ArticleDrug metabolism and disposition: the biological fate of chemicals2011
Influence of drug solubility and lipophilicity on transscleral retinal delivery of six corticosteroids.
Article in Drug metabolism and disposition: the biological fate of chemicals, 2011. The graph could read no effect estimate from its abstract, so it casts no vote on the map. It carries an expression of concern. Cited by 21 papers.
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Who cites it
21 citing papers in PubMed.
- Pharmacokinetic model for drug delivery by Ozurdex.Drug delivery and translational research · 2026Article
- Suprachoroidal injection of triamcinolone acetonide as adjuvant to surgical treatment of epiretinal membrane.International journal of retina and vitreous · 2025Article
- Fluocinolone Acetonide Implant for Uveitis: Dissecting Responder and Non-Responder Outcomes at a Tertiary Center.Biomedicines · 2024Article
- Corticosteroids in ophthalmology: drug delivery innovations, pharmacology, clinical applications, and future perspectives.Drug delivery and translational research · 2021Review
- Ion-Complex Microcrystal Formulation Provides Sustained Delivery of a Multimodal Kinase Inhibitor from the Subconjunctival Space for Protection of Retinal Ganglion Cells.Pharmaceutics · 2021Article
- Mucoadhesive Poloxamer-Based Hydrogels for the Release of HP-β-CD-Complexed Dexamethasone in the Treatment of Buccal Diseases.Pharmaceutics · 2021Article
- Polymeric micelles for the ocular delivery of triamcinolone acetonide: preparation andDrug delivery · 2020Article
- Sunitinib malate-loaded biodegradable microspheres for the prevention of corneal neovascularization in rats.Journal of controlled release : official journal of the Controlled Release Society · 2020Article
- Therapeutic implications of nanomedicine for ocular drug delivery.Drug discovery today · 2019Review
- Controlled release of corticosteroid with biodegradable nanoparticles for treating experimental autoimmune uveitis.Journal of controlled release : official journal of the Controlled Release Society · 2019Article
- The Potential of Fluocinolone Acetonide to Mitigate Inflammation and Lipid Accumulation in 2D and 3D Foam Cell Cultures.BioMed research international · 2018Article
- Characterization of liposomal carriers for the trans-scleral transport of Ranibizumab.Scientific reports · 2017Article
- Dexamethasone distribution characteristic following controllable continuous sub-tenon drug delivery in rabbit.Drug delivery · 2017Article
- Controllable continuous sub-tenon drug delivery of dexamethasone disodium phosphate to ocular posterior segment in rabbit.Drug delivery · 2017Article
- The effect of ocular pigmentation on transscleral delivery of triamcinolone acetonide.Journal of ocular pharmacology and therapeutics : the official journal of the Association for Ocular Pharmacology and Therapeutics · 2013Article
- Withaferin A effectively targets soluble vimentin in the glaucoma filtration surgical model of fibrosis.PloS one · 2013Article
- RETRACTED: Influence of choroidal neovascularization and biodegradable polymeric particle size on transscleral sustained delivery of triamcinolone acetonide.International journal of pharmaceutics · 2012Article
- Hydrophilic prodrug approach for reduced pigment binding and enhanced transscleral retinal delivery of celecoxib.Molecular pharmaceutics · 2012Article
- Brain mitochondrial drug delivery: influence of drug physicochemical properties.Pharmaceutical research · 2011Article
- Nanotechnology approaches for ocular drug delivery.Middle East African journal of ophthalmologyReview
Corrections and comments
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Authors and funding
3 authors.
Funding
Abstract
The influence of drug properties including solubility, lipophilicity, tissue partition coefficients, and in vitro transscleral permeability on ex vivo and in vivo transscleral delivery from corticosteroid suspensions was determined. Solubility, tissue/buffer partition coefficients for bovine sclera and choroid-retinal pigment epithelium (CRPE), and in vitro bovine sclera and sclera-choroid-retinal pigment epithelium (SCRPE) transscleral transport were determined at pH 7.4 for triamcinolone, prednisolone, dexamethasone, fluocinolone acetonide, triamcinolone acetonide, and budesonide in solution. Ex vivo and in vivo transscleral delivery was assessed in Brown Norway rats after posterior subconjunctival injection of a 1 mg/ml suspension of each corticosteroid. Corticosteroid solubility and partition coefficients ranged from ∼ 17 to 300 μg/ml and 3.0 to 11.4 for sclera and from 7.1 to 35.8 for CRPE, respectively, with the more lipophilic molecules partitioning more into both tissues. Transport across sclera and SCRPE was in the range of 3.9 to 10.7% and 0.3 to 1.8%, respectively, with the transport declining with an increase in lipophilicity. Ex vivo and in vivo transscleral delivery indicated tissue distribution in the order CRPE ≥ sclera > retina > vitreous. Tissue partitioning showed a positive correlation with drug lipophilicity (R(2) = 0.66-0.96). Ex vivo and in vivo sclera, CRPE, retina, and vitreous tissue levels of all corticosteroids showed strong positive correlation with drug solubility (R(2) = 0.91-1.0) but not lipophilicity (R(2) = 0.24-0.41) or tissue partitioning (R(2) = 0.24-0.46) when delivered as suspensions. In vivo delivery was lower in all eye tissues assessed than ex vivo delivery, with the in vivo/ex vivo ratios being the lowest in the vitreous (0.085-0.212). Upon exposure to corticosteroid suspensions ex vivo or in vivo, transscleral intraocular tissue distribution was primarily driven by the drug solubility.
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