ArticlePharmaceutical research2009
Enhanced corneal absorption of erythromycin by modulating P-glycoprotein and MRP mediated efflux with corticosteroids.
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 19 papers.
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Who cites it
19 citing papers in PubMed, 54 citations in OpenAlex.
- Multidrug resistance-associated protein 2 (MRP2/ABCC2) haplotypes significantly affect the pharmacokinetics of tacrolimus in kidney transplant recipients.Clinical pharmacokinetics · 2013Trial
- Transporter Protein Expression of Corneal Epithelium in Rabbit and Porcine: Evaluation of Models for Ocular Drug Transport Study.Molecular pharmaceutics · 2024Article
- Overview of processed excipients in ocular drug delivery: Opportunities so far and bottlenecks.Heliyon · 2024Review
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- Advances in the use of prodrugs for drug delivery to the eye.Expert opinion on drug delivery · 2017Review
- A comprehensive insight on ocular pharmacokinetics.Drug delivery and translational research · 2016Review
- Prodrug approach to improve absorption of prednisolone.International journal of pharmaceutics · 2015Article
- Interaction Studies of Resolvin E1 Analog (RX-10045) with Efflux Transporters.Journal of ocular pharmacology and therapeutics : the official journal of the Association for Ocular Pharmacology and Therapeutics · 2015Article
- Binary and ternary combinations of anti-HIV protease inhibitors: effect on gene expression and functional activity of CYP3A4 and efflux transporters.Drug metabolism and drug interactions · 2014Article
- Gene expression profiling of transporters in the solute carrier and ATP-binding cassette superfamilies in human eye substructures.Molecular pharmaceutics · 2013Article
- Differential effect of P-gp and MRP2 on cellular translocation of gemifloxacin.International journal of pharmaceutics · 2011Article
- A novel cell-associated protection assay demonstrates the ability of certain antibiotics to protect ocular surface cell lines from subsequent clinical Staphylococcus aureus challenge.Antimicrobial agents and chemotherapy · 2011Article
- Effect of ABCC2 (MRP2) transport function on erythromycin metabolism.Clinical pharmacology and therapeutics · 2011Article
- Modulation of drug block of the cardiac potassium channel KCNA5 by the drug transporters OCTN1 and MDR1.British journal of pharmacology · 2010Article
- Interaction between topically and systemically coadministered P-glycoprotein substrates/inhibitors: effect on vitreal kinetics.Drug metabolism and disposition: the biological fate of chemicals · 2010Article
- Interaction of gatifloxacin with efflux transporters: a possible mechanism for drug resistance.International journal of pharmaceutics · 2010Article
- Interaction of ocular hypotensive agents (PGF2 alpha analogs-bimatoprost, latanoprost, and travoprost) with MDR efflux pumps on the rabbit cornea.Journal of ocular pharmacology and therapeutics : the official journal of the Association for Ocular Pharmacology and Therapeutics · 2009Article
- Role of transporters in ocular drug delivery system.Pharmaceutical research · 2009Article
- Nanotechnology approaches for ocular drug delivery.Middle East African journal of ophthalmologyReview
Corrections and comments
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Authors and funding
5 authors at 1 institution in 1 country.
Funding
Abstract
purposeThe objectives were (i) to test in vivo functional activity of MRP2 on rabbit corneal epithelium and (ii) to evaluate modulation of P-gp and MRP2 mediated efflux of erythromycin when co-administered with corticosteroids.
methodsCultured rabbit primary corneal epithelial cells (rPCECs) was employed as an in vitro model for rabbit cornea. Cellular accumulation and bi-directional transport studies were conducted across Madin-Darby Canine Kidney (MDCK) cells overexpressing MDR1 and MRP2 proteins to delineate transporter specific interaction of steroids. Ocular pharmacokinetic studies were conducted in rabbits following a single-dose infusion of erythromycin in the presence of specific inhibitors and steroids.
resultsBi-directional transport of erythromycin across MDCK-MDR1 and MDCK-MRP2 cells showed significant difference between BL-AP and AP-BL permeability, suggesting that erythromycin is a substrate for P-gp and MRP2. Cellular accumulation of erythromycin in rPCEC was inhibited by steroids in a dose dependent manner. MK571, a specific MRP inhibitor, modulated the aqueous humor concentration of erythromycin in vivo. Even, steroids inhibited P-gp and MRP2 mediated efflux with maximum increase in k(a), AUC(0-infinity), C(max) and C(last) values of erythromycin, observed with 6alpha-methyl prednisolone.
conclusionMRP2 is functionally active along with P-gp in effluxing drug molecules out of corneal epithelium. Steroids were able to significantly inhibit both P-gp and MRP2 mediated efflux of erythromycin.
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Registered trials
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