ArticleMolecular pharmaceutics2013
Mediation of in vitro cytochrome p450 activity by common pharmaceutical excipients.
Article in Molecular pharmaceutics, 2013. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 12 papers.
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The abstract states no effect estimate the extractor could read, or names no intervention and outcome on the map, so this paper lights no cell and moves no belief. It is still indexed, cited and linked below.
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Who cites it
12 citing papers in PubMed, 49 citations in OpenAlex.
- Biofunctional Excipients: Their Emerging Role in Overcoming the Inherent Poor Biopharmaceutical Characteristics of Drugs.Pharmaceutics · 2025Review
- Assessing CYP2C8-Mediated Pharmaceutical Excipient-Drug Interaction Potential: A Case Study of Tween 80 and Cremophor EL-35.Pharmaceutics · 2021Article
- The biological fate of the polymer nanocarrier material monomethoxy poly(ethylene glycol)-Acta pharmaceutica Sinica. B · 2021Article
- Three-dimensional aspects of formulation excipients in drug discovery: a critical assessment on orphan excipients, matrix effects and drug interactions.Journal of pharmaceutical analysis · 2020Review
- Pharmaceutical Excipients and Drug Metabolism: A Mini-Review.International journal of molecular sciences · 2020Review
- In Silico Investigation of First-Pass Effect on Selected Small Molecule Excipients and Structural Dynamics of P-glycoprotein.Bioinformatics and biology insights · 2020Article
- Structure and inhibition mechanism of the catalytic domain of human squalene epoxidase.Nature communications · 2019Article
- Towards a rational design of solid drug nanoparticles with optimised pharmacological properties.Journal of interdisciplinary nanomedicine · 2016Article
- A review of polymers as multifunctional excipients in drug dosage form technology.Saudi pharmaceutical journal : SPJ : the official publication of the Saudi Pharmaceutical Society · 2016Review
- The Effects of Pharmaceutical Excipients on Gastrointestinal Tract Metabolic Enzymes and Transporters-an Update.The AAPS journal · 2016Article
- Physiologically Based Pharmacokinetic Modelling to Inform Development of Intramuscular Long-Acting Nanoformulations for HIV.Clinical pharmacokinetics · 2015Article
- Optimizing nanomedicine pharmacokinetics using physiologically based pharmacokinetics modelling.British journal of pharmacology · 2014Review
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Authors and funding
5 authors at 1 institution in 1 country.
Funding
Abstract
Polymers and surfactants are commonly used as excipients in oral formulations and are generally considered to be inert. However, relatively few studies have assessed their interaction with enzymes involved in the absorption, distribution, metabolism, and elimination of drugs. We have investigated the impact of twenty-three commonly used excipients (ten polymers and thirteen surfactants) on seven cytochrome P450 (CYP450) isoforms using baculosome-derived CYP450 enzymes across a range of concentrations. Time-course fluorescent readings were then taken to generate IC50 (inhibition) or EC50 (activation) values for excipient effects on CYP450 activity. All excipients had an observable effect activity of at least one CYP450 isoform with the majority of excipients altering substrate metabolism of at least 57% of CYP450s studied. In addition, most excipients were capable of inhibiting and increasing activity of several different CYP450 isoforms. Although the majority of these effects required concentrations outside those achievable therapeutically (>100 μM), almost 20% were seen at concentrations below 100 μM, and these results indicate that several excipients have the potential to modify the pharmacokinetics of administered drugs.
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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.