Bioavailability of fluorescein from a new drug delivery system in human eyes

Steinfeld, A.

doi:10.1136/bjo.88.1.48

Cited by 15 publications

(9 citation statements)

References 23 publications

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“…The fluorescent dye test is one of the most prevalent methods used in preclinical animal tests. Increase of the remnant dye in the eyeball indicates an increase of corneal permeability and damage (1 , 37 , 38) . Therefore, the protective effect of PEP-1-FK506BP on dry eye injury was examined with corneal fluorescein staining.…”

Section: Resutls and Dicsussionmentioning

confidence: 99%

The effects of PEP-1-FK506BP on dry eye disease in a rat model

Kim¹,

Lee²,

Ku³

et al. 2015

BMB Reports

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As FK506 binding proteins (FK506BPs) are known to play an important role in the regulation of a variety of biological processes related to cell survival, this study was designed to examined the protective effects of FK506 binding protein 12 (FK506BP) on low humidity air flow induced dry eye in a rat model using transduced PEP-1-FK506BP. After the topical application of PEP-1-FK506BP, tear volumes were markedly increased and significant prevention of cornea damage was observed compared with dry eye rats. Further, immunohistochemical analysis demonstrated that PEP-1-FK506BP markedly prevented damage to the cornea, the bulbar conjunctiva, and the palpebral conjunctiva epithelial lining compared with dry eye rats. In addition, caspase-3 and PARP expression levels were found to be decreased. These results demonstrated that topical application of PEP-1-FK506BP significantly ameliorates dry eye injury in an animal model. Thus, we suggest that PEP-1-FK506BP can be developed as a new ophthalmic drop to treat dry eye diseases. [BMB Reports 2015; 48(3): 153-158]

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Section: Resutls and Dicsussionmentioning

confidence: 99%

The effects of PEP-1-FK506BP on dry eye disease in a rat model

Kim¹,

Lee²,

Ku³

et al. 2015

BMB Reports

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“…As a measure for intraocular fluorescein concentration, the autofluorescence level was assessed in various anterior compartments. 9,10 Methods This study adhered to the tenets of the Declaration of Helsinki, was approved by the Medical Ethics Committee of the Erasmus Medical Center (Rotterdam, The Netherlands), and is registered on www.trialregister.nl (NTR3404). This study was designed as an open-label proof-of-principle trial for which 18 healthy volunteers (age >18) were recruited, all of whom provided written informed consent.…”

Section: Introductionmentioning

confidence: 99%

A New Spray Device to Deliver Topical Ocular Medication: Penetration of Fluorescein to the Anterior Segment

RooijJeroen

Wubbels

KruijfWilbur

2015

Journal of Ocular Pharmacology and Therapeutics

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“…33 Another prodrug in the market is levobunolol, which itself is active, as is its ocular metabolite, dihydrolevobunolol. 37 Another technology, which is currently in clinical trials, involves coating a plastic rod with the drug (e.g., fluorescein or clonidine). Loteprednol etabonate, an active "soft drug" (a drug specifically designed to produce targeted local activity, with prompt metabolic inactivation and consequently limited systemic exposure), is metabolized by ocular esterases to the inactive PJ-90 and PJ-91; it is currently marketed for the treatment of ocular inflammation and allergy.…”

Section: Translational Medicinementioning

confidence: 99%

“…In clinical studies, they found a greater fluorescein concentration in the anterior chamber with the use of the lyophilisate than with the use of eyedrops (Figure 2b). 37 Another technology, which is currently in clinical trials, involves coating a plastic rod with the drug (e.g., fluorescein or clonidine). 38,39 In the continuum between drops and implants, several agents have been formulated in erodible inserts designed to be placed in the lower cul-de-sac of the eye.…”

Section: Translational Medicinementioning

confidence: 99%

Ophthalmic Drug Delivery: Development and Regulatory Considerations

Novack

2009

Clin Pharmacol Ther

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This review presents an update on the development of ophthalmic drug delivery systems (Table 1), as well as regulatory aspects of product development. This review is based on full papers and published patents as of November 2008. PersPectiveLocal ocular delivery provides unique therapeutic opportunities and challenges. Drugs can be delivered directly to the anterior portions of the eye in relatively simple formulations, providing, de facto, an enhanced therapeutic index. The eye is an immuneprivileged site, 1 and can be visualized noninvasively. Given the low levels of most biotransformation enzymes, drug-drug interactions are typically not a major issue. 2 However, a recent article suggests a potentially important role for certain drug transports 3 that might be involved in drug-drug interactions. On the other hand, the posterior segment has numerous barriers to drug delivery. The eye is contained in the semi-rigid sclera, changes in eye volume result in potentially dangerous changes in intraocular pressure. Multiple sampling of target tissues is difficult, and therefore pharmacokinetic-pharmacodynamic interactions are rarely possible to understand. 2 There are many potential routes for local delivery of therapeutic molecules to the eye (as recently reviewed by Weiner, 4 Figure 1). The intravitreal route is now approved for two anti-vascular endothelial growth factor treatments for choroidal neovascularization caused by "wet" age-related macular degeneration (pegaptanib and ranibizumab) and also for corticosteroid treatments for intraocular inflammation (triamcinolone acetonide as Triescence and Trivaris). Sub-Tenon injections are under clinical investigation for delivering an ocular hypotensive agent (anecortave acetate). 5 In a landmark review a quarter century ago, Shell applied to ophthalmology the principles involved in improving pharmacotherapy: minimizing pulsatile drug concentrations and keeping tissue concentrations of the drugs at just above minimally effective levels but below toxic levels. 6 This approach resulted in the pilocarpine ocular therapeutic system (Ocusert, Figure 2a).In the same era, Kass used electronic monitors to determine the levels of compliance of patients with respect to glaucoma medications. He reported that patients missed 13-25% of prescribed doses, made timing errors, and had trouble instilling eyedrops. [7][8][9] There is a renewed interest in ophthalmic drug delivery systems due to (i) the availability of technical capacity to execute many of the early-stage ideas presented by Shell, 6 (ii) regulatory approval of three pharmacotherapies for the treatment of wet age-related macular degeneration, (iii) expanded understanding obtained through electronic monitoring studies showing that patient compliance is an issue, 10 (iv) renewed acknowledgment based that proper eyedrop instillation is challenging, 11,12 and (v) an increasing geriatric population at risk for degenerative eye disorders. OPhthalmic Drug DeliveryThe use of eyedrops is a relatively inefficient delivery system beca...

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Bioavailability of fluorescein from a new drug delivery system in human eyes

Cited by 15 publications

References 23 publications

The effects of PEP-1-FK506BP on dry eye disease in a rat model

The effects of PEP-1-FK506BP on dry eye disease in a rat model

A New Spray Device to Deliver Topical Ocular Medication: Penetration of Fluorescein to the Anterior Segment

Ophthalmic Drug Delivery: Development and Regulatory Considerations

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