Increased corneal permeability induced by the dual effects of transient tear film acidification and exposure to benzalkonium chloride

Keller, Nicole; Moore, Dennis; Carper, Deborah; Longwell, Anna

doi:10.1016/0014-4835(80)90114-1

Cited by 59 publications

(17 citation statements)

References 7 publications

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“…The barrier offered to the diffusion of lipophobic solutes by the corneal epithelium can be reduced five or ten times in a controlled manner by treatment of the surface of the eye with water (MAURICE 1955), nonionic detergents (MARSH and MAURICE 1971), or acidic drops (KELLER et al 1980). The endothelial permeability has been reported to rise two to three times on mild trauma (MAURICE 1951(MAURICE , 1955, and the fluorescein permeability was found to be more than doubled 7 days after surgery in patients who had been operated on for cataract .…”

Section: Permeabilitymentioning

confidence: 97%

Ocular Pharmacokinetics

Maurice¹,

Mishima²

1984

Handbook of Experimental Pharmacology

222

169

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Section: Permeabilitymentioning

confidence: 97%

Ocular Pharmacokinetics

Maurice¹,

Mishima²

1984

Handbook of Experimental Pharmacology

222

169

View full text Add to dashboard Cite

“…In contrast, 0.01% BAK failed to increase the corneal permeability of inulin. 15 Similarly 0.01% BAK did not alter the corneal permeability of fluorescein in humans in vivo. Additionally, three repeated administrations (50 µL each) of 0.01% BAK/0.1% EDTA with 2 min intervals failed to increase the corneal permeability, but five repeated administrations of this solution did increase the corneal permeability in humans in vivo.…”

Section: Figure 1seffectmentioning

confidence: 99%

Effect of Benzalkonium Chloride/EDTA on the Ocular Bioavailability of Ketorolac Tromethamine following Ocular Instillation to Normal and De-epithelialized Corneas of Rabbits

Madhu¹,

Rix²,

Shackleton³

et al. 1996

Journal of Pharmaceutical Sciences

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This study was designed to examine the effect of benzalkonium chloride/ethylenediaminetetraacetic acid (BAK/EDTA) on the ocular bioavailability (Focular) of ketorolac tromethamine after ocular instillation to normal and de-epithelialized corneas of rabbits both in vitro and in vivo. The in vitro Focular of the formulations was measured in flow-through perfusion chambers. For in vivo studies, a 35 microL dose of 0.5% ketorolac tromethamine with or without BAK/EDTA was instilled into rabbit eyes with intact or de-epithelialized corneas. At 0.5, 1, 2, 4, 6, and 8 h postdose, rabbits were euthanized, and the corneas and aqueous humor were collected from both eyes. The ketorolac concentrations from both in vivo and in vitro samples were quantified by reversed-phase high-performance liquid chromatography. The in vitro study results indicated that BAK/EDTA statistically significantly increased the Focular of ketorolac through de-epithelialized corneas but not through intact corneas. The in vivo study results showed that BAK/EDTA had no effect on the Focular of ketorolac in rabbits with intact corneas, based on the values of the area under the aqueous humor concentration versus time curves (AUC0-6h) of ketorolac. As expected, de-epithelialization of the corneas produced a faster and greater ocular absorption of ketorolac as evidenced by the smaller Tmax and larger AUC values compared to those for the intact corneas in vivo. However, BAK/EDTA decreased the ocular absorption of ketorolac in rabbits with de-epithelialized corneas. The half-lives (t 1/2) of ketorolac in corneal tissue and aqueous humor were longer in rabbits with intact corneas than those in rabbits with de-epithelialized corneas. In conclusion, the in vivo Focular of ketorolac was not altered by BAK/EDTA in rabbits with intact corneas, but it was decreased by BAK/EDTA in rabbits with de-epithelialized corneas. Therefore, the formulation with ketorolac alone may be better as a post-operative ocular analgesic.

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“…Vyas et al (14) reported that there was approximately a 2.5 times increase in the ocular bioavailability of timolol maleate (a water soluble drug) encapsulated in niosomes as compared to timolol maleate solution. An increased ocular bioavailability of water-soluble drugs, entrapped in niosomes, may be due to the fact that surfactants act as penetration enhancers by removing the mucus layer and breaking junctional complexes (15)(16)(17)(18).…”

Section: Introductionmentioning

confidence: 99%

Niosome-Encapsulated Gentamicin for Ophthalmic Controlled Delivery

2008

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Abstract. The objective of the present research was to investigate the feasibility of using non-ionic surfactant vesicles (niosomes) as carriers for the ophthalmic controlled delivery of a water soluble local antibiotic; gentamicin sulphate. Niosomal formulations were prepared using various surfactants (Tween 60, Tween 80 or Brij 35), in the presence of cholesterol and a negative charge inducer dicetyl phosphate (DCP) in different molar ratios and by employing a thin film hydration technique. The ability of these vesicles to entrap the studied drug was evaluated by determining the entrapment efficiency %EE after centrifugation and separation of the formed vesicles. Photomicroscopy and transmission electron microscopy as well as particle size analysis were used to study the formation, morphology and size of the drug loaded niosomes. Results showed a substantial change in the release rate and an alteration in the %EE of gentamicin sulphate from niosomal formulations upon varying type of surfactant, cholesterol content and presence or absence of DCP. In-vitro drug release results confirmed that niosomal formulations have exhibited a high retention of gentamicin sulphate inside the vesicles such that their in vitro release was slower compared to the drug solution. A preparation with 1:1:0.1 molar ratio of Tween 60, cholesterol and DCP gave the most advantageous entrapment (92.02%±1.43) and release results (Q 8h =66.29%±1.33) as compared to other compositions. Ocular irritancy test performed on albino rabbits, showed no sign of irritation for all tested niosomal formulations.

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Increased corneal permeability induced by the dual effects of transient tear film acidification and exposure to benzalkonium chloride

Cited by 59 publications

References 7 publications

Ocular Pharmacokinetics

Ocular Pharmacokinetics

Effect of Benzalkonium Chloride/EDTA on the Ocular Bioavailability of Ketorolac Tromethamine following Ocular Instillation to Normal and De-epithelialized Corneas of Rabbits

Niosome-Encapsulated Gentamicin for Ophthalmic Controlled Delivery

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