957
Views
24
CrossRef citations to date
0
Altmetric
Reviews

Ophthalmic preservatives: focus on polyquaternium-1

, MD, , PhD & , MD
Pages 1425-1438 | Published online: 09 Sep 2011

Bibliography

  • Freeman PD, Kahook MY. Preservatives in topical ophthalmic medications: historical and clinical perspectives. Exp Rev Ophthalmol 2009;4:59-64
  • Noecker R. Effects of common ophthalmic preservatives on ocular health. Adv Ther 2001;18:205-15
  • Yee RW. The effect of drop vehicle on the efficacy and side effects of topical glaucoma therapy: a review. Curr Opin Ophthalmol 2007;18:134-9
  • Kaur IP, Lal S, Rana C, Ocular preservatives: associated risks and newer options. Cutan Ocul Toxicol 2009;28:93-103
  • Epstein SP, Ahdoot M, Marcus E, Asbell PA. Comparative toxicity of preservatives on immortalized corneal and conjunctival epithelial cells. J Ocul Pharmacol Ther 2009;25:113-19
  • Baudouin C, Labbe A, Liang H, Preservatives in eyedrops: the good, the bad and the ugly. Prog Retin Eye Res 2010;29:312-34
  • Baudouin C. Side effects of antiglaucomatous drugs on the ocular surface. Curr Opin Ophthalmol 1996;7:80-6
  • Novack GD, Evans R. Commercially available ocular hypotensive products: preservative concentration, stability, storage, and in-life utilization. J Glaucoma 2001;10:483-6
  • Kahook MY. Travoprost Z ophthalmic solution with sofZia: clinical safety and efficacy. Exp Rev Ophthalmol 2007;2:363-8
  • Ammar DA, Noecker RJ, Kahook MY. Effects of benzalkonium chloride-preserved, polyquad-preserved, and sofZia-preserved topical glaucoma medications on human ocular epithelial cells. Adv Ther 2010;27:837-45
  • Whitson JT, Ochsner KI, Moster MR, The safety and intraocular pressure-lowering efficacy of brimonidine tartrate 0.15% preserved with polyquaternium-1. Ophthalmology 2006;113:1333-9
  • Kahook MY, Ammar DA. In vitro toxicity of topical ocular prostaglandin analogs and preservatives on corneal epithelial cells. J Ocul Pharmacol Ther 2010;26:259-63
  • Lucero JC. Inventor. Enhancement of benzalkonium chloride preservative activity in formulations containing an incompatible drug using amino acids having net positive charge. US5504113; 1995
  • Tripathi BJ, Tripathi RC, Kolli SP. Cytotoxicity of ophthalmic preservatives on human corneal epithelium. Lens Eye Toxic Res 1992;9:361-75
  • Codling CE, Hann AC, Maillard JY, Russell AD. An investigation into the antimicrobial mechanisms of action of two contact lens biocides using electron microscopy. Cont Lens Anterior Eye 2005;28:163-8
  • Codling CE, Jones BV, Mahenthiralingam E, Identification of genes involved in the susceptibility of Serratia marcescens to polyquaternium-1. J Antimicrob Chemother 2004;54:370-5
  • Codling CE, Maillard JY, Russell AD. Aspects of the antimicrobial mechanisms of action of a polyquaternium and an amidoamine. J Antimicrob Chemother 2003;51:1153-8
  • Katz LJ. Twelve-month evaluation of brimonidine-purite versus brimonidine in patients with glaucoma or ocular hypertension. J Glaucoma 2002;11:119-26
  • Yee RW, Norcom EG, Zhao XC. Comparison of the relative toxicity of travoprost 0.004% without benzalkonium chloride and latanoprost 0.005% in an immortalized human cornea epithelial cell culture system. Adv Ther 2006;23:511-19
  • Allergan. LUMIGAN® 0.01% and 0.03% (bimatoprost ophthalmic solution). Package Insert. Irvine, CA; 2001
  • Furuse M, Hirase T, Itoh M, Occludin: a novel integral membrane protein localizing at tight junctions. J Cell Biol 1993;123:1777-88
  • Furuse M, Fujita K, Hiiragi T, Claudin-1 and -2: novel integral membrane proteins localizing at tight junctions with no sequence similarity to occludin. J Cell Biol 1998;141:1539-50
  • Pauly A, Meloni M, Brignole-Baudouin F, Multiple endpoint analysis of the 3D-reconstituted corneal epithelium after treatment with benzalkonium chloride: early detection of toxic damage. Invest Ophthalmol Vis Sci 2009;50:1644-52
  • Ly LT, Cavanagh HD, Petroll WM. Confocal assessment of the effects of fourth-generation fluoroquinolones on the cornea. Eye Contact Lens 2006;32:161-5
  • Whitson JT, Cavanagh HD, Lakshman N, Petroll WM. Assessment of corneal epithelial integrity after acute exposure to ocular hypotensive agents preserved with and without benzalkonium chloride. Adv Ther 2006;23:663-71
  • Okabe K, Kimura H, Okabe J, Effect of benzalkonium chloride on transscleral drug delivery. Invest Ophthalmol Vis Sci 2005;46:703-8
  • Majumdar S, Hippalgaonkar K, Repka MA. Effect of chitosan, benzalkonium chloride and ethylenediaminetetraacetic acid on permeation of acyclovir across isolated rabbit cornea. Int J Pharm 2008;348:175-8
  • Podder SK, Moy KC, Lee VH. Improving the safety of topically applied timolol in the pigmented rabbit through manipulation of formulation composition. Exp Eye Res 1992;54:747-57
  • Baudouin C, de Lunardo C. Short-term comparative study of topical 2% carteolol with and without benzalkonium chloride in healthy volunteers. Br J Ophthalmol 1998;82:39-42
  • Easty DL, Nemeth-Wasmer G, Vounatsos JP, Comparison of a non-preserved 0.1% T-Gel eye gel (single dose unit) with a preserved 0.1% T-Gel eye gel (multidose) in ocular hypertension and glaucomatous patients. Br J Ophthalmol 2006;90:574-8
  • Uusitalo H, Kaarniranta K, Ropo A. Pharmacokinetics, efficacy and safety profiles of preserved and preservative-free tafluprost in healthy volunteers. Acta Ophthalmol Suppl (Oxf) 2008;242:7-13
  • Hamacher T, Airaksinen J, Saarela V, Efficacy and safety levels of preserved and preservative-free tafluprost are equivalent in patients with glaucoma or ocular hypertension: results from a pharmacodynamics analysis. Acta Ophthalmol Suppl (Oxf) 2008;242:14-19
  • Shedden A, Adamsons IA, Getson AJ, Comparison of the efficacy and tolerability of preservative-free and preservative-containing formulations of the dorzolamide/timolol fixed combination (COSOPT) in patients with elevated intraocular pressure in a randomized clinical trial. Graefes Arch Clin Exp Ophthalmol 2010;248:1757-64
  • Lewis RA, Katz GJ, Weiss MJ, Travoprost 0.004% with and without benzalkonium chloride: a comparison of safety and efficacy. J Glaucoma 2007;16:98-103
  • Gross RL, Peace JH, Smith SE, Duration of IOP reduction with travoprost BAK-free solution. J Glaucoma 2008;17:217-22
  • Stark RL. Inventor. This invention relates to the quaternary ammonium salt, alpha-4-[-tris (2-hydroxyethyl) ammonium chloride-2-butenyl] poly[1-dimethyl ammonium chloride-2-butenyl]-w-tris (2-hydroxyethyl) ammonium chloride, providing aqueous disinfecting solutions for contact lenses as well as a preservative for ocular solutions including contact lens treating solutions. 4407791; 1983
  • Siketu D, Nelm DS. Inventors. Preserved ophthalmic drug compositions containing polymeric quaternary ammonium compounds. 5603929; 1997
  • Gandolfi S, Paredes T, Goldberg I, Comparison of a travoprost BAK-free formulation preserved with polyquaternium-1 with BAK-preserved travoprost in ocular hypertension or open-angle glaucoma. Eur J Ophthalmol; 2011. doi 10.5301/ejo.5000001
  • Rosenthal RA, Buck SL, Henry CL, Schlech BA. Evaluation of the preserving efficacy of lubricant eye drops with a novel preservative system. J Ocul Pharmacol Ther 2006;22:440-8
  • US Pharmacopeia. Available from: http://www.pharmacopeia.cn/v29240/usp29nf24s0_c51.html
  • Ph.Eur. 2008. 5.1.3 Efficacy of Antimicrobial Preservation. In: European Pharmacopoeia, 6th ed. European Directorate for the Quality of Medicines & Healthcare (EDQM) Council of Europe, Strasbourg 2007
  • Rosenthal RA, Buck S, McAnally C, Antimicrobial comparison of a new multi-purpose disinfecting solution to a 3% hydrogen peroxide system. CLAO J 1999;25:213-17
  • Standardization ECf. European Standard EN ISO 14730:2000 E. In: Ophthalmic Optics-Contact lens care products – Antimicrobial preservative efficacy testing and guidance on determining discard date. Management Centre: rue de Stassart, 36 B-1050 Brussels
  • Rosenthal RA, Henry CL, Stone RP, Schlech BA. Anatomy of a regimen: consideration of multipurpose solutions during non-compliant use. Cont Lens Anterior Eye 2003;26:17-26
  • Zhu H, Ding A, Bandara M, Broad spectrum of antibacterial activity of a new multipurpose disinfecting solution. Eye Contact Lens 2007;33:278-83
  • Rosenthal RA, Dassanayake NL, Schlitzer RL, Biocide uptake in contact lenses and loss of fungicidal activity during storage of contact lenses. Eye Contact Lens 2006;32:262-6
  • Rosenthal RA, McDonald MM, Schlitzer RL, Loss of bactericidal activity from contact lens storage solutions. CLAO J 1997;23:57-62
  • Rosenthal RA, Bell WM, Abshire R. Disinfecting action of a new multi-purpose disinfection solution for contact lenses. Cont Lens Anterior Eye 1999;22:104-9
  • Chang DC, Grant GB, O'Donnell K, Multistate outbreak of Fusarium keratitis associated with use of a contact lens solution. JAMA 2006;296:953-63
  • Hong J, Bielory L. Allergy to ophthalmic preservatives. Curr Opin Allergy Clin Immunol 2009;9:447-53
  • Ventura MT, Di Corato R, Di Leo E, Eyedrop-induced allergy: clinical evaluation and diagnostic protocol. Immunopharmacol Immunotoxicol 2003;25:529-38
  • EMEA public statement on antimicrobial preservatives in ophthalmic preparations for human use. EMEA/622721/2009. London, UK
  • Perry HD, Donnenfeld ED. Issues in the use of preservative-free topicals. Manag Care 2003;12:39-41
  • Gasset AR. Benzalkonium chloride toxicity to the human cornea. Am J Ophthalmol 1977;84:169-71
  • Debbasch C, Brignole F, Pisella PJ, Quaternary ammoniums and other preservatives' contribution in oxidative stress and apoptosis on Chang conjunctival cells. Invest Ophthalmol Vis Sci 2001;42:642-52
  • Champeau E, Edelhauser H. Effect of ophthalmic preservatives on the ocular surface: conjunctival and corneal uptake and distribution of benzal- konium chloride and chlorhexidine digluconate. In: Holly F, Lamberts D, Mac Keen D. editors. The preocular tear film in health, disease, and contact lens wear. Lubbock, TX: 1998. p. 292-302
  • Cha SH, Lee JS, Oum BS, Kim CD. Corneal epithelial cellular dysfunction from benzalkonium chloride (BAC) in vitro. Clin Experiment Ophthalmol 2004;32:180-4
  • Burstein NL. Corneal cytotoxicity of topically applied drugs, vehicles and preservatives. Surv Ophthalmol 1980;25:15-30
  • Eleftheriadis H, Cheong M, Sandeman S, Corneal toxicity secondary to inadvertent use of benzalkonium chloride preserved viscoelastic material in cataract surgery. Br J Ophthalmol 2002;86:299-305
  • Chou A, Hori S, Takase M. Ocular toxicity of beta-blockers and benzalkonium chloride in pigmented rabbits: electrophysiological and morphological studies. Jpn J Ophthalmol 1985;29:13-23
  • de Saint Jean M, Debbasch C, Brignole F, Toxicity of preserved and unpreserved beta-blocker eyedrops in an in vitro model of human conjunctival cells. J Fr Ophtalmol 2000;23:111-21
  • Fraunfelder FW. Corneal toxicity from topical ocular and systemic medications. Cornea 2006;25:1133-8
  • Epstein SP, Chen D, Asbell PA. Evaluation of biomarkers of inflammation in response to benzalkonium chloride on corneal and conjunctival epithelial cells. J Ocul Pharmacol Ther 2009;25:415-24
  • Monti D, Chetoni P, Burgalassi S, Increased corneal hydration induced by potential ocular penetration enhancers: assessment by differential scanning calorimetry (DSC) and by desiccation. Int J Pharm 2002;232:139-47
  • McCarey B, Edelhauser H. In vivo corneal epithelial permeability following treatment with prostaglandin analogs [correction of analoges] with or without benzalkonium chloride. J Ocul Pharmacol Ther 2007;23:445-51
  • Ayaki M, Iwasawa A, Inoue Y. Toxicity of antiglaucoma drugs with and without benzalkonium chloride to cultured human corneal endothelial cells. Clin Ophthalmol 2010;4:1217-22
  • Kahook MY, Noecker R. Quantitative analysis of conjunctival goblet cells after chronic application of topical drops. Adv Ther 2008;25:743-51
  • Noecker RJ, Herrygers LA, Anwaruddin R. Corneal and conjunctival changes caused by commonly used glaucoma medications. Cornea 2004;23:490-6
  • Pham XT, Huff JW. Cytotoxicity evaluation of multipurpose contact lens solutions using an in vitro test battery. CLAO J 1999;25:28-35
  • Meloni M, Pauly A, Servi BD, Occludin gene expression as an early in vitro sign for mild eye irritation assessment. Toxicol In Vitro 2010;24:276-85
  • Lopez Barnal D, Ubels JL. Quantitative evaluation of the corneal epithelial barrier: effect of artificial tears and preservatives. Curr Eye Res 1991;10:645-56
  • Labbe A, Pauly A, Liang H, Comparison of toxicological profiles of benzalkonium chloride and polyquaternium-1: an experimental study. J Ocul Pharmacol Ther 2006;22:267-78
  • Ubels JL, McCartney MD, Lantz WK, Effects of preservative-free artificial tear solutions on corneal epithelial structure and function. Arch Ophthalmol 1995;113:371-8
  • Brignole-Baudouin F, Riancho L, Liang H, Baudouin C. Comparative toxicology study of travoprost BAK-free, travoprost BAK-preserved, and latanoprost BAK-preserved ophthalmic solutions: an in vitro study on human conjunctival epithelial cells. Curr Eye Res In press
  • Liang H, Brignole-Baudouin F, Riancho L, Baudouin C. Minimal ocular surface toxicity associated with travoprost BAK-free versus travoprost and latanoprost BAK-preserved ophthalmic solutions in vivo. Ophthal Res Submitted
  • Brignole-Baudouin F, Riancho L, Liang H, Nakib Z, In vitro comparative toxicology of polyquad-preserved and benzalkonium chloride-preserved travoprost/timolol fixed combination and latanoprost/timolol fixed combination. J Ocul Pharmacol Ther 2011;27:273-80
  • Liang H, Brignole-Baudouin F, Pauly A, Polyquad-preserved travoprost/timolol, benzalkonium chloride (BAK)-preserved travoprost/timolol, and latanoprost/timolol in fixed combinations: a rabbit ocular surface study. Adv Ther 2011;28:311-25
  • Henry JC, Peace JH, Stewart JA, Stewart WC. Efficacy, safety, and improved tolerability of travoprost BAK-free ophthalmic solution compared with prior prostaglandin therapy. Clin Ophthalmol 2008;2:613-21
  • Katz G, Springs CL, Craven ER, Montecchi-Palmer M. Ocular surface disease in patients with glaucoma or ocular hypertension treated with either BAK-preserved latanoprost or BAK-free travoprost. Clin Ophthalmol 2010;4:1253-61
  • Horsley MB, Kahook MY. Effects of prostaglandin analog therapy on the ocular surface of glaucoma patients. Clin Ophthalmol 2009;3:291-5
  • Whitson JT, Trattler WB, Matossian C, Ocular surface tolerability of prostaglandin analogs in patients with glaucoma or ocular hypertension. J Ocul Pharmacol Ther 2010;26:287-92
  • Hall JQ Jr, Paugh JR, Peinovich MC, A pilot study of the effect of silicone-hydrogel lenses and marketed multipurpose solutions on human epithelial barrier function. Invest Ophthalmol Vis Sci 2007;48:E-Abstract 5400
  • Webb JR, Paugh JR, Ramsey AC, Meadows D. Clinical and epithelial barrier function evidence of lens material and care solution bio-incompatibilities. Invest Ophthalmol Vis Sci 2008;49:E-Abstract 2019
  • Dassanayake NL, Garofalo R, Carey C, Correlating biocide uptake and release profiles with corneal staining and subjective symptoms. Invest Ophthalmol Vis Sci 2005;46:E-Abstract 915
  • Epstein AB. Contact lens care products effect on corneal sensitivity and patient comfort. Eye Contact Lens 2006;32:128-32
  • Gibbs DE, Stein JM, Rockett J, Opti-Free chemical disinfectant: a safety study with various soft contact lenses. CLAO J 1989;15:57-60
  • Morgan JF, Perry DL, Stein JM, Randeri KJ. The margin of safety of polyquaternium-1 preserved lens care solutions: a phase I clinical study. CLAO J 1988;14:76-80
  • Lipener C. A randomized clinical comparison of OPTI-FREE EXPRESS and. ReNu MultiPLUS multipurpose lens care solutions. Adv Ther 2009;26:435-46
  • Jones L, MacDougall N, Sorbara LG. Asymptomatic corneal staining associated with the use of balafilcon silicone-hydrogel contact lenses disinfected with a polyaminopropyl biguanide-preserved care regimen. Optom Vis Sci 2002;79:753-61
  • Situ P, Simpson TL, Jones LW, Fonn D. Effects of silicone hydrogel contact lens wear on ocular surface sensitivity to tactile, pneumatic mechanical and chemical stimulation. Invest Ophthalmol Vis Sci 2010; doi.iovs.09-4807 [pii]10.1167/iovs.09-4807
  • Young G, Keir N, Hunt C, Woods CA. Clinical evaluation of long-term users of two contact lens care preservative systems. Eye Contact Lens 2009;35:50-8
  • Zigler L, Cedrone R, Evans D, Clinical evaluation of silicone hydrogel lens wear with a new multipurpose disinfection care product. Eye Contact Lens 2007;33:236-43
  • Santodomingo-Rubido J. The comparative clinical performance of a new polyhexamethylene biguanide- vs a polyquad-based contact lens care regime with two silicone hydrogel contact lenses. Ophthalmic Physiol Opt 2007;27:168-73
  • Gayton JL. Etiology, prevalence, and treatment of dry eye disease. Clin Ophthalmol 2009;3:405-12
  • Christensen MT. Corneal staining reductions observed after treatment with Systane Lubricant Eye Drops. Adv Ther 2008;25:1191-9
  • Mocanu C, Barascu D, Birjovanu F, Assessment of systane in severe dry eye. Oftalmologia 2008;52:105-10
  • Hartstein I, Khwarg S, Przydryga J. An open-label evaluation of HP-Guar gellable lubricant eye drops for the improvement of dry eye signs and symptoms in a moderate dry eye adult population. Curr Med Res Opin 2005;21:255-60
  • Rolando M, Autori S, Badino F, Barabino S. Protecting the ocular surface and improving the quality of life of dry eye patients: a study of the efficacy of an HP-guar containing ocular lubricant in a population of dry eye patients. J Ocul Pharmacol Ther 2009;25:271-8
  • De Saint Jean M, Brignole F, Bringuier AF, Effects of benzalkonium chloride on growth and survival of Chang conjunctival cells. Invest Ophthalmol Vis Sci 1999;40:619-30
  • Leung EW, Medeiros FA, Weinreb RN. Prevalence of ocular surface disease in glaucoma patients. J Glaucoma 2008;17:350-5
  • Rossi GC, Tinelli C, Pasinetti GM, Dry eye syndrome-related quality of life in glaucoma patients. Eur J Ophthalmol 2009;19:572-9
  • Pisella PJ, Pouliquen P, Baudouin C. Prevalence of ocular symptoms and signs with preserved and preservative free glaucoma medication. Br J Ophthalmol 2002;86:418-23
  • Nordmann JP, Auzanneau N, Ricard S, Berdeaux G. Vision related quality of life and topical glaucoma treatment side effects. Health Qual Life Outcomes 2003;1:75
  • Broadway DC, Grierson I, O'Brien C, Hitchings RA. Adverse effects of topical antiglaucoma medication. II. The outcome of filtration surgery. Arch Ophthalmol 1994;112:1446-54
  • Guzey M, Satici A, Karaman SK, The effect of lubricating eye drop containing hydroxypropyl guar on perimetry results of patients with glaucoma and trachomatous dry eye. Ophthalmologica 2010;224:109-15
  • Schmier JK, Lau EC, Covert DW. Two-year treatment patterns and costs in glaucoma patients initiating treatment with prostaglandin analogs. Clin Ophthalmol 2010;4:1137-43
  • Friedman DS, Hahn SR, Gelb L, Doctor-patient communication, health-related beliefs, and adherence in glaucoma results from the Glaucoma Adherence and Persistency Study. Ophthalmology 2008;115:1320-7; 7 e1-3

Reprints and Corporate Permissions

Please note: Selecting permissions does not provide access to the full text of the article, please see our help page How do I view content?

To request a reprint or corporate permissions for this article, please click on the relevant link below:

Academic Permissions

Please note: Selecting permissions does not provide access to the full text of the article, please see our help page How do I view content?

Obtain permissions instantly via Rightslink by clicking on the button below:

If you are unable to obtain permissions via Rightslink, please complete and submit this Permissions form. For more information, please visit our Permissions help page.