Effect of the preservative benzalkonium chloride eye drops on the state of mitochondrial enzymes tissues of the anterior eye

2014 ◽  
Vol 50 (4) ◽  
pp. 80-87
Author(s):  
V Senishin ◽  
◽  
S Rafalyuk ◽  
Keyword(s):  
Benzalkonium Chloride ◽  
The State ◽  
Eye Drops ◽  
Mitochondrial Enzymes

scholarly journals Benzalkonium chloride corneal toxicity post-cataract surgery

2020 ◽  
Vol 17 (1) ◽  
pp. 56-60
Author(s):  
Keith Ong ◽  
Leonard Ong
Keyword(s):  
Cataract Surgery ◽  
Benzalkonium Chloride ◽  
Corneal Stroma ◽  
Eye Drops ◽  
Descemet's Membrane ◽  
Corneal Toxicity ◽  
Descemet’S Membrane ◽  
Free Steroid

Two patients with presumed benzalkonium chloride (BAK) corneal toxicity after routine cataract surgery are presented. Patient 1 had corneal stroma and Descemet’s membrane folds. Patient 2 had moderate superficial punctate epithelial erosions (SPEE). They were on Chlorsig, Maxidex, and Acular eye drops tds postoperatively. The corneas of these two patients improved when BAK was removed or minimized from the postoperative eye drop regimen. Two vials of 1 ml dexamethasone 4mg/ml for injection were added to Chlorsig 10 ml bottle to substitute for Maxidex eye drops. BAK toxicity should be suspected when the cornea is not as clear as expected postoperatively. A practical way to eliminate BAK from postoperative eye drops is described, and would be useful until pharmaceuticals mass-produce BAK-free steroid eye drops economically.

scholarly journals COMPARISON OF PRESERVATIVES EFFICACY OF BENZALKONIUM CHLORIDE, THIMEROSAL AND BENZYL ALCOHOL IN EYE DROP PRODUCTS CONTAINING CHLORAMPHENICOL

2020 ◽  
pp. 100-105
Author(s):  
SRI AGUNG FITRI KUSUMA ◽  
MARLINE ABDASSAH ◽  
FITASARY MARYATI
Keyword(s):  
Benzyl Alcohol ◽  
Benzalkonium Chloride ◽  
Room Temperature ◽  
Storage Time ◽  
Storage Period ◽  
Diffusion Method ◽  
Eye Drops ◽  
Inhibition Zones ◽  
In Vitro Stability

Objective: The aim of this study was to compare the preservative efficacy of benzalkonium chloride, thimerosal and benzyl alcohol in eye drops formulation containing chloramphenicol as the active agents for producing the sterile and effective eye drops.Methods: The efficacy of preservatives was assayed by evaluating the physical appearance, pH stability, sterility and the antibacterial effectivity of the formulated eye drops. Each of 0.5% chloramphenicol was formulated with different preservatives of benzalkonium chloride, thimerosal and benzyl alcohol at its recommended concentration, 0.01%; 0.01% and 1%, respectively. The in vitro stability was examined periodically for the eye drops formulation stored at room temperature during the 28-day period. The effectiveness of the antibacterial effect of chloramphenicol in eye drops was assayed by using the agar diffusion method against Escherichia coli and evaluated for the diameter of inhibition zones. Result: The clarity of the eye drops formula produced clear solutions. The eye drops formula exhibited relatively stabile on pH. All the formulated eye drops were sterile during the storage time. The appropriate of the sterilization method was thought to contribute to the sterility of eye drops which did not contain preservatives. In addition, it was assumed that the pre-reaction of chloramphenicol in inhibiting the contaminants in the eye drop may occur during the storage time. This hypothesis was confirmed by the inhibitory diameter stability produced by the eye drop formulas containing preservatives compared to that of not. The decrease in inhibition diameter occurred during the storage period (28 d) of each formula was as follows: F0 (51.58%), F1 (35.76%), F2 (31.86%), and F3 (35.35%). The best stability based on the antibacterial activity of the chloramphenicol eye drops was produced by F2 which used 0.01% thimerosal as its preservative. The differences in inhibition diameter were significantly influenced by the presence and the type of preservatives. Conclusion: 0.01% thimerosal indicated the best improvement on the efficacy of 0.5% chloramphenicol eye drop.

scholarly journals Comparative efficacy study of brimonidine tartrate 0.15% and timolol maleate 0.5% ophthalmic solution (benzalkonium chloride free) versus Brimolol® (with benzalkonium chloride) following single ocular instillation in New Zealand white rabbits

2020 ◽  
Vol 9 (7) ◽  
pp. 1050
Author(s):  
Amit Thavkar ◽  
Sateesh Kumar Chauhan ◽  
Subhas Bhowmick ◽  
Vinod Burade
Keyword(s):  
Intraocular Pressure ◽  
New Zealand ◽  
Repeated Measures ◽  
Benzalkonium Chloride ◽  
Ophthalmic Solution ◽  
Eye Drops ◽  
Timolol Maleate ◽  
Repeated Measures Analysis ◽  
Brimonidine Tartrate ◽  
Ophthalmic Solutions

Background: Benzalkonium chloride (BKC) is the most used preservative in topical eye drops but it causes effects such as dry eye and trabecular meshwork degeneration. Polyhexamethylene biguanide (PHMB) is a polymeric biguanide is a less harmful preservative used in ophthalmic solutions. The objective of this study to com-pare the efficacy of PHMB preserved versus BKC preserved ophthalmic solutions containing brimonidine tartrate and timolol maleate on intraocular pressure (IOP) following single ocular instillation in New Zealand white (NZW) rabbits.Methods: This study was conducted on 12 normotensive male NZW rabbits (2.9-3.6 kg) between 6-9 months of age. Animals received single ocular instillation of 35 µl ophthalmic solution containing brimonidine tartrate 0.15 %w/v and timolol maleate 0.5% w/v with PHMB as preservative (n=6, test) or BKC as preservative (n=6, reference) as per the randomization. Intraocular pressure (IOP) was measured before and 2, 4, 6, 8 and 24 hours after instillation using a pneumatonometer. Percentage change in IOP from pre-instillation values were calculated. Changes in IOP were analysed using the repeated-measures analysis of variance followed by Bonferroni post-test.Results: Single ocular instillation of PHMB and BKC formulations show significant IOP reduction up to 6 hours as compared with baseline (p<0.05). Reduction in IOP was 35.8% and 32.0% at 2 hours with PHMB and BKC formulations respectively. No differences were observed between the test and reference groups for change in IOP from baseline.Conclusions: PHMB preserved brimonidine tartrate 0.15% w/v and timolol maleate 0.5% w/v ophthalmic solution was comparable to BKC preserved solution in normotensive NZW rabbits.

scholarly journals Benzalkonium Chloride-Preserved Anti-Glaucomatous Eye Drops and Their Effect on Human Conjunctival Goblet Cells in vitro

2021 ◽  
pp. 69-75
Author(s):  
Anne Hedengran ◽  
Xenia Begun ◽  
Olivia Müllertz ◽  
Zaynab Mouhammad ◽  
Rupali Vohra ◽  
...  
Keyword(s):  
Cell Viability ◽  
Cell Survival ◽  
Goblet Cell ◽  
Benzalkonium Chloride ◽  
Goblet Cells ◽  
Eye Drops ◽  
Dependent Manner ◽  
The Impact ◽  
Conjunctival Goblet Cells

<b><i>Introduction:</i></b> Most intraocular pressure (IOP)-lowering eye drops are preserved with benzalkonium chloride (BAK). This can increase side effects and decrease adherence. Particularly, damage to the mucin-producing conjunctival goblet cells may be an issue due to instability of the tear film. We aimed to investigate the effect of IOP-lowering eye drops preserved with BAK on cultured human conjunctival goblet cells. <b><i>Methods:</i></b> Eye drops Brimonidine Tartrate Teva (BT) with 0.005% BAK, Dorzolamide Stada (DS) with 0.0075% BAK, Optimol<sup>®</sup> (OP) with 0.01% BAK, and Latanoprost Teva (LT) with 0.02% BAK were included. Human primary cultured goblet cell survival was evaluated using a lactate dehydrogenase assay on human goblet cells after treatment for 30 min and 6 h with the different anti-glaucoma drug formulations. <b><i>Results:</i></b> All eye drops examined, except BT, reduced goblet cell survival. The impact of eye drops on goblet cell viability was correlated with the time of exposure as well as to the concentration of BAK. After 30 min of exposure, cell viability was 93% for BT (0.005% BAK; <i>p</i> = 0.93), 71% for DS (0.0075% BAK; <i>p</i> = 0.067), 70% for OP (0.01% BAK; <i>p</i> = 0.054), and 69% for LT (0.02% BAK; <i>p</i> = 0.022), and exposure for 6 h reduced cell survival to 74% for BT (<i>p</i> = 0.217), 52% for DS (<i>p</i> = 0.011), 34% for OP (<i>p</i> = 0.017), and 31% for LT (<i>p</i> = 0.0007). <b><i>Conclusion:</i></b> LT, OP, and DS reduced human goblet cell survival in a time-dependent manner. BT did not affect goblet cell survival. Cell survival was correlated with the BAK concentration in the eye drops making 0.02% BAK-preserved LT most toxic and 0.005% BAK-preserved BT least toxic. Based on the present study, decreasing BAK in eye drops for chronic use seems important to reduce damage to the goblet cells. However, future studies are needed to further explore this finding.

scholarly journals Effects of Eye Drops Containing Hyaluronic Acid-Nimesulide Conjugates in a Benzalkonium Chloride-Induced Experimental Dry Eye Rabbit Model

Pharmaceutics ◽  
2021 ◽  
Vol 13 (9) ◽  
pp. 1366
Author(s):  
Tzu-Yang Chen ◽  
Ching-Li Tseng ◽  
Chih-An Lin ◽  
Hua-Yang Lin ◽  
Parthiban Venkatesan ◽  
...  
Keyword(s):  
Hyaluronic Acid ◽  
Dry Eye ◽  
Goblet Cell ◽  
Corneal Epithelium ◽  
Benzalkonium Chloride ◽  
Immunofluorescent Staining ◽  
Prolonged Treatment ◽  
Eye Drops ◽  
Cell Recovery ◽  
Anti Inflammatory

Dry eye syndrome (DES) is a common ocular disease worldwide. Currently, anti-inflammatory agents and immunosuppressive drugs, such as cyclosporine A, have been widely used to treat this chronic condition. However, the multifactorial etiology of DES, poor tolerance, low bioavailability, and prolonged treatment to response time have limited their usage. In this study, nimesulide, a cyclooxygenase (COX)-2 selective inhibitor, was conjugated with hyaluronic acid (HA), and the HA-nimesulide conjugates were expected to increase the solubility and biocompatibility for alleviating the DES in the benzalkonium chloride (BAC)-induced goblet cell-loss dry eye model. The therapeutic efficacy of HA-nimesulide was assessed using fluorescein staining, goblet cell density by conjunctival impression cytology, and histology and immunohistochemistry of corneal tissues. Compared to commercial artificial tears and Restasis®, the HA-nimesulide conjugates could promote goblet cell recovery and enhance the regeneration of the corneal epithelium. Importantly, immunofluorescent staining studies demonstrated that the HA-nimesulide conjugates could decrease the number of infiltrating CD11b-positive cells after two weeks of topical application. In the anti-inflammatory test, the HA-nimesulide conjugates could inhibit the production of pro-inflammatory cytokines and prostaglandin E2 (PGE2) in the lipopolysaccharide (LPS)-stimulated Raw 264.7 cell model. In conclusion, we demonstrated that HA-nimesulide conjugates had anti-inflammatory activity, and promoted goblet cell recovery and corneal epithelium regeneration when used as topical eye drops; accordingly, the HA-nimesulide conjugates could potentially be effective for the treatment of DES.

scholarly journals Repeated Exposure to Benzalkonium Chloride in the Ex Vivo Eye Irritation Test (EVEIT): Observation of Isolated Corneal Damage and Healing

2008 ◽  
Vol 36 (1) ◽  
pp. 25-32 ◽  
Author(s):  
Markus Frentz ◽  
Miriam Goss ◽  
Martin Reim ◽  
Norbert F. Schrage
Keyword(s):  
Benzalkonium Chloride ◽  
Ex Vivo ◽  
Lactate Production ◽  
Eye Drops ◽  
Self Healing ◽  
Preclinical Testing ◽  
Eye Irritation ◽  
Dependent Inhibition ◽  
Irritation Test ◽  
To Come

The prediction of side-effects is a key issue in the REACH initiative on chemicals, in the production of cosmetics and in the preclinical testing of drugs. A new ex vivo test for repeated substance application is presented, that is able to identify corrosive and irritant effects on the eye by using crucial endpoints, such as cellular and morphological damage, and healing characteristics. The test is intended to replace the Draize eye test and to improve the preclinical testing of drugs and chemicals that are likely to come into direct contact with the cornea. The Ex Vivo Eye Irritation Test (EVEIT) is a self-healing system, involving living corneas obtained from abattoir rabbit eyes. The corneas are cultured in a similar way to the method used during the transplantation of corneal grafts. The corneas are exposed to multiple small, mechanical abrasions, and then test substances are repeatedly dropped onto the centres of the corneas. The test substances applied in this study were citrate-buffered hyaluronate eye drops and an artificial tear replacement, with increasing concentrations of up to 0.1% benzalkonium chloride. A dose-dependent inhibition of recovery and impairment of the lactate production mechanism in the cornea was observed with benzalkonium chloride treatment.

Sign in / Sign up

Export Citation Format

Share Document