scholarly journals An In Vitro Evaluation for Corneal Damages after Instillation of Eye Drops Using Rat Debrided Corneal Epithelium: Changes in Corneal Damage of Benzalkonium Chloride by Addition of Thickening Agent

2012 ◽  
Vol 132 (7) ◽  
pp. 837-843 ◽  
Author(s):  
Noriaki Nagai ◽  
Yoshimasa Ito ◽  
Norio Okamoto ◽  
Yoshikazu Shimomura
Keyword(s):  
Corneal Epithelium ◽  
Benzalkonium Chloride ◽  
Eye Drops ◽  
Thickening Agent ◽  
Corneal Damage

scholarly journals Kynurenic Acid Accelerates Healing of Corneal Epithelium In Vitro and In Vivo

2021 ◽  
Vol 14 (8) ◽  
pp. 753
Author(s):  
Anna Matysik-Woźniak ◽  
Waldemar A. Turski ◽  
Monika Turska ◽  
Roman Paduch ◽  
Mirosław Łańcut ◽  
...  
Keyword(s):  
Epithelial Cell ◽  
Corneal Epithelium ◽  
Kynurenic Acid ◽  
Pharmaceutical Products ◽  
Corneal Epithelial Cell ◽  
Eye Drops ◽  
Conjunctival Epithelium ◽  
Corneal Erosion

Kynurenic acid (KYNA) is an endogenous compound with a multidirectional effect. It possesses antiapoptotic, anti-inflammatory, and antioxidative properties that may be beneficial in the treatment of corneal injuries. Moreover, KYNA has been used successfully to improve the healing outcome of skin wounds. The aim of the present study is to evaluate the effects of KYNA on corneal and conjunctival cells in vitro and the re-epithelization of corneal erosion in rabbits in vivo. Normal human corneal epithelial cell (10.014 pRSV-T) and conjunctival epithelial cell (HC0597) lines were used. Cellular metabolism, cell viability, transwell migration, and the secretion of IL-1β, IL-6, and IL-10 were determined. In rabbits, after corneal de-epithelization, eye drops containing 0.002% and 1% KYNA were applied five times a day until full recovery. KYNA decreased metabolism but did not affect the proliferation of the corneal epithelium. It decreased both the metabolism and proliferation of conjunctival epithelium. KYNA enhanced the migration of corneal but not conjunctival epithelial cells. KYNA reduced the secretion of IL-1β and IL-6 from the corneal epithelium, leaving IL-10 secretion unaffected. The release of all studied cytokines from the conjunctival epithelium exposed to KYNA was unchanged. KYNA at higher concentration accelerated the healing of the corneal epithelium. These favorable properties of KYNA suggest that KYNA containing topical pharmaceutical products can be used in the treatment of ocular surface diseases.

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 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 Decrease in Corneal Damage due to Benzalkonium Chloride by the Addition of Mannitol into Timolol Maleate Eye Drops

2015 ◽  
Vol 64 (7) ◽  
pp. 743-750 ◽  
Author(s):  
Noriaki Nagai ◽  
Chiaki Yoshioka ◽  
Tadatoshi Tanino ◽  
Yoshimasa Ito ◽  
Norio Okamoto ◽  
...  
Keyword(s):  
Benzalkonium Chloride ◽  
Eye Drops ◽  
Timolol Maleate ◽  
Corneal Damage

scholarly journals Decrease in Corneal Damage due to Benzalkonium Chloride by the Addition of Sericin into Timolol Maleate Eye Drops

2013 ◽  
Vol 62 (3) ◽  
pp. 159-166 ◽  
Author(s):  
Noriaki Nagai ◽  
Yoshimasa Ito ◽  
Norio Okamoto ◽  
Yoshikazu Shimomura
Keyword(s):  
Benzalkonium Chloride ◽  
Eye Drops ◽  
Timolol Maleate ◽  
Corneal Damage

scholarly journals Comparison of cytotoxicity of fluoroquinolone antimicrobial eye drops and its effect on their bioavailability

2017 ◽  
Vol 10 (1) ◽  
pp. 77-86 ◽  
Author(s):  
Tamara S Hintuba ◽  
Yuri V Takhtaev ◽  
Igor N Okolov ◽  
Vera A Motyleva ◽  
Roman B Shlyakman
Keyword(s):  
Corneal Epithelium ◽  
Benzalkonium Chloride ◽  
High Yield ◽  
Eye Drops ◽  
Cytostatic Effect ◽  
Cytotoxic Potential ◽  
The Russian Federation ◽  
Chamber Fluid ◽  
Preservative Free

In addition to the breadth of activity of antibacterial medications as well as to their pharmacokinetic and pharmacodynamic properties, their safety and bioavailability represent an important aspect. Currently, there is no consensus on fluoroquinolone toxicity. The aim of the present study was to compare the total cytotoxic effect on corneal epithelium and bioavailability of three antibacterial fluoroquinolone eye drops, registered in the Russian Federation: 1) Oftaquix™ (levofloxacin 5 mg/ml; preservative benzalkonium chloride (BAC) 0.05 mg/ml; produced by Santen Oy, Finland), hereafter “levofloxacin (original)”; 2) Signicef® (levofloxacin 5 mg/ml; preservative BAC 0.1 mg/ml; produced by Sentiss Pharma Pvt. Ltd., India), hereafter “levofloxacin (generic)”; 3) Vigamox® (moxifloxacin® 5 mg/ml; preservative-free; produced by Alcon Laboratories, Inc., USA) hereafter “moxifloxacin” - using in vivo methods and determining the possible effect of preservative presence (in different concentration) or of its absence on reaching the minimal threshold concentrations of the antibiotic in the anterior chamber fluid, using the high-yield liquid chromatography combined with mass-spectrometric detection. The study showed that tested antibacterial medications could exert a cytostatic effect on the corneal epithelium at in vivo conditions and differ in their cytotoxic potential. Benzalkonium chloride presence in Signicef in a concentration twice as high than that of the main medication (Oftaquix) causes a proven by confocal microscopy effect on the corneal epithelium, and this may influence the bioavailability of the medication.

Effects of Benzalkonium Chloride on Pilocarpine-induced Opacity in Porcine Isolated Corneas

1993 ◽  
Vol 21 (3) ◽  
pp. 372-383
Author(s):  
Haruyoshi Igarashi ◽  
Yasunaga Katsuta ◽  
Kayoko Sawa ◽  
Yuu Chiba ◽  
Michio Kozima ◽  
...  
Keyword(s):  
Benzalkonium Chloride ◽  
High Performance ◽  
Physiological Saline ◽  
Experimental Period ◽  
Eye Drops ◽  
In Vitro Test ◽  
Endothelial Surface ◽  
Descemet's Membrane ◽  
Descemet’S Membrane

The incubation of isolated porcine corneas (intact, with the epithelium or endothelium plus Descemet's membrane removed, or with both the epithelium and endothelium plus Descemet's membrane removed) with solutions of pilocarpine HCl (5 X 10 4M or 5 x 10-3M) for four hours caused very little increase in opacity when compared with corneas incubated with physiological saline. However, at a higher concentration (5 x 10-2M), the application of pilocarpine to the endothelial surface, or to both the epithelial and endothelial surfaces of intact corneas, caused an obvious increase in opacity. The addition of the preservative benzalkonium chloride (BC; 0.005%) to pilocarpine solutions caused an increase in opacity, but in no circumstances did this appear to be other than an additive effect, since incubation with BC alone had an opacifying effect. This in vitro test confirms that pilocarpine is a safe drug for application as eye-drops. Studies using high performance liquid chromatography showed that BC increased the amount of pilocarpine passing through the cornea from the epithelial to the endothelial surface. A small amount of BC also passed through the cornea over the 4-hour experimental period.

Regeneration of the anterior corneal epithelium after transplantation of the limbic cell suspension in vitro on the model of the partial limbic insufficiency

2010 ◽  
Vol 27 (5) ◽  
pp. 61-65
Author(s):  
P. Bezdetko ◽  
◽  
E. Ilyina ◽  
O. Naumova ◽  
Yu. Mikulinskiy ◽  
...  
Keyword(s):  
Cell Suspension ◽  
Corneal Epithelium
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