ArticleInvestigative ophthalmology & visual science2011
Sclera-choroid-RPE transport of eight β-blockers in human, bovine, porcine, rabbit, and rat models.
Article in Investigative ophthalmology & visual science, 2011. The graph could read no effect estimate from its abstract, so it casts no vote on the map. It has been retracted, and should not be counted. Cited by 17 papers.
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The abstract states no effect estimate the extractor could read, or names no intervention and outcome on the map, so this paper lights no cell and moves no belief. It is still indexed, cited and linked below.
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Who cites it
17 citing papers in PubMed, 32 citations in OpenAlex.
- Intraocular reflectance of the ocular fundus and its impact on increased retinal hazard.Zeitschrift fur medizinische Physik · 2022Article
- Permeability of the Retina and RPE-Choroid-Sclera to Three Ophthalmic Drugs and the Associated Factors.Pharmaceutics · 2021Article
- Location and pressure dependent transmission of human and porcine sclera: an anterior to posterior examination.Graefe's archive for clinical and experimental ophthalmology = Albrecht von Graefes Archiv fur klinische und experimentelle Ophthalmologie · 2017Article
- Topical Ocular Drug Delivery to the Back of the Eye by Mucus-Penetrating Particles.Translational vision science & technology · 2015Article
- Prediction of passive drug permeability across the blood-retinal barrier.Pharmaceutical research · 2014Article
- Drug and gene delivery to the back of the eye: from bench to bedside.Investigative ophthalmology & visual science · 2014Review
- Nanomedicines for back of the eye drug delivery, gene delivery, and imaging.Progress in retinal and eye research · 2013Review
- Hypoxia alters ocular drug transporter expression and activity in rat and calf models: implications for drug delivery.Molecular pharmaceutics · 2013Article
- Immunohistochemical and functional characterization of peptide, organic cation, neutral and basic amino acid, and monocarboxylate drug transporters in human ocular tissues.Drug metabolism and disposition: the biological fate of chemicals · 2013Article
- Suprachoroidal delivery in a rabbit ex vivo eye model: influence of drug properties, regional differences in delivery, and comparison with intravitreal and intracameral routes.Molecular vision · 2013Article
- Pigmented-MDCK (P-MDCK) cell line with tunable melanin expression: an in vitro model for the outer blood-retinal barrier.Molecular pharmaceutics · 2012Article
- Transporter targeted gatifloxacin prodrugs: synthesis, permeability, and topical ocular delivery.Molecular pharmaceutics · 2012Article
- MRI study of subconjunctival and intravitreal injections.Journal of pharmaceutical sciences · 2012Article
- Intraocular distribution of melanin in human, monkey, rabbit, minipig and dog eyes.Experimental eye research · 2012Article
- Ocular drug delivery for glaucoma management.Pharmaceutics · 2012Article
- Hydrophilic prodrug approach for reduced pigment binding and enhanced transscleral retinal delivery of celecoxib.Molecular pharmaceutics · 2012Article
- Influence of drug solubility and lipophilicity on transscleral retinal delivery of six corticosteroids.Drug metabolism and disposition: the biological fate of chemicals · 2011Article
Corrections and comments
- Retraction · 2015-03-01Concerns/Issues about Data · Falsification/Fabrication of Data · Investigation by Company/Institution · Misconduct by Author · Unreliable Data ·
- Commented on by
- Retracted
Authors and funding
4 authors at 2 institutions in 1 country.
Funding
Abstract
purposeTo determine the influence of drug lipophilicity, ocular pigmentation, and species differences on transscleral solute transport.
methodsThe transport of eight β-blockers across excised sclera/sclera-choroid-RPE (SCRPE) of albino rabbit, pigmented rabbit, human, porcine, and bovine eyes was determined over 6 hours. The ex vivo transscleral β-blocker transport to the vitreous at the end of 6 hours was determined in euthanatized, pigmented Brown Norway rats. The thicknesses of the sclera and SCRPE and the melanin content in choroid-RPE (CRPE) were measured to determine whether species differences in drug transport can be explained on this basis.
resultsSolute lipophilicity inversely correlated with the SCRPE cumulative percentage of transport in all species (R(2) ≥ 0.80). The CRPE impeded the SCRPE transport of all β-blockers (51%-64% resistance in the rabbits; 84%-99.8% in the bovine and porcine eyes) more than the sclera, with the impedance increasing with lipophilicity. SCRPE transport followed the trend albino rabbit > pigmented rabbit > human > porcine > bovine, and a cross-species comparison showed good Spearman's rho correlation (R(2) ≥ 0.85). Bovine (R(2) = 0.84), porcine (R(2) = 0.84), and human (R(2) = 0.71) SCRPE transport was more predictive than that in the rabbit models (R(2) = 0.60-0.61) of transscleral solute transport to the vitreous in rats. The CRPE concentrations were higher in pigmented rabbits than in albino rabbits. The melanin content of the CRPE exhibited the trend albino rabbit ≪ pigmented rabbit < porcine ∼ bovine < rat. Normalization to scleral thickness abolished the species differences in scleral transport. Normalization to SCRPE thickness and melanin content significantly reduced species differences in SCRPE transport.
conclusionsOwing to the presence of pigment and drug binding, choroid-RPE is the principal barrier to transscleral β-blocker transport, with the barrier being more significant for lipophilic β-blockers. Although different in magnitude between species, sclera/SCRPE transport can be correlated between species. Tissue thickness accounts for the species differences in scleral transport. Differences in tissue thickness and melanin content largely account for the species differences in SCRPE transport.
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Registered trials
Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.