The Cytotoxic Effects of Preserved and Preservative-Free Prostaglandin Analogs on Human Corneal and Conjunctival Epithelium<i>In Vitro</i>and the Distribution of Benzalkonium Chloride Homologs in Ocular Surface Tissues<i>In Vivo</i>

Pellinen, Pertti; Huhtala, Anne; Tolonen, Ari; Lokkila, Jukka; Mäenpää, J; Uusitalo, Hannu

doi:10.3109/02713683.2011.626909

Cited by 55 publications

(44 citation statements)

References 40 publications

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“…6 On the other hand, another report described that travoprost was slightly cytotoxic. 14 The results from these in vitro studies indicate that tafluprost has lower cytotoxicity than travoprost. Based on the results of the present study, we believe that switching from travoprost to tafluprost alleviated the toxicity against corneal epithelial cells, resulting in the decreased SPK scores.…”

Section: Discussionmentioning

confidence: 96%

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Comparison of Corneal Safety and Intraocular Pressure–Lowering Effect of Tafluprost Ophthalmic Solution with Other Prostaglandin Ophthalmic Solutions

Kumagami

Wakiyama

Kusano

et al. 2014

Journal of Ocular Pharmacology and Therapeutics

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Purpose: The benzalkonium chloride (BAK) content of tafluprost ophthalmic solution (Tapros Ò : tafluprost) has been reduced to balance corneal safety and preservative effectiveness (old formulation: 0.01%; new formulation: 0.001%). However, no reports have been published on its clinical effect. Therefore, we conducted a clinical research study to compare the safety of BAK-reduced tafluprost on the ocular surface with other prostaglandin ophthalmic solutions. Methods: This clinical study included 28 glaucoma patients (28 eyes) with a treatment history of latanoprost ophthalmic solution (Xalatan Ò ) or travoprost ophthalmic solution (Travatan Z Ò ), who presented with corneal epithelial disorders. The subjects were switched to BAK-reduced tafluprost, and its effect on the ocular surface was examined after 1 and 2 months of treatment [using fluorescein staining score, hyperemia, tear film breakup time, and intraocular pressure (IOP) lowering]. Results: In all analyzed subjects (N = 27), the fluorescein staining score was significantly improved after switching to BAK-reduced tafluprost (P < 0.0001). Conversely, the IOP-lowering effect was not notably changed. The subjects switched from latanoprost (n = 10) showed significant improvement in fluorescein staining score (P < 0.05) as well as in IOP lowering (P < 0.01). The subjects switched from travoprost (n = 17) also showed significant improvement in fluorescein staining score (P < 0.001), but without a significant change in IOP lowering. Conclusions: Tafluprost with reduced BAK has potential as a superior antiglaucoma drug, not only for its IOPlowering effect, but also for its good corneal safety profile.

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Section: Discussionmentioning

confidence: 96%

“…13 In addition, preservative-free prostaglandin ophthalmic solutions have been shown to exhibit very low cytotoxicity against corneal epithelial cells. 14 These findings suggest that the excipients, primarily preservatives, play a major role in the corneal epithelial disorders caused by prostaglandin ophthalmic solutions.…”

Section: Discussionmentioning

confidence: 96%

Comparison of Corneal Safety and Intraocular Pressure–Lowering Effect of Tafluprost Ophthalmic Solution with Other Prostaglandin Ophthalmic Solutions

Kumagami

Wakiyama

Kusano

et al. 2014

Journal of Ocular Pharmacology and Therapeutics

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“…This total score was recorded for each participant. The impact of dry eye was then assessed categorically as normal (scores of 0-12), mild (scores of [13][14][15][16][17][18][19][20][21][22], moderate (scores of [23][24][25][26][27][28][29][30][31][32], or severe (scores of 33-100), as previously described (17,24).…”

Section: Ocular Surface Disease Indexmentioning

confidence: 99%

Ocular Surface Disease in Patients under Topical Treatment for Glaucoma

Pérez-Bartolomé

Martínez-de-la-Casa

Arriola‐Villalobos

et al. 2017

European Journal of Ophthalmology

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ORIGINAL RESEARCH ARTICLE disease, conjunctivitis, and keratitis (3). Ocular surface disease is frequently observed in glaucoma patients and is thought to be the consequence of the chronic use of IOP-lowering eyedrops (4, 5). As a comorbidity of glaucoma, OSD has been held responsible for poor treatment adherence (6) and worsening of patient quality of life (6, 7). In treated glaucoma patients, abnormal tear film function has been detected using objective tests such as fluorescein corneal staining, tear film breakup time (TBUT), osmolarity, or meibomian gland score, although the severity of symptoms varies widely among studies (8-11). Both OSD and glaucoma are age-related diseases (7, 12), though individuals with glaucoma show a higher prevalence of OSD than do those without glaucoma (13). There is increasing evidence to suggest that the preservatives used in antiglaucoma medications may worsen the signs and symptoms of OSD. Benzalkonium chloride (BAK) is one of the first preservatives introduced and is currently the most widely used ophthalmic preservative. Several in vitro and animal studies have shown that solutions containing BAK cause corneal neurotoxicity, tear film disruption, and trabecular meshwork damage (14, 15). As a less harmful preservative,

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“…The structure of the liposome vesicles additionally provides a protective shield to the molecules of interest (Figure 1) against the degradation, biotransformation, or elimination, that “free” molecules may undergo (Allen and Cullis, 2004). Additionally, this formulation is predicted to reduce the cytotoxicity of drug molecules (Pleyer et al, 1995), a major limitation when topically administering drugs to the eye (Furrer et al, 2002, Pellinen et al, 2012, Kovoor et al, 2004). This liposomal formulation is both easy to prepare and reproducible for generating carriers that have consistent dimensions, charge, and a high peptide delivery efficiency.…”

Section: Introductionmentioning

confidence: 99%

Preparation and optimisation of anionic liposomes for delivery of small peptides and cDNA to human corneal epithelial cells

Neves

Duan

Voelker

et al. 2016

Journal of Microencapsulation

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Drug delivery to corneal epithelial cells is challenging due to the intrinsic mechanisms that protect the eye. Here we report a novel liposomal formulation to encapsulate and deliver a short sequence peptide into human corneal epithelial cells (hTCEpi). Using a mixture of Phosphatidylcholine/Caproylamine/Dioleoylphosphatidylethanolamine (PC/CAP/DOPE), we encapsulated a fluorescent peptide, resulting in anionic liposomes with an average size of 138.8 ± 34 nm and a charge of −18.2 ± 1.3 mV. After 2 h incubation with the peptide-encapsulated liposomes, 66% of corneal epithelial (hTCEpi) cells internalized the FITC-labelled peptide, demonstrating the ability of this formulation to effectively deliver peptide to hTCEpi cells. Additionally, lipoplexes (liposomes complexed with plasmid DNA) were also able to transfect hTCEpi cells, albeit at a modest level (8% of the cells). Here, we describe this novel anionic liposomal formulation intended to enhance the delivery of small cargo molecules in situ.

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The Cytotoxic Effects of Preserved and Preservative-Free Prostaglandin Analogs on Human Corneal and Conjunctival EpitheliumIn Vitroand the Distribution of Benzalkonium Chloride Homologs in Ocular Surface TissuesIn Vivo

Cited by 55 publications

References 40 publications

Comparison of Corneal Safety and Intraocular Pressure–Lowering Effect of Tafluprost Ophthalmic Solution with Other Prostaglandin Ophthalmic Solutions

Comparison of Corneal Safety and Intraocular Pressure–Lowering Effect of Tafluprost Ophthalmic Solution with Other Prostaglandin Ophthalmic Solutions

Ocular Surface Disease in Patients under Topical Treatment for Glaucoma

Preparation and optimisation of anionic liposomes for delivery of small peptides and cDNA to human corneal epithelial cells

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