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1.
Int Ophthalmol ; 44(1): 211, 2024 May 02.
Article in English | MEDLINE | ID: mdl-38696090

ABSTRACT

PURPOSE: To evaluate the effects of sodium hyaluronate drops on dry eye parameters and corneal epithelial thickness following cataract surgery. METHODS: The study included 84 patients who underwent uncomplicated phacoemulsification. In Group A, 0.15% sodium hyaluronate drops were added to the postoperative antibiotic/anti-inflammatory treatment. In Group B, only antibiotic/anti-inflammatory treatment was applied. Preoperatively and at 1 week and 1 month postoperatively, all the patients were evaluated in respect of tear break-up time (TBUT), the Schirmer test under anesthesia, the corneal fluorescein staining (CFS) score, mean central corneal thickness (CCT) and mean central corneal epithelial thickness (CCET), and the two groups were compared. RESULTS: A statistically significant difference was determined between the two groups at postoperative 1 month in respect of TBUT, Schirmer test, CFS score, and CCET (p < 0.01). In Group A, a statistically significant increase was determined in the TBUT and Schirmer values at 1 month postoperatively (p < 0.01, p = 0.01, respectively) and in Group B, these values were decreased compared to preoperatively (p < 0.01). The CCET was determined to be significantly thinner in Group B 1 month postoperatively (p < 0.01). A significant increase in CCT was observed in both groups at postoperative 1 week (p < 0.01) and preoperative values were reached at 1 month postoperatively. CONCLUSION: In the patient group using sodium hyaluronate, significant differences were determined in all dry eye parameters and CCET. The use of hyaluronate sodium drops after cataract surgery was seen to improve dry eye parameters and contribute to a healthy ocular surface by ensuring continuity of the corneal epithelium.


Subject(s)
Dry Eye Syndromes , Epithelium, Corneal , Hyaluronic Acid , Ophthalmic Solutions , Phacoemulsification , Humans , Hyaluronic Acid/administration & dosage , Dry Eye Syndromes/drug therapy , Dry Eye Syndromes/diagnosis , Female , Male , Aged , Epithelium, Corneal/drug effects , Epithelium, Corneal/pathology , Middle Aged , Ophthalmic Solutions/administration & dosage , Phacoemulsification/methods , Viscosupplements/administration & dosage , Prospective Studies , Tears/metabolism , Postoperative Complications/prevention & control , Cataract Extraction/methods
2.
Vestn Oftalmol ; 140(2): 102-111, 2024.
Article in Russian | MEDLINE | ID: mdl-38742506

ABSTRACT

Dry eye disease (DED) is pathogenetically based on inflammation of the ocular surface. A step-by-step approach to DED treatment involves early initiation of anti-inflammatory therapy, including instillation of cyclosporine A (CsA). However, recommendations for the use of topical CsA in clinical practice are limited. This article presents an expert consensus on practical recommendations for the management of patients with DED, including indications, time of initiation and duration of CsA therapy, comparison of CsA forms currently registered in the Russian Federation, as well as issues of patient education.


Subject(s)
Cyclosporine , Emulsions , Humans , Administration, Ophthalmic , Cyclosporine/administration & dosage , Dry Eye Syndromes/drug therapy , Dry Eye Syndromes/etiology , Immunosuppressive Agents/administration & dosage , Ophthalmic Solutions/administration & dosage , Treatment Outcome , Xerophthalmia/etiology , Xerophthalmia/drug therapy , Xerophthalmia/diagnosis
3.
AAPS PharmSciTech ; 25(5): 119, 2024 May 30.
Article in English | MEDLINE | ID: mdl-38816667

ABSTRACT

Loteprednol etabonate (LE) is a topical corticosteroid for the symptomatic management of ocular conditions, encompassing both allergic and infectious etiologies. Owing to the dynamic and static barriers of the eye, LE exhibits significantly low bioavailability, necessitating an increase in the frequency of drug administration. The objective of this study is to overcome the limitations by developing niosomal systems loaded with LE. Design of Experiments (DoE) approach was used for the development of optimal niosome formulation. The optimal formulation was characterized using DLS, FT-IR, and DSC analysis. In vitro and ex vivo release studies were performed to demonstrate drug release patterns. After that HET-CAM evaluation was conducted to determine safety profile. Then, in vivo studies were carried out to determine therapeutic activity of niosomes. Zeta potential (ZP), particle size, polydispersity index (PI), and encapsulation efficacy (EE) were -33.8 mV, 89.22 nm, 0.192, and 89.6%, respectively. Medicated niosomes had a broad distribution within rabbit eye tissues and was absorbed by the aqueous humor of the bovine eye for up to 6 h after treatment. Cumulative permeated drug in the bovine eye and rabbit eye were recorded 52.45% and 54.8%, respectively. 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.


Subject(s)
Delayed-Action Preparations , Dry Eye Syndromes , Liposomes , Loteprednol Etabonate , Animals , Rabbits , Delayed-Action Preparations/administration & dosage , Delayed-Action Preparations/pharmacokinetics , Loteprednol Etabonate/administration & dosage , Loteprednol Etabonate/pharmacokinetics , Dry Eye Syndromes/drug therapy , Cattle , Drug Liberation , Particle Size , Disease Models, Animal , Administration, Ophthalmic , Biological Availability , Drug Delivery Systems/methods , Eye/metabolism , Eye/drug effects , Aqueous Humor/metabolism , Chemistry, Pharmaceutical/methods , Ophthalmic Solutions/administration & dosage , Ophthalmic Solutions/pharmacokinetics
5.
Int J Nanomedicine ; 19: 4021-4040, 2024.
Article in English | MEDLINE | ID: mdl-38736657

ABSTRACT

Cataract is a leading cause of blindness globally, and its surgical treatment poses a significant burden on global healthcare. Pharmacologic therapies, including antioxidants and protein aggregation reversal agents, have attracted great attention in the treatment of cataracts in recent years. Due to the anatomical and physiological barriers of the eye, the effectiveness of traditional eye drops for delivering drugs topically to the lens is hindered. The advancements in nanomedicine present novel and promising strategies for addressing challenges in drug delivery to the lens, including the development of nanoparticle formulations that can improve drug penetration into the anterior segment and enable sustained release of medications. This review introduces various cutting-edge drug delivery systems for cataract treatment, highlighting their physicochemical properties and surface engineering for optimal design, thus providing impetus for further innovative research and potential clinical applications of anti-cataract drugs.


Subject(s)
Cataract , Drug Delivery Systems , Nanomedicine , Humans , Cataract/drug therapy , Nanomedicine/methods , Drug Delivery Systems/methods , Nanoparticles/chemistry , Animals , Lens, Crystalline/drug effects , Cataract Extraction , Nanoparticle Drug Delivery System/chemistry , Ophthalmic Solutions/chemistry , Ophthalmic Solutions/pharmacokinetics , Ophthalmic Solutions/administration & dosage
7.
Sci Rep ; 14(1): 12459, 2024 05 30.
Article in English | MEDLINE | ID: mdl-38816428

ABSTRACT

The aim was clinical evaluation of the efficacy of topical insulin eye drops in patients with refractory persistent epithelial defects (PEDs). This prospective non-randomized investigation was conducted to examine the efficacy of insulin eye drops in treating patients with PEDs that did not respond to conventional therapy. A total of twenty-three patients were included in the study, and they were administered insulin eye drops formulated as 1 U/mL, four times a day. The rate of epithelial defect resolution and time to complete corneal re-epithelialization were considered primary outcome measures. The relative prognostic impact of initial wound size and other parameters, including age, sex, smoking, diabetes, and hypertension were also analyzed. The results showed that during follow-up (maximum 50 days), a total of 16 patients (69.6%) achieved improvement. Insulin eye drops significantly reduced the corneal wounding area in 75% of patients with small epithelial defects (5.5 mm2 or less) during 20 days. Only 61% of patients with moderate epithelial defects (5.51-16 mm2) showed a significant recovery in 20-30 days. Also, 71% of patients with a defect size greater than 16 mm2, demonstrated a significant improvement in the rate of corneal epithelial wound healing in about 50 days. In conclusion topical insulin reduces the PED area and accelerates the ocular surface epithelium wound healing.


Subject(s)
Epithelium, Corneal , Insulin , Ophthalmic Solutions , Humans , Male , Female , Middle Aged , Epithelium, Corneal/drug effects , Epithelium, Corneal/pathology , Insulin/administration & dosage , Aged , Ophthalmic Solutions/administration & dosage , Prospective Studies , Adult , Wound Healing/drug effects , Administration, Topical , Corneal Diseases/drug therapy , Corneal Diseases/pathology , Treatment Outcome , Re-Epithelialization/drug effects
8.
Harefuah ; 163(5): 278-285, 2024 May.
Article in Hebrew | MEDLINE | ID: mdl-38734939

ABSTRACT

INTRODUCTION: The importance of myopia management lies in the desire to minimize the potential ocular risks that increase with high myopia. AIMS: To assess the decrease in myopia progression using topical low dose atropine combined with peripheral blur contact lenses (CL). METHODS: This retrospective review study included 25 children between the ages of 8.5 years to 14 years. The children all had a minimal increase in myopia of 0.75D during the year prior to treatment. The children were divided into two groups. The control group included 14 children who wore single-vision spectacles )SV) averaging 3.20±0.9D ranging from 1.5-5.3D. The study group included 11 children who wore dual-focus CL, with an average prescription of 3.4±0.7D ranging from 2.5 to 4.3D, for one year. At that point, when an additional myopia increase was observed, the children were additionally treated with topical 0.01% atropine for two years (CL+A0.01). RESULTS: There was an increase in myopia in the SV group of 1.12±0.52D, 1.08±0.56D and 0.96±0.53D in the first, second, and third years, respectively. The myopia increase in the CL+A0.01 group was 0.57±0.48D, 0.14±0.34D, and 0.17±0.29D in the first, second, and third years, respectively. CONCLUSIONS: Low-dose atropine combined with peripheral blur contact lenses was effective in decreasing myopia progression in this study. Additional, larger-scale studies are required in the future. DISCUSSION: This study found a significant decrease in myopia progression in the second and third years of treatment. The CL group showed less effectivity than the CL+A0.01 group.


Subject(s)
Atropine , Contact Lenses , Disease Progression , Myopia , Humans , Atropine/administration & dosage , Child , Myopia/therapy , Myopia/physiopathology , Retrospective Studies , Adolescent , Male , Female , Treatment Outcome , Mydriatics/administration & dosage , Ophthalmic Solutions/administration & dosage , Eyeglasses
9.
Vestn Oftalmol ; 140(2. Vyp. 2): 73-79, 2024.
Article in Russian | MEDLINE | ID: mdl-38739134

ABSTRACT

The management protocol for patients with neovascular age-related macular degeneration (nAMD) involves multiple intravitreal injections (IVI) of anti-VEGF drugs. The ability to reduce the peak intraocular pressure (IOP) rise is greatly important in clinical practice. PURPOSE: This study evaluates the effect of topical hypotensive drugs on the short-term IOP rise after IVI of anti-VEGF drugs in patients with nAMD. MATERIAL AND METHODS: The prospective study included 80 patients with newly diagnosed nAMD. Before the start of treatment, the patients were divided into 4 groups of 20 people each: 1st - controls, who received no prophylactic drugs, in the 2nd, 3rd and 4th groups local instillations of one drop of hypotensive drugs brinzolamide 1%, brinzolamide-timolol, brimonidine-timolol were performed in the conjunctival sac twice: 1 day before the injection (at 20:00) and on the day of the injection 2 hours before the manipulation (at 08:00), respectively. IOP was measured in each patient using ICare Pro non-contact tonometer before injection, as well as 1 min, 30 and 60 min after injection. RESULTS: Prophylactic use of hypotensive drugs was associated with a significant decrease in IOP immediately after IVI compared to the same parameter in the 1st group (p<0.001), the maximum decrease in IOP values was observed when using a fixed combination of brimonidine-timolol by 12.1 mm Hg compared to the controls (p<0.001), the combination of brinzolamide-timolol reduced IOP by 8.5 mm Hg (p<0.001), brinzolamide 1% led to the smallest decrease in IOP - by 5.1 mm Hg (p<0.001). CONCLUSION: Study patients that received instillations of brimonidine-timolol combination of one drop into the conjunctival sac 1 day before the injection and on the day of the injection showed the maximum decrease in IOP compared to patients of the other groups.


Subject(s)
Angiogenesis Inhibitors , Intraocular Pressure , Intravitreal Injections , Ocular Hypertension , Sulfonamides , Humans , Male , Female , Aged , Intraocular Pressure/drug effects , Ocular Hypertension/prevention & control , Ocular Hypertension/drug therapy , Ocular Hypertension/physiopathology , Angiogenesis Inhibitors/administration & dosage , Prospective Studies , Sulfonamides/administration & dosage , Treatment Outcome , Antihypertensive Agents/administration & dosage , Vascular Endothelial Growth Factor A/antagonists & inhibitors , Tonometry, Ocular/methods , Middle Aged , Timolol/administration & dosage , Brimonidine Tartrate/administration & dosage , Ophthalmic Solutions/administration & dosage , Thiazines/administration & dosage , Macular Degeneration/drug therapy , Macular Degeneration/diagnosis
10.
Biol Pharm Bull ; 47(5): 1033-1042, 2024.
Article in English | MEDLINE | ID: mdl-38797668

ABSTRACT

Eye drops, including solutions and suspensions, are essential dosage forms to treat ophthalmic diseases, with poorly water-soluble drugs typically formulated as ophthalmic suspensions. In addition to low bioavailability, suspensions exhibit limited efficacy, safety, and usability due to the presence of drug particles. Improving bioavailability can reduce the drug concentrations and the risk of problems associated with suspended drug particles. However, practical penetration enhancers capable of improving bioavailability remain elusive. Herein, we focused on penetratin (PNT), a cell-penetrating peptide (CPP) that promotes active cellular transport related to macromolecule uptake, such as micropinocytosis. According to the in vitro corneal uptake study using a reconstructed human corneal epithelial tissue model, LabCyte CORNEA-MODEL24, PNT enhanced the uptake of Fluoresbrite® YG carboxylate polystyrene microspheres without covalent binding. In an ex vivo porcine eye model, the addition of 10 µM PNT to rebamipide ophthalmic suspension markedly improved the corneal uptake of rebamipide; however, the addition of 100 µM PNT was ineffective due to potentially increased particle size by aggregation. This article provides basic information on the application of PNT as a penetration enhancer in ophthalmic suspensions, including the in vitro and ex vivo studies mentioned above, as well as the 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) cytotoxicity assay and storage stability at different pH values.


Subject(s)
Cell-Penetrating Peptides , Cornea , Ophthalmic Solutions , Suspensions , Animals , Cell-Penetrating Peptides/chemistry , Cell-Penetrating Peptides/administration & dosage , Ophthalmic Solutions/administration & dosage , Humans , Cornea/metabolism , Cornea/drug effects , Swine , Quinolones/administration & dosage , Quinolones/pharmacokinetics , Quinolones/chemistry , Administration, Ophthalmic , Biological Availability , Epithelium, Corneal/drug effects , Epithelium, Corneal/metabolism , Particle Size , Alanine/analogs & derivatives
11.
Int Ophthalmol ; 44(1): 193, 2024 Apr 24.
Article in English | MEDLINE | ID: mdl-38653918

ABSTRACT

PURPOSE: This study evaluated the tear film stability in patients with symptoms of dry eye after installation of dual polymer hydroxypropyl guar/sodium hyaluronate (DPHG/SH) vs single polymer SH. METHODS: Patients with recently diagnosed mild to moderate dry eye disease (OSDI score 23-32 points) were included. For each patient, the right eye was randomized to receive DPHG/SH or 0.15% SH. Just after the administration of the drop to the right eye, the fellow eye received the other eye drop. The first non-invasive Keratograph first break-up time (NIKBUT), average NIKBUT and tear meniscus height (TMH) were measured before administration of the eye drops, at 1-min, 15 min, 30 min, 60 min, 90 min, and 120 min after instillation. RESULTS: A total of 29 patients aged 22.8 ± 2.2 years participated in the study (21 women). No differences between the eye receiving DPHG/SH and single polymer SH were observed for the first NIKBUT (p = 0.45) and average NIKBUT (p = 0.24) variables at any time point. Both DPHG/SH and single polymer SH increased the TMH (p of time effect < 0.001), but with no difference between groups (p = 0.95). CONCLUSION: Both DPHG/SH and single polymer SH solutions provide lubrication of the eye surface, however, with no difference in NIKBUT and TMH evaluations for up to two hours following administration.


Subject(s)
Dry Eye Syndromes , Hyaluronic Acid , Ophthalmic Solutions , Tears , Humans , Dry Eye Syndromes/drug therapy , Dry Eye Syndromes/diagnosis , Female , Hyaluronic Acid/administration & dosage , Male , Ophthalmic Solutions/administration & dosage , Young Adult , Adult , Polysaccharides/administration & dosage , Polymers , Viscosupplements/administration & dosage , Prospective Studies
12.
J Ocul Pharmacol Ther ; 40(4): 215-221, 2024 May.
Article in English | MEDLINE | ID: mdl-38597912

ABSTRACT

Purpose: This study aimed to determine the onset and duration of action of 3 commercially available topical anesthetic solutions in Brazil, using the Cochet-Bonnet esthesiometer (Luneau®, Paris, France) and to quantitatively assess patient-reported discomfort during application. Methods: A prospective, randomized, masked, and double-blind study was conducted, involving 40 eyes from 21 patients. Patients were administered each one of the topical anesthetics weekly, and corneal sensitivity was measured using the Cochet-Bonnet esthesiometer's corneal touch threshold (CTT). Patients rated the burning sensation using a visual analogue scale (VAS). Results: Among the 21 patients (42.9% male), with a mean age of 31.95 years (±standard deviation = 10.17, range = 22.0-58.0), corneal sensitivity significantly decreased 30 s after application, returning to baseline after 30 min for all groups (P < 0.0001). Significant differences in CTT were observed at 5 min, with proparacaine exhibiting a superior anesthetic effect (P = 0.0003), at 10 min, where tetracaine displayed the most substantial anesthetic effect (P = 0.0135), and at 20 min, where tetracaine demonstrated the highest anesthetic efficacy (P < 0.0001). VAS scores indicated the most intense burning sensation with tetracaine (P < 0.0001). Men reported experiencing more discomfort during instillation compared with women (P = 0.0168). Conclusions: Proparacaine exhibited the fastest onset of action among the 3 topical anesthetics and provided a more comfortable eye sensation during instillation. However, tetracaine demonstrated the longest duration of action despite causing more discomfort.


Subject(s)
Anesthetics, Local , Cornea , Procaine , Propoxycaine , Tetracaine , Humans , Male , Female , Tetracaine/administration & dosage , Tetracaine/pharmacology , Adult , Double-Blind Method , Propoxycaine/administration & dosage , Propoxycaine/pharmacology , Anesthetics, Local/administration & dosage , Anesthetics, Local/pharmacology , Middle Aged , Prospective Studies , Cornea/drug effects , Procaine/administration & dosage , Procaine/pharmacology , Procaine/analogs & derivatives , Procaine/adverse effects , Young Adult , Ophthalmic Solutions/administration & dosage , Pain Measurement/methods
13.
J Ocul Pharmacol Ther ; 40(4): 240-245, 2024 May.
Article in English | MEDLINE | ID: mdl-38598266

ABSTRACT

Purpose: To compare the efficacy of Brinzolamide-Brimonidine (BB) (1%+0.2%) with the gold standard Latanoprost-Timolol (LT) (0.005%+0.5%) in treating primary open-angle glaucoma (POAG) and ocular hypertension (OHT). Methods: A 1-year prospective study, spanning from May 2022 to May 2023, conducted at a tertiary eye-care hospital. Participants, aged 40-60, with a baseline intraocular pressure (IOP) >21 mm Hg, requiring a >30% reduction, were enrolled. Group A (n = 100) received BB, and Group B (n = 100) received LT. Outcomes were assessed at 1 month (IOP difference from baseline), 3 and 6 months (mean diurnal variations). Results: The mean age at presentation was 55.5 ± 4.5 years in Group A and 54.7 ± 4.2 years in Group B. At 1 month, Group A exhibited a mean IOP of 18.7 mm Hg, while Group B had 17.6 mm Hg, with no statistically significant difference (P = 0.53). No significant diurnal variation was observed in either group (P = 0.07). Target pressure was achieved in 88% of patients in Group A and slightly higher at 92% in Group B. Moreover, no serious side effects were reported, and compliance was higher in Group B (98%) compared to Group A (96%). Conclusion: Although LT showed slightly better and sustained IOP reduction, the difference was not statistically significant. Both BB and LT demonstrated comparable outcomes for managing POAG and OHT.


Subject(s)
Antihypertensive Agents , Brimonidine Tartrate , Glaucoma, Open-Angle , Intraocular Pressure , Latanoprost , Ocular Hypertension , Sulfonamides , Timolol , Humans , Glaucoma, Open-Angle/drug therapy , Middle Aged , Intraocular Pressure/drug effects , Ocular Hypertension/drug therapy , Latanoprost/administration & dosage , Latanoprost/therapeutic use , Latanoprost/pharmacology , Brimonidine Tartrate/administration & dosage , Brimonidine Tartrate/therapeutic use , Brimonidine Tartrate/pharmacology , Brimonidine Tartrate/adverse effects , Male , Female , Prospective Studies , Timolol/administration & dosage , Timolol/therapeutic use , Timolol/adverse effects , Antihypertensive Agents/administration & dosage , Antihypertensive Agents/therapeutic use , Antihypertensive Agents/adverse effects , Antihypertensive Agents/pharmacology , Adult , Sulfonamides/administration & dosage , Sulfonamides/therapeutic use , Sulfonamides/adverse effects , Sulfonamides/pharmacology , Thiazines/administration & dosage , Thiazines/therapeutic use , Thiazines/adverse effects , Drug Combinations , Treatment Outcome , Ophthalmic Solutions/administration & dosage
14.
J Ocul Pharmacol Ther ; 40(4): 232-239, 2024 May.
Article in English | MEDLINE | ID: mdl-38621178

ABSTRACT

Purpose: To assess over 2 weeks, the effect of 3 different low concentrations of atropine on pupillary diameter and accommodative amplitude in children with myopia. Methods: Fifty-eight children with myopia [spherical equivalent (SE) of -0.50 diopters (D) or worse, astigmatism of less than or equal to 2.00 D] were randomly allocated to 3 groups receiving 0.01%, 0.02%, or 0.03% atropine eye drops, once nightly for 2 weeks. The primary outcome was the change from baseline in pupillary diameter and accommodative amplitude with each of the concentrations. Results: Fifty-seven participants (114 eyes), aged between 6 and 12 years, completed the 2-week trial (mean age 9.3 ± 1.7 years and mean SE -3.53 ± 1.79 D). After 2 weeks of use, all the 3 concentrations were found to have a statistically significant effect on both the pupillary diameter and accommodative amplitude. Accommodative amplitude reduced by an average of 5.23 D, 9.28 D, and 9.32 D, and photopic pupil size increased by an average of 0.95 ± 1.05 mm, 1.65 ± 0.93 mm, and 2.16 ± 0.88 mm with 0.01%, 0.02%, and 0.03%, respectively. Of the eyes, a total of 5.3% and 5.9% of the eyes on 0.02% and 0.03% atropine had a mean residual accommodative amplitude of <5 D. The percentage of eyes having a pupillary dilation >3 mm were 4.8%, 10.5%, and 23.5% for 0.01%, 0.02%, and 0.03% atropine, respectively. Conclusions: Low-dose atropine had an effect on pupillary diameter and accommodative amplitude. With the highest concentration assessed, that is, 0.03% nearly 1 of 4 eyes had pupillary dilation of >3 mm. Clinical Trial Registration number: NCT03699423.


Subject(s)
Accommodation, Ocular , Atropine , Mydriatics , Myopia , Ophthalmic Solutions , Pupil , Humans , Atropine/administration & dosage , Atropine/pharmacology , Child , Myopia/drug therapy , Myopia/physiopathology , Accommodation, Ocular/drug effects , Pupil/drug effects , Male , Female , Ophthalmic Solutions/administration & dosage , Mydriatics/administration & dosage , Mydriatics/pharmacology , Mydriatics/therapeutic use , Dose-Response Relationship, Drug
16.
Int J Pharm ; 657: 124110, 2024 May 25.
Article in English | MEDLINE | ID: mdl-38604539

ABSTRACT

The goal of this investigation is to develop stable ophthalmic nanoformulations containing cannabidiol (CBD) and its analog cannabidiol-valine-hemisuccinate (CBD-VHS) for improved ocular delivery. Two nanoformulations, nanoemulsion (NE) and nanomicelles (NMC), were developed and evaluated for physicochemical characteristics, drug-excipient compatibility, sterilization, thermal analysis, surface morphology, ex-vivo transcorneal permeation, corneal deposition, and stability. The saturation solubility studies revealed that among the surfactants tested, Cremophor EL had the highest solubilizing capacity for CBD (23.3 ± 0.1 mg/mL) and CBD-VHS (11.2 ± 0.2 mg/mL). The globule size for the lead CBD formulations (NE and NMC) ranged between 205 and 270 nm while CBD-VHS-NMC formulation had a particle size of about 78 nm. The sterilized formulations, except for CBD-VHS-NMC at 40 °C, were stable for three months of storage (last time point tested). Release, in terms of CBD, in the in-vitro release/diffusion studies over 18 h, were faster from the CBD-VHS nanomicelles (38 %) compared to that from the CBD nanoemulsion (16 %) and nanomicelles (33 %). Transcorneal permeation studies revealed improvement in CBD permeability and flux with both formulations; however, a greater improvement was observed with the NMC formulation compared to the NE formulation. In conclusion, the nanoformulations prepared could serve as efficient topical ocular drug delivery platforms for CBD and its analog.


Subject(s)
Administration, Ophthalmic , Cannabidiol , Cornea , Drug Stability , Emulsions , Nanoparticles , Particle Size , Solubility , Cannabidiol/administration & dosage , Cannabidiol/chemistry , Cannabidiol/pharmacokinetics , Animals , Cornea/metabolism , Cornea/drug effects , Nanoparticles/chemistry , Rabbits , Micelles , Valine/analogs & derivatives , Valine/chemistry , Valine/administration & dosage , Valine/pharmacokinetics , Drug Liberation , Lipids/chemistry , Excipients/chemistry , Permeability , Chemistry, Pharmaceutical/methods , Drug Compounding/methods , Surface-Active Agents/chemistry , Ophthalmic Solutions/administration & dosage
17.
Indian J Ophthalmol ; 72(6): 896-901, 2024 Jun 01.
Article in English | MEDLINE | ID: mdl-38623708

ABSTRACT

PURPOSE: To analyze the medical management of primary open-angle glaucoma (POAG) and ocular hypertension (OHT) and the placement of fixed-drug combination drugs (FDC) in the treatment paradigm at a tertiary eye care center in South India. METHODS: Retrospective study (January 2011-December 2015) of newly diagnosed POAG and OHT patients (≥18 years) with ≥5 years follow-up. Primary outcome included percentage use of different antiglaucoma drugs (at initiation) and FDCs at the first, second, and third progression (sequencing). Secondary outcomes: Percentage discontinuation for different FDCs, efficacy parameters (decrease in intraocular pressure (IOP)/visual field), adverse events, and the median number of antiglaucoma medications (AGMs) after 5 years. RESULTS: Three hundred and seventy eyes (198 patients) were analyzed; 84% of them had POAG. Prostaglandin analogs (PGAs) were the most common (66.2%). FDCs were started in 48 eyes (12.9%), with brimonidine + timolol combination being the most common. FDC usage at subsequent modifications was 10.1%, 24.04%, and 30.0%. Beta-blockers and PGAs were the most frequently prescribed AGMs in our practice pattern, with ß-blockers being the most consistent one. CONCLUSION: This study is a fairly large study with a minimum of a 5-year follow-up of patients with POAG and OHT and gives insights into the treatment patterns, use of FDCs, and the need for multiple medications over time.


Subject(s)
Antihypertensive Agents , Glaucoma, Open-Angle , Intraocular Pressure , Tertiary Care Centers , Humans , Retrospective Studies , India/epidemiology , Intraocular Pressure/drug effects , Intraocular Pressure/physiology , Male , Antihypertensive Agents/administration & dosage , Female , Glaucoma, Open-Angle/drug therapy , Glaucoma, Open-Angle/physiopathology , Middle Aged , Tertiary Care Centers/statistics & numerical data , Follow-Up Studies , Drug Combinations , Ocular Hypertension/drug therapy , Ocular Hypertension/diagnosis , Aged , Adult , Ophthalmic Solutions/administration & dosage , Treatment Outcome , Dose-Response Relationship, Drug , Visual Fields/physiology , Drug Therapy, Combination
18.
AAPS PharmSciTech ; 25(5): 92, 2024 Apr 29.
Article in English | MEDLINE | ID: mdl-38684590

ABSTRACT

PURPOSE: Dry eye syndrome (DES), arising from various etiologic factors, leads to tear film instability and ocular surface damage. Given its anti-inflammatory effects, cyclosporine A (CsA) has been widely used as a short-term treatment option for DES. However, poor bioavailability and solubility of CsA in aqueous phase make the development of a cyclosporine A-based eye drop for ocular topical application a huge challenge. METHODS: In this study, a novel strategy for preparing cyclosporine A-loaded silk fibroin nanoemulsion gel (CsA NBGs) was proposed to address these barriers. Additionally, the rheological properties, ocular irritation potential, tear elimination kinetics, and pharmacodynamics based on a rabbit dry eye model were investigated for the prepared CsA NBGs. Furthermore, the transcorneal mechanism across the ocular barrier was also investigated. RESULTS: The pharmacodynamics and pharmacokinetics of CsA NBGs exhibited superior performance compared to cyclosporine eye drops, leading to a significant enhancement in the bioavailability of CsA NBGs. Furthermore, our investigation into the transcorneal mechanism of CsA NBGs revealed their ability to be absorbed by corneal epithelial cells via the paracellular pathway. CONCLUSION: The CsA NBG formulation exhibits promising potential for intraocular drug delivery, enabling safe, effective, and controlled administration of hydrophobic drugs into the eye. Moreover, it enhances drug retention within the ocular tissues and improves systemic bioavailability, thereby demonstrating significant clinical translational prospects.


Subject(s)
Biological Availability , Cyclosporine , Dry Eye Syndromes , Fibroins , Gels , Ophthalmic Solutions , Rabbits , Animals , Fibroins/chemistry , Cyclosporine/administration & dosage , Cyclosporine/pharmacokinetics , Cyclosporine/chemistry , Dry Eye Syndromes/drug therapy , Ophthalmic Solutions/administration & dosage , Drug Delivery Systems/methods , Administration, Ophthalmic , Solubility , Male , Emulsions/chemistry , Cornea/metabolism , Cornea/drug effects , Disease Models, Animal
19.
JAMA Ophthalmol ; 142(4): 337-343, 2024 Apr 01.
Article in English | MEDLINE | ID: mdl-38451509

ABSTRACT

Importance: Dry eye disease (DED) is a prevalent eye disorder. Cyclosporine is an effective immunomodulator that is widely used in DED; however, due to its highly hydrophobic nature, delivery of cyclosporine to the ocular surface is challenging. Objective: To evaluate the efficacy and safety of SHR8028, a water-free cyclosporine ophthalmic solution, 0.1%, compared with vehicle in Chinese participants with DED. Design, Setting, and Participants: This was a multicenter, double-blind, vehicle-controlled, phase 3 randomized clinical trial conducted from March 4, 2021, to July 22, 2022. Adult participants with moderate to severe DED were recruited from 12 hospitals in China. Study data were analyzed April 2, 2022, for the primary analysis. Interventions: Following a 14-day run-in period with an artificial tear, participants were randomly assigned (1:1) to receive water-free cyclosporine or vehicle (1 eye drop in each eye twice daily). After a 29-day treatment, participants of both groups were given the option to receive water-free cyclosporine for an additional 12 weeks for longer-term safety assessment. Main Outcomes and Measures: The primary end points were changes from baseline in total corneal fluorescein staining (tCFS) using the National Eye Institute scale and in dryness score on a visual analog scale at day 29. Results: A total of 206 participants (mean [SD] age, 47.8 [14.2] years; 185 female [90%]) were enrolled, with 103 each in the cyclosporine group and the vehicle group. At day 29, the cyclosporine group experienced improved tCFS compared with vehicle (change [Δ] = -1.8; 95% CI, -2.7 to -1.0; P < .001), with a tCFS score decrease from baseline of -4.8 in the cyclosporine group and -3.0 in the vehicle group. Dryness score decreased from baseline in both groups (-19.2 vs -15.4; Δ = -3.8; 95% CI, -9.2 to 1.6; P = .17). During the 29-day treatment, treatment-related adverse events were reported in 15 participants (14.6%) in the cyclosporine group and 11 participants (10.7%) in the vehicle group. Conclusions And Relevance: Results demonstrated superiority of a water-free cyclosporine, 0.1%, eye solution over vehicle in improving tCFS score at day 29 in Chinese participants with DED. However, dryness score (VAS) was not improved at day 29. Trial Registration: ClinicalTrials.gov Identifier: NCT05841043.


Subject(s)
Cyclosporine , Dry Eye Syndromes , Adult , Humans , Female , Middle Aged , Cyclosporine/therapeutic use , Double-Blind Method , Treatment Outcome , Fluorescein , Ophthalmic Solutions/administration & dosage , Lubricant Eye Drops/therapeutic use , Tears
20.
J Ocul Pharmacol Ther ; 40(4): 204-214, 2024 May.
Article in English | MEDLINE | ID: mdl-38527183

ABSTRACT

Background: Insulin and insulin-like growth factor (IGF)-1 receptors are present in ocular tissues such as corneal epithelium, keratocytes, and conjunctival cells. Insulin plays a crucial role in the growth, differentiation, and proliferation of corneal epithelial cells, as well as in wound healing processes in various tissues. Purpose: This review explores the potential role of topical insulin in the treatment of ocular surface diseases. Specifically, it examines its impact on corneal nerve regeneration, sub-basal plexus corneal nerves, and its application in conditions like corneal epithelial defects, dry eye disease, and diabetic keratopathy. Methods: The review analyzes studies conducted over the past decade that have investigated the use of topical insulin in ocular surface diseases. It focuses on indications, drug preparation methods, side effects, efficacy outcomes, and variations in insulin concentrations and dosages used. Results: While off-label use of topical insulin has shown promising results in refractory corneal epithelial defects, its efficacy in dry eye disease is yet to be demonstrated. Variations in concentrations, dilutions, and dosing guidelines have been reported. However, limited data on ocular penetration, ocular toxicity, and systemic side effects pose challenges to its widespread utility. Conclusion: This review synthesizes findings from ocular investigations on topical insulin to assess its potential applicability in treating ocular surface and corneal diseases. By highlighting indications, preparation methods, side effects, and efficacy outcomes, it aims to provide insights into the current status and future prospects of using topical insulin in ophthalmic practice.


Subject(s)
Dry Eye Syndromes , Insulin , Ophthalmic Solutions , Humans , Insulin/administration & dosage , Insulin/therapeutic use , Dry Eye Syndromes/drug therapy , Ophthalmic Solutions/administration & dosage , Ophthalmic Solutions/therapeutic use , Corneal Diseases/drug therapy , Animals , Administration, Ophthalmic , Administration, Topical , Cornea/drug effects , Cornea/metabolism
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