ArticlePharmaceutical research2009
Transcorneal permeation of L- and D-aspartate ester prodrugs of acyclovir: delineation of passive diffusion versus transporter involvement.
Article in Pharmaceutical research, 2009. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 22 papers.
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Who cites it
22 citing papers in PubMed, 46 citations in OpenAlex.
- Overview of processed excipients in ocular drug delivery: Opportunities so far and bottlenecks.Heliyon · 2024Review
- In vivo degradation forms, anti-degradation strategies, and clinical applications of therapeutic peptides in non-infectious chronic diseases.European journal of pharmacology · 2022Review
- Ciprofloxacin self-dissolvable Soluplus based polymeric films: a novel proposal to improve the management of eye infections.Drug delivery and translational research · 2021Article
- Ex-Vivo Trans-Corneal and Trans-Scleral Diffusion Studies with Ocular Formulations of Glutathione as an Antioxidant Treatment for Ocular Diseases.Pharmaceutics · 2020Article
- Ocular Surface Disease and Glaucoma Medications: A Clinical Approach.Eye & contact lens · 2019Review
- Ex vivo rabbit cornea diffusion studies with a soluble insert of moxifloxacin.Drug delivery and translational research · 2018Article
- Diclofenac sodium ion exchange resin complex loaded melt cast films for sustained release ocular delivery.Drug delivery · 2017Article
- Development of a Δ9-Tetrahydrocannabinol Amino Acid-Dicarboxylate Prodrug With Improved Ocular Bioavailability.Investigative ophthalmology & visual science · 2017Article
- A comprehensive insight on ocular pharmacokinetics.Drug delivery and translational research · 2016Review
- Topical ophthalmic lipid nanoparticle formulations (SLN, NLC) of indomethacin for delivery to the posterior segment ocular tissues.European journal of pharmaceutics and biopharmaceutics : official journal of Arbeitsgemeinschaft fur Pharmazeutische Verfahrenstechnik e.V · 2016Article
- Prodrug approach to improve absorption of prednisolone.International journal of pharmaceutics · 2015Article
- Evaluation of topical hesperetin matrix film for back-of-the-eye delivery.European journal of pharmaceutics and biopharmaceutics : official journal of Arbeitsgemeinschaft fur Pharmazeutische Verfahrenstechnik e.V · 2015Article
- 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
- Prodrug strategies in ocular drug delivery.Medicinal chemistry (Shariqah (United Arab Emirates)) · 2012Review
- Effect of ion pairing on in vitro transcorneal permeability of a Δ(9) -tetrahydrocannabinol prodrug: potential in glaucoma therapy.Journal of pharmaceutical sciences · 2012Article
- Ocular drug delivery.The AAPS journal · 2010Review
- Evaluation of active and passive transport processes in corneas extracted from preserved rabbit eyes.Journal of pharmaceutical sciences · 2010Article
- Vitreal kinetics of quinidine in rabbits in the presence of topically coadministered P-glycoprotein substrates/modulators.Drug metabolism and disposition: the biological fate of chemicals · 2009Article
- Role of transporters in ocular drug delivery system.Pharmaceutical research · 2009Article
Corrections and comments
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Authors and funding
6 authors at 1 institution in 1 country.
Funding
Abstract
purposeThe aim of this study was to evaluate the contribution of amino acid transporters in the transcorneal permeation of the aspartate (Asp) ester acyclovir (ACV) prodrug.
methodsPhysicochemical characterization, solubility and stability of acyclovir L-aspartate (L-Asp-ACV) and acyclovir D-aspartate (D-Asp-ACV) were studied. Transcorneal permeability was evaluated across excised rabbit cornea.
resultsSolubility of L-Asp-ACV and D-Asp-ACV were about twofold higher than that of ACV. The prodrugs demonstrated greater stability under acidic conditions. Calculated pK(a) and logP values for both prodrugs were identical. Transcorneal permeability of L-Asp-ACV (12.1 +/- 1.48 x 10(-6) cm/s) was fourfold higher than D-Asp-ACV (3.12 +/- 0.36 x 10(-6) cm/s) and ACV (3.25 +/- 0.56 x 10(-6) cm/s). ACV generation during the transport process was minimal. L-Asp-ACV transport was sodium and energy dependent but was not inhibited by glutamic acid. Addition of BCH, a specific B(0,+) and L amino acid transporter inhibitor, decreased transcorneal L-Asp-ACV permeability to 2.66 +/- 0.21 x 10(-6) cm/s. L-Asp-ACV and D-Asp-ACV did not demonstrate significant difference in stability in ocular tissue homogenates.
conclusionThe results demonstrate that enhanced transport of L-Asp-ACV is as a result of corneal transporter involvement (probably amino acid transporter B(0,+)) and not as a result of changes in physicochemical properties due to prodrug derivatization (permeability of D-Asp-ACV and ACV were not significantly different).
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