ArticleJournal of pharmaceutical sciences2013
Development and evaluation of a novel microemulsion formulation of elacridar to improve its bioavailability.
Article in Journal of pharmaceutical sciences, 2013. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 24 papers.
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The trial behind it
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
24 citing papers in PubMed, 48 citations in OpenAlex.
- Elacridar Reverses P-gp-Mediated Drug Resistance in Ovarian Cancer Cells in 2D and 3D Culture Models.International journal of molecular sciences · 2025Article
- Elacridar Inhibits BCRP Protein Activity in 2D and 3D Cell Culture Models of Ovarian Cancer and Re-Sensitizes Cells to Cytotoxic Drugs.International journal of molecular sciences · 2025Article
- Pharmacogenomics influence on MDR1-associated cancer resistance and innovative drug delivery approaches: advancing precision oncology.Medical oncology (Northwood, London, England) · 2025Review
- The Role of Elacridar, a P-gp Inhibitor, in the Re-Sensitization of PAC-Resistant Ovarian Cancer Cell Lines to Cytotoxic Drugs in 2D and 3D Cell Culture Models.International journal of molecular sciences · 2025Article
- Quinolone: a versatile therapeutic compound class.Molecular diversity · 2023Review
- Murine Central Nervous System and Bone Marrow Distribution of the Aurora A Kinase Inhibitor Alisertib: Pharmacokinetics and Exposure at the Sites of Efficacy and Toxicity.The Journal of pharmacology and experimental therapeutics · 2022Article
- Optimization of dose and route of administration of the P-glycoprotein inhibitor, valspodar (PSC-833) and the P-glycoprotein and breast cancer resistance protein dual-inhibitor, elacridar (GF120918) as dual infusion in rats.Pharmacology research & perspectives · 2021Article
- Endothelial Regulation of Drug Transport in a 3D Vascularized Tumor Model.Advanced functional materials · 2020Article
- Enhancing Brain Retention of a KIF11 Inhibitor Significantly Improves its Efficacy in a Mouse Model of Glioblastoma.Scientific reports · 2020Article
- Intraperitoneal Route of Drug Administration: Should it Be Used in Experimental Animal Studies?Pharmaceutical research · 2019Review
- Oral delivery of lycopene-loaded microemulsion for brain-targeting: preparation, characterization, pharmacokinetic evaluation and tissue distribution.Drug delivery · 2019Article
- Brain Distributional Kinetics of a Novel MDM2 Inhibitor SAR405838: Implications for Use in Brain Tumor Therapy.Drug metabolism and disposition: the biological fate of chemicals · 2019Article
- Pharmacokinetics of the P-gp Inhibitor Tariquidar in Rats After Intravenous, Oral, and Intraperitoneal Administration.European journal of drug metabolism and pharmacokinetics · 2018Article
- Intravenous infusion for the controlled exposure to the dual ABCB1 and ABCG2 inhibitor elacridar in nonhuman primates.Drug delivery and translational research · 2018Article
- Incorporation of lipolysis in monolayer permeability studies of lipid-based oral drug delivery systems.Drug delivery and translational research · 2018Article
- Article
- Renal Drug Transporters and Drug Interactions.Clinical pharmacokinetics · 2017Review
- Clinical pharmacokinetics of an amorphous solid dispersion tablet of elacridar.Drug delivery and translational research · 2017Article
- Development of a novel microemulsion for oral absorption enhancement of all-trans retinoic acid.International journal of nanomedicine · 2017Article
- Validation of a liquid chromatographic method for the pharmaceutical quality control of products containing elacridar.Journal of pharmaceutical analysis · 2016Article
Corrections and comments
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Authors and funding
3 authors at 1 institution in 1 country.
Funding
Abstract
The study objective was to develop a formulation of elacridar to overcome its dissolution-rate-limited bioavailability. Elacridar is a P-glycoprotein (P-gp) and breast cancer resistance protein (BCRP) inhibitor that has been used to improve the brain distribution of drugs that are substrates of P-gp and BCRP. The chronic use of elacridar is restricted because of the poor solubility leading to poor oral bioavailability. A microemulsion formulation using Cremophor EL, Carbitol, and Captex 355 (6:3:1) was developed. The elacridar microemulsion was effective in the inhibition of P-gp and Bcrp in Madin-Darby canine kidney II-transfected cells. Friend Leukemia Virus Strain B (FVB) mice were used to determine the bioavailability of elacridar after a 10 mg/kg dose of elacridar in the microemulsion, intraperitoneally (i.p.) and orally (p.o.); and the absolute bioavailability was determined to be 1.3 and 0.47, respectively. Coadministration of elacridar microemulsion i.p. with p.o. erlotinib in FVB mice improved the erlotinib brain penetration threefold. The current study shows that a microemulsion formulation of elacridar is effective in improving the bioavailability of elacridar and is an effective inhibitor of P-gp and Bcrp, in vitro and in vivo. It offers an alternative to the suspension and allows a decrease in the dose required to achieve a significant inhibitory effect at the blood-brain barrier.
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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.