular Inflammation • Ophthalmology • Sjogren's Syndrome

PCR-Based Evaluation of Viral Load Reduction in Adenoviral Conjunctivitis: A Comparative Study of Ganciclovir and Povidone-Iodine. (PubMed, Ocul Immunol Inflamm) - "To evaluate the efficacy of topical ganciclovir (GCV), povidone-iodine (PVP-I), and their combination with loteprednol etabonate (LE) in reducing viral load and improving clinical outcomes in adenoviral conjunctivitis. PVP-I significantly decreased viral load in the early phase, while PVP-I/LE and GCV/LE combinations led to faster clinical improvement. Subepithelial infiltrates were significantly lower in the PVP-I/LE group, suggesting this combination may help prevent complications and offer an effective treatment option."

Journal • Conjunctivitis • Dry Eye Disease • Ocular Infections • Ocular Inflammation • Ophthalmology

Mucoadhesive Micellar Eyedrops for the Treatment of Ocular Inflammation. (PubMed, Acta Biomater) - "Commercial eyedrops, like Oceanside® (0.5% loteprednol etabonate (LE) ophthalmic suspension), suffer from low ocular bioavailability and require frequent dosing to maintain therapeutic levels...These micelles showed high PBA conjugation efficiency (>67%), a 12-day sustained release of LE, strong mucin adhesion, in vitro and in vivo biocompatibility. In a mouse model of corneal inflammation, a once-daily LE-loaded micellar eyedrop matched the efficacy of the commercial LE eyedrop (Oceanside®, 0.5%), which is dosed four times daily, reducing corneal opacity, preserving corneal structure, and decreasing inflammation."

Journal • Inflammation • Keratitis • Ocular Inflammation • Ophthalmology

Childhood-onset ocular mucous membrane pemphigoid presenting with peripheral ulcerative keratitis: a case report and review of the literature. (PubMed, J Ophthalmic Inflamm Infect) - "Pediatric mucous membrane pemphigoid with ocular involvement is a rare condition of which few reports have been published, resulting in scarce information regarding its clinical course and response to treatment. We report the first case observed in a Hispanic patient, opening with peripheral ulcerative keratitis, and responding successfully to methotrexate."

Journal • Conjunctivitis • Immunology • Inflammation • Keratitis • Ocular Infections • Ocular Inflammation • Ophthalmology • Pediatrics

Predictive Factors for Long-Term De Novo Intraocular Pressure Elevation After Descemet Membrane Endothelial Keratoplasty. (PubMed, Cornea) - "Pseudoexfoliation, prolonged steroid use, and peripheral anterior synechiae were identified as risk factors for IOP elevation after DMEK. In these complex cases, switching to a milder steroid at an earlier stage may be recommended, provided that the balance is maintained to avoid compromising graft survival."

Biomarker • Journal • Glaucoma • Ophthalmology • Transplantation

Effects of Loteprednol Etabonate and Ketorolac Tromethamine on Intraocular Inflammation and Oxidative Stress After Paracentesis-Induced Blood-Aqueous Barrier Breakdown in Cats. (PubMed, Vet Ophthalmol) - "LE and KT effectively reduced PGE2 levels following paracentesis. LE also significantly decreased TP levels, mitigated miosis, and preserved GSH, indicating reduced oxidative stress. Considering that KT also reduced PGE2 levels, further studies are warranted to determine whether KT might effectively reduce protein influx into the anterior chamber at later time points."

Journal • Inflammation • Ocular Inflammation • Ophthalmology • Uveitis

Improved Therapy of Ocular Inflammation via Eyedrops Containing Mucoadhesive Drug-Eluting Nanoparticles (ARVO 2025) - "Methods Drug-loaded micelles (PBA-LE-MCs) were synthesized by self-assembly of phenylboronic acid (PBA)-bearing block copolymers with loteprednol etabonate (LE, a corticosteroid) and incorporated into a hyaluronic acid-based matrix to form mucoadhesive eyedrops...Layman Abstract (optional): Provide a 50-200 word description of your work that non-scientists can understand. Describe the big picture and the implications of your findings, not the study itself and the associated details."

Ocular Inflammation • Ophthalmology • IL1B • IL6 • PTPRC

Overcoming barriers in formulating practically insoluble loteprednol etabonate in ophthalmic nanoemulsion. (PubMed, Eur J Pharm Sci) - "LE retention within oil droplets (above 90% of the initial LE content) despite biorelevant dilution simulating tear turnover suggests the potential for direct LE absorption from the NE oil droplets into the lipophilic corneal epithelium. The results obtained encourage the extension of the studies in terms of in vitro permeability and in vivo eye-related bioavailability assessment to prove the potential of the proposed LE formulation."

Journal • Dry Eye Disease • Ophthalmology

Loteprednol etabonate alleviates NLRP3 inflammasome-associated inflammatory diseases in mice by suppressing the transcription of IL-1β. (PubMed, Int J Biol Macromol) - "Furthermore, in mouse models of NLRP3 inflammasome-associated inflammatory diseases, including LPS-induced sepsis and DSS-induced colitis, intraperitoneal injection of LE significantly suppressed inflammatory response and improved mice survival rate. Collectively, these findings identify LE as a novel inhibitor of NLRP3 inflammasome activation, offering a promising therapeutic strategy for the treatment of NLRP3 inflammasome-associated inflammatory diseases."

Journal • Preclinical • Gastroenterology • Gastrointestinal Disorder • Immunology • Infectious Disease • Inflammation • Septic Shock • IL1B • NLRP3

Preparation of dried nanoemulsion formulation by electrospinning. (PubMed, Eur J Pharm Sci) - "The aim of this study was to investigate electrospinning as a method for the preparation of a solid eye preparation based on nanoemulsion loaded with the anti-inflammatory drug loteprednol etabonate...A rheological study revealed the predominant elastic behavior of the dispersed nanofibers, which indicates the formation of a weak gel after the dispersion of the dried nanoemulsion in tear fluid at the ocular surface. The biocompatibility of the dried nanoemulsions in the form of nanofibers after a single and multiple-dose application was confirmed using the 3D HCE-T model of the stratified epithelium of the human cornea, suggesting that this innovative solid eye preparation could represent a new approach to the treatment of dry eye disease."

Journal • Dry Eye Disease • Ophthalmology

The Role of Loteprednol in Reducing Post-Intravitreal Injection Related Pain (clinicaltrials.gov) - P=N/A | N=72 | Recruiting | Sponsor: Virginia Polytechnic Institute and State University | Trial completion date: Dec 2024 ➔ Jun 2025 | Trial primary completion date: Sep 2024 ➔ May 2025

Trial completion date • Trial primary completion date • Age-related Macular Degeneration • Macular Degeneration • Ophthalmology • Pain • Retinal Disorders

Ophthalmic corticosteroids-related adverse events: the FDA adverse event reporting system (FAERS) database pharmacovigilance study. (PubMed, Front Pharmacol) - "A total of 9,854 ADRs related to ophthalmic corticosteroids were retrieved, with the most frequently reported drugs being Ozurdex (1,784 cases), Lotemax (3,239 cases), and Durezol (2,789 cases)...Additionally, Maxidex has been linked to endocrine disorders, while Ozurdex, Iluvien, and Triesence exhibited significant signals for product issues, likely related to their intraocular injection procedures...These findings highlight the need for careful monitoring and individualized treatment plans to minimize the risk of ADRs in patients receiving corticosteroid therapy. Future studies combining FAERS data with large-scale clinical research are needed to explore these safety concerns further."

Adverse events • Journal • Cataract • Endocrine Disorders • Infectious Disease • Inflammation • Ocular Inflammation • Ophthalmology • Pain • Retinal Disorders • Uveitis

Prolonged Release Niosomes For Ocular Delivery of Loteprednol: Ocular Distribution Assessment on Dry Eye Disease Induced Rabbit Model. (PubMed, AAPS PharmSciTech) - "Loteprednol etabonate (LE) is a topical corticosteroid for the symptomatic management of ocular conditions, encompassing both allergic and infectious etiologies...No irritation or hemorrhagic situation was observed according to the results of HET-CAM study. Thus, novel LE-loaded niosomal formulations could be considered as a promising treatment option for the dry-eye-disease (DED) due to enhanced bioavailability and decreased side effects."

Journal • Preclinical • Dry Eye Disease • Hematological Disorders • Ophthalmology

Exploring the Influence of Drug Substance Solid-State Properties on the In Vitro Drug Release Performance of Dexamethasone Ophthalmic Ointments (ARVO 2024) - "Purpose: This study aims at (i) exploring how variations in polymorphic forms, crystallinity, and particle size distribution of dexamethasone (DEX) affects its in vitro release (IVR) performance from ophthalmic ointments, and (ii) to integrate these findings with research on loteprednol etabonate (LTE) and acyclovir (ACY) ointments, to offer a broader perspective on the effect of drug substance characteristics on IVR... The solid-state characteristics of DEX significantly influence its IVR from ophthalmic ointments, being more influenced by solid-state form, particularly the amorphous state, than by particle size. This phenomenon is also observed in LTE ointments.1 Both DEX and LTE, being moderately lipophilic compounds (logP = 1.8-2.0), demonstrate a strong affinity for the oleaginous base, and are subject to size reduction and normalization through high-shear mixing with petrolatum. Conversely, for the hydrophilic drug ACY (logP = -1.6), particle size is crucial, with..."

Preclinical • Ophthalmology

Mucoadhesive Micellar Eyedrop for Sustained Delivery of Anti-inflammatory Drugs to Injured Eyes (ARVO 2024) - "Purpose: Ocular inflammation is one of the leading causes of blindness worldwide, and corticosteroid eye drops (e.g., loteprednol etabonate (LE) drops) are the mainstay of therapy... LE-MCs showed suitable size, optimal drug release, and excellent biocompatibility. Our mucoadhesive eye drops may eliminate the need for intensive administration of eye drops and hold promise as a safe and efficient solution for corneal inflammation."

Keratitis • Ocular Inflammation • Ophthalmology

Anti-inflammatory medication use after cataract surgery: online survey of practice patterns. (PubMed, J Cataract Refract Surg) - "Most surgeons prescribed topical AIM after routine cataract surgery. Many surgeons injected intraocular or periocular AIM while prescribing topical AIM. The diversity of practice patterns may reflect the lack of clear evidence-based guidelines."

Journal • Surgery • Cataract • Ophthalmology

Managing Dry Eye Disease with Novel Medications: Mechanism, Study Validity, Safety, Efficacy, and Practical Application. (PubMed, Pharmacy (Basel)) - "The keywords "Dry Eye Disease", "lifitegrast", "cyclosporine", "loteprednol etabonate", "varenicline nasal spray", and "perfluorohexyloctane" were used to identify these medications' landmark trials. In conclusion, these FDA-approved novel medications exhibit safety and efficacy in managing DED. Further research is needed on long-term outcomes, efficacy, and side-effect comparisons, and combination therapy benefits."

Journal • Review • Dry Eye Disease • Ophthalmology

Characterization of CYP3A5 Selective Inhibitors for Reaction Phenotyping of Drug Candidates. (PubMed, AAPS J) - "The selectivity of difluprednate in HLM is much weaker than that in the recombinant enzymes due to hydrolysis of the acetate group in HLM. Based on the selectivity data, loteprednol etabonate can be utilized as an orthogonal approach, when experimental fraction metabolized of CYP3A5 is greater than 0.5, to understand CYP3A5 contribution to drug metabolism and its clinical significance. Future endeavors to identify even more selective CYP3A5 inhibitors are warranted to enable accurate determination of CYP3A5 contribution to metabolism versus CYP3A4."

Journal • CYP3A5

Engineering a drug eluting ocular patch for delivery and sustained release of anti-inflammatory therapeutics. (PubMed, AIChE J) - "Herein, we engineered a photocrosslinkable adhesive patch (GelPatch) incorporated with micelles (MCs) loaded with Loteprednol etabonate (LE) for delivery and sustained release of drug...In addition, subcutaneous implantation of the MC loaded GelPatch in rats confirmed its in vivo biocompatibility and stability within 28 days. This non-invasive, adhesive, and biocompatible drug eluting patch can be used as a matrix for the delivery and sustained release of hydrophobic drugs."

Journal • Inflammation • Ocular Inflammation • Ophthalmology

The Role of Loteprednol in Reducing Post-Intravitreal Injection Related Pain (clinicaltrials.gov) - P=N/A | N=72 | Recruiting | Sponsor: Virginia Polytechnic Institute and State University | Trial primary completion date: Sep 2023 ➔ Sep 2024

Trial primary completion date • Age-related Macular Degeneration • Macular Degeneration • Ophthalmology • Pain • Retinal Disorders

Determination of the Toxicity Preferences of Ocular Drug Delivery System by Comparing Two Different Toxicity Bioassays. (PubMed, Assay Drug Dev Technol) - "The toxicity of loteprednol etabonate loaded solid lipid nanoparticles, lipid nanostructured carriers, and nanoemulsion were compared...It is noteworthy that the HET-CAM assay offers a more cost-effective and environmentally friendly alternative to the MTT assay, as it does not require cell culture and generates less toxic waste. This information may be useful to consider when selecting between the two assays."

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