ArticlePloS one2014
In vitro evaluation of the inhibitory potential of pharmaceutical excipients on human carboxylesterase 1A and 2.
Article in PloS one, 2014. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 14 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.
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
14 citing papers in PubMed, 37 citations in OpenAlex.
- Experimental and In Silico Approaches to Study Carboxylesterase Substrate Specificity.Journal of xenobiotics · 2026Review
- Dose, Kidney Function, and a Drug-Excipient Interaction Impair Mycophenolate Mofetil Prodrug Activation in Kidney Transplant Recipients.European journal of drug metabolism and pharmacokinetics · 2025Observational
- Biopharmaceutical Factors Involved in the Disposition of Mycophenolic Acid: A Comprehensive Review of ADME Properties and Their Potential Impact on Mycophenolic Acid Plasma Exposure.Current drug metabolism · 2025Review
- Mammalian Esterase Activity: Implications for Peptide Prodrugs.Biochemistry · 2024Article
- Regulation of carboxylesterases and its impact on pharmacokinetics and pharmacodynamics: an up-to-date review.Expert opinion on drug metabolism & toxicology · 2024Review
- Prognostic and Immunological Roles of CES2 in Breast Cancer and Potential Application of CES2-Targeted Fluorescent Probe DDAB in Breast Surgery.International journal of general medicine · 2023Article
- Fundamental Aspects of Lipid-Based Excipients in Lipid-Based Product Development.Pharmaceutics · 2022Review
- Co-Spray Dried Nafamostat Mesylate with Lecithin and Mannitol as Respirable Microparticles for Targeted Pulmonary Delivery: Pharmacokinetics and Lung Distribution in Rats.Pharmaceutics · 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
- In Silico Investigation of First-Pass Effect on Selected Small Molecule Excipients and Structural Dynamics of P-glycoprotein.Bioinformatics and biology insights · 2020Article
- Prognostic Impact of Carboxylesterase 2 in Cholangiocarcinoma.Scientific reports · 2019Article
- Human carboxylesterases: a comprehensive review.Acta pharmaceutica Sinica. B · 2018Review
- Enhancement of Dissolution Rate and Intestinal Stability of Clopidogrel Hydrogen Sulfate.European journal of drug metabolism and pharmacokinetics · 2016Article
- Regulations of Xenobiotics and Endobiotics on Carboxylesterases: A Comprehensive Review.European journal of drug metabolism and pharmacokinetics · 2016Review
Corrections and comments
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Authors and funding
9 authors at 3 institutions in 2 countries.
Funding
No grant is acknowledged in the PubMed record.
Abstract
Two major forms of human carboxylesterase (CES), CES1A and CES2, dominate the pharmacokinetics of most prodrugs such as imidapril and irinotecan (CPT-11). Excipients, largely used as insert vehicles in formulation, have been recently reported to affect drug enzyme activity. The influence of excipients on the activity of CES remains undefined. In this study, the inhibitory effects of 25 excipients on the activities of CES1A1 and CES2 were evaluated. Imidapril and CPT-11 were used as substrates and cultured with liver microsomes in vitro. Imidapril hydrolase activities of recombinant CES1A1 and human liver microsomes (HLM) were strongly inhibited by sodium lauryl sulphate (SLS) and polyoxyl 40 hydrogenated castor oil (RH40) [Inhibition constant (Ki) = 0.04 ± 0.01 μg/ml and 0.20 ± 0.09 μg/ml for CES1A1, and 0.12 ± 0.03 μg/ml and 0.76 ± 0.33 μg/ml, respectively, for HLM]. The enzyme hydrolase activity of recombinant CES2 was substantially inhibited by Tween 20 and polyoxyl 35 castor oil (EL35) (K(i) = 0.93 ± 0.36 μg/ml and 4.4 ± 1.24 μg/ml, respectively). Thus, these results demonstrate that surfactants such as SLS, RH40, Tween 20 and EL35 may attenuate the CES activity; such inhibition should be taken into consideration during drug administration.
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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.