ArticleInternational journal of pharmaceutics2010
Interaction of gatifloxacin with efflux transporters: a possible mechanism for drug resistance.
Article in International journal of pharmaceutics, 2010. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 21 papers.
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Trials whose registry record cites this paper, or whose number appears in the abstract. A trial that started after this paper was published is citing it as background, not reporting it.
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Who cites it
21 citing papers in PubMed, 37 citations in OpenAlex.
- Evaluation of initial and steady-state gatifloxacin pharmacokinetics and dose in pulmonary tuberculosis patients by using monte carlo simulations.Antimicrobial agents and chemotherapy · 2013Trial
- Gatifloxacin detection in the nanoscale: a review exploring current biosensing technologies and future opportunities.RSC advances · 2025Review
- Drug Transporters and Metabolizing Enzymes in Antimicrobial Drug Pharmacokinetics: Mechanisms, Drug-Drug Interactions, and Clinical Implications.Biomolecules · 2025Review
- Gatifloxacin Loaded Nano Lipid Carriers for the Management of Bacterial Conjunctivitis.Antibiotics (Basel, Switzerland) · 2023Article
- Advantages of Cubosomal Formulation for Gatifloxacin Delivery in the Treatment of Bacterial Keratitis: In Vitro and In Vivo Approach Using Clinical Isolate of Methicillin-ResistantMaterials (Basel, Switzerland) · 2022Article
- A "Double-Edged" Scaffold: Antitumor Power within the Antibacterial Quinolone.Current medicinal chemistry · 2016Review
- The Role of Eukaryotic and Prokaryotic ABC Transporter Family in Failure of Chemotherapy.Frontiers in pharmacology · 2016Review
- 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
- Dipeptide prodrug approach to evade efflux pumps and CYP3A4 metabolism of lopinavir.International journal of pharmaceutics · 2014Article
- Amino Acid Prodrugs: An Approach to Improve the Absorption of HIV-1 Protease Inhibitor, Lopinavir.Pharmaceuticals (Basel, Switzerland) · 2014Article
- 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
- Bitter melon extracts enhance the activity of chemotherapeutic agents through the modulation of multiple drug resistance.Journal of pharmaceutical sciences · 2013Article
- Article
- Targeted lipid based drug conjugates: a novel strategy for drug delivery.International journal of pharmaceutics · 2012Article
- Transfected MDCK cell line with enhanced expression of CYP3A4 and P-glycoprotein as a model to study their role in drug transport and metabolism.Molecular pharmaceutics · 2012Article
- Sodium dependent multivitamin transporter (SMVT): a potential target for drug delivery.Current drug targets · 2012Review
- Bactericidal effect of S-nitrosothiols against clinical isolates from keratitis.Clinical ophthalmology (Auckland, N.Z.) · 2012Article
- Effect of emergence of fluoroquinolone resistance on intrinsic expression of P-glycoprotein phenotype in corneal epithelial cells.Journal of ocular pharmacology and therapeutics : the official journal of the Association for Ocular Pharmacology and Therapeutics · 2011Article
- Differential effect of P-gp and MRP2 on cellular translocation of gemifloxacin.International journal of pharmaceutics · 2011Article
- Multidrug resistance proteins (MRPs/ABCCs) in cancer chemotherapy and genetic diseases.The FEBS journal · 2011Review
Corrections and comments
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Authors and funding
5 authors at 1 institution in 1 country.
Funding
Abstract
The purpose of the study is to screen the interactions of fourth generation fluoroquinolone-gatifloxacin with efflux pumps, i.e., P-gp, MRP2 and BCRP. Mechanism of gatifloxacin interaction with efflux transporters may explain its acquired resistance. Such clarification may lead to the development of strategies to overcome efflux and enhance its bioavailability at target site. This process will aid in the reduction of dose volume, further eliminating the chances of systemic toxicity from topical gatifloxacin eye drops. MDCK cell lines transfected with the targeted efflux transporters were used for this study. [(14)C] Erythromycin was selected as a model substrate for P-gp and MRP2 whereas Hoechst 33342 was employed as a substrate for BCRP. Uptake and transport studies of these substrates were performed in the presence of gatifloxacin to delineate its interaction with efflux transporters. Further the efflux ratio in the presence of gatifloxacin was calculated from bidirectional transport studies. The concentration of [(14)C] erythromycin and Hoechst 33342 was measured using scintillation counter and fluorescence plate reader, respectively. A concentration dependent inhibition effect in the presence of gatifloxacin was revealed on [(14)C] erythromycin uptake. The efflux ratio (BL-AP/AP-BL) of substrates was found to approach unity at higher gatifloxacin concentrations. Increased concentration of gatifloxacin did not elevate uptake of Hoechst 33342. All these studies were validated with known inhibitors as positive control. Uptake and transport studies support the hypothesis that gatifloxacin is a substrate for P-gp, MRP2 but not for BCRP. Possible interactions of gatifloxacin with P-gp and MRP2 may be a possible mechanism for acquired resistance of gatifloxacin. This information can be further extended to design prodrugs or formulations in order to prevent development of acquired resistance and improve therapeutic efficacy with its reduction in side effects.
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