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Pharmaceutics
Special Issues
Bioanalysis and Metabolomics, 2nd Edition
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Bioanalysis and Metabolomics, 2nd Edition

A special issue of Pharmaceutics (ISSN 1999-4923). This special issue belongs to the section "Pharmacokinetics and Pharmacodynamics".

Deadline for manuscript submissions: 20 May 2024 | Viewed by 6717

Special Issue Editors

Prof. Dr. Kwang-Hyeon Liu

E-Mail Website
Guest Editor
College of Pharmacy and Research Institute of Pharmaceutical Sciences, Kyungpook National University, Daegu 41566, Republic of Korea
Interests: drug metabolism; metabolomics; lipidomics
Special Issues, Collections and Topics in MDPI journals
Prof. Dr. Hye Suk Lee

E-Mail Website
Guest Editor
College of Pharmacy, The Catholic University of Korea, Bucheon 14662, Republic of Korea
Interests: bioanalysis; drug metabolism; pharmacokinetics; drug interactions
Special Issues, Collections and Topics in MDPI journals

Special Issue Information

Dear Colleagues,

Recently, techniques for analyzing endogenous and exogenous substances present in biological samples have been developed due to the development of analytical instruments that combine chromatography and mass spectrometry. As a result, as micro-analysis of drugs is possible, microdosing methods for studying the pharmacokinetics of drugs in humans through the administration of sub-therapeutic doses have been developed and applied in clinical trials. In addition, metabolomics techniques that target endogenous substances in biological samples have been developed, and various studies on biomarkers that can be used to diagnose the disease early and evaluate the efficacy of drugs have been actively conducted. This Special Issue aims to highlight current progress in bioanalysis related to drug metabolism and pharmacokinetics and drug- and disease-related metabolomics.

Prof. Dr. Kwang-Hyeon Liu
Prof. Dr. Hye Suk Lee
Guest Editors

Manuscript Submission Information

Manuscripts should be submitted online at www.mdpi.com by registering and logging in to this website. Once you are registered, click here to go to the submission form. Manuscripts can be submitted until the deadline. All submissions that pass pre-check are peer-reviewed. Accepted papers will be published continuously in the journal (as soon as accepted) and will be listed together on the special issue website. Research articles, review articles as well as short communications are invited. For planned papers, a title and short abstract (about 100 words) can be sent to the Editorial Office for announcement on this website.

Submitted manuscripts should not have been published previously, nor be under consideration for publication elsewhere (except conference proceedings papers). All manuscripts are thoroughly refereed through a single-blind peer-review process. A guide for authors and other relevant information for submission of manuscripts is available on the Instructions for Authors page. Pharmaceutics is an international peer-reviewed open access monthly journal published by MDPI.

Please visit the Instructions for Authors page before submitting a manuscript. The Article Processing Charge (APC) for publication in this open access journal is 2900 CHF (Swiss Francs). Submitted papers should be well formatted and use good English. Authors may use MDPI's English editing service prior to publication or during author revisions.

Keywords

  • bioanalysis
  • method validation
  • pharmacokinetics
  • metabolomics
  • lipidomics
  • biomarkers
  • mass spectrometry

Related Special Issue

Published Papers (4 papers)

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Research

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14 pages, 3236 KiB  
Article
Evaluation of the Drug-Induced Liver Injury Potential of Saxagliptin through Reactive Metabolite Identification in Rats
by Ki-Young Kim, Yeo-Jin Jeong, So-Young Park, Eun-Ji Park, Ji-Hyeon Jeon, Im-Sook Song and Kwang-Hyeon Liu
Pharmaceutics 2024, 16(1), 106; https://doi.org/10.3390/pharmaceutics16010106 - 13 Jan 2024
Viewed by 1011
Abstract
A liver injury was recently reported for saxagliptin, which is a dipeptidyl peptidase-4 (DPP-4) inhibitor. However, the underlying mechanisms of saxagliptin-induced liver injury remain unknown. This study aimed to evaluate whether saxagliptin, a potent and selective DPP-4 inhibitor that is globally used for [...] Read more.
A liver injury was recently reported for saxagliptin, which is a dipeptidyl peptidase-4 (DPP-4) inhibitor. However, the underlying mechanisms of saxagliptin-induced liver injury remain unknown. This study aimed to evaluate whether saxagliptin, a potent and selective DPP-4 inhibitor that is globally used for treating type 2 diabetes mellitus, binds to the nucleophiles in vitro. Four DPP-4 inhibitors, including vildagliptin, were evaluated for comparison. Only saxagliptin and vildagliptin, which both contain a cyanopyrrolidine group, quickly reacted with L-cysteine to enzyme-independently produce thiazolinic acid metabolites. This saxagliptin–cysteine adduct was also found in saxagliptin-administered male Sprague–Dawley rats. In addition, this study newly identified cysteinyl glycine conjugates of saxagliptin and 5-hydroxysaxagliptin. The observed metabolic pathways were hydroxylation and conjugation with cysteine, glutathione, sulfate, and glucuronide. In summary, we determined four new thiazoline-containing thiol metabolites (cysteine and cysteinylglycine conjugates of saxagliptin and 5-hydroxysaxagliptin) in saxagliptin-administered male rats. Our results reveal that saxagliptin can covalently bind to the thiol groups of cysteine residues of endogenous proteins in vivo, indicating the potential for saxagliptin to cause drug-induced liver injury. Full article
(This article belongs to the Special Issue Bioanalysis and Metabolomics, 2nd Edition)
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12 pages, 1876 KiB  
Article
Preclinical Bioavailability Assessment of a Poorly Water-Soluble Drug, HGR4113, Using a Stable Isotope Tracer
by Eun Ji Ha, Jeong In Seo, Shaheed Ur Rehman, Hyung Soon Park, Sang-Ku Yoo and Hye Hyun Yoo
Pharmaceutics 2023, 15(6), 1684; https://doi.org/10.3390/pharmaceutics15061684 - 08 Jun 2023
Cited by 1 | Viewed by 1114
Abstract
Drug solubility limits intravenous dosing for poorly water-soluble medicines, which misrepresents their bioavailability estimation. The current study explored a method using a stable isotope tracer to assess the bioavailability of drugs that are poorly water-soluble. HGR4113 and its deuterated analog, HGR4113-d7, were tested [...] Read more.
Drug solubility limits intravenous dosing for poorly water-soluble medicines, which misrepresents their bioavailability estimation. The current study explored a method using a stable isotope tracer to assess the bioavailability of drugs that are poorly water-soluble. HGR4113 and its deuterated analog, HGR4113-d7, were tested as model drugs. To determine the level of HGR4113 and HGR4113-d7 in rat plasma, a bioanalytical method using LC-MS/MS was developed. The HGR4113-d7 was intravenously administered to rats that were orally pre-administered HGR4113 at different doses; subsequently, the plasma samples were collected. HGR4113 and HGR4113-d7 were simultaneously determined in the plasma samples, and bioavailability was calculated using plasma drug concentration values. The bioavailability of HGR4113 was 53.3% ± 19.5%, 56.9% ± 14.0%, and 67.8% ± 16.7% after oral dosages of 40, 80, and 160 mg/kg, respectively. By eliminating the differences in clearance between intravenous and oral dosages at different levels, acquired data showed that the current method reduced measurement errors in bioavailability when compared to the conventional approach. The present study suggests a prominent method for evaluating the bioavailability of drugs with poor aqueous solubility in preclinical studies. Full article
(This article belongs to the Special Issue Bioanalysis and Metabolomics, 2nd Edition)
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21 pages, 1122 KiB  
Article
An Approach to Evaluate the Effective Cytoplasmic Concentration of Bioactive Agents Interacting with a Selected Intracellular Target Protein
by Yuri V. Khramtsov, Alexey V. Ulasov, Andrey A. Rosenkranz, Tatiana A. Slastnikova, Tatiana N. Lupanova, Georgii P. Georgiev and Alexander S. Sobolev
Pharmaceutics 2023, 15(2), 324; https://doi.org/10.3390/pharmaceutics15020324 - 18 Jan 2023
Cited by 4 | Viewed by 1392
Abstract
To compare the effectiveness of various bioactive agents reversibly acting within a cell on a target intracellular macromolecule, it is necessary to assess effective cytoplasmic concentrations of the delivered bioactive agents. In this work, based on a simple equilibrium model and the cellular [...] Read more.
To compare the effectiveness of various bioactive agents reversibly acting within a cell on a target intracellular macromolecule, it is necessary to assess effective cytoplasmic concentrations of the delivered bioactive agents. In this work, based on a simple equilibrium model and the cellular thermal shift assay (CETSA), an approach is proposed to assess effective concentrations of both a delivered bioactive agent and a target protein. This approach was tested by evaluating the average concentrations of nuclear factor erythroid 2-related factor 2 (Nrf2) and Kelch-like ECH-associated-protein 1 (Keap1) proteins in the cytoplasm for five different cell lines (Hepa1, MEF, RAW264.7, 3LL, and AML12) and comparing the results with known literature data. The proposed approach makes it possible to analyze both binary interactions and ternary competition systems; thus, it can have a wide application for the analysis of protein–protein or molecule–protein interactions in the cell. The concentrations of Nrf2 and Keap1 in the cell can be useful not only in analyzing the conditions for the activation of the Nrf2 system, but also for comparing the effectiveness of various drug delivery systems, where the delivered molecule is able to interact with Keap1. Full article
(This article belongs to the Special Issue Bioanalysis and Metabolomics, 2nd Edition)
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Review

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26 pages, 2272 KiB  
Review
Comprehensive Two-Dimensional Gas Chromatography as a Bioanalytical Platform for Drug Discovery and Analysis
by Atiqah Zaid, Norfarizah Hanim Hassan, Philip J. Marriott and Yong Foo Wong
Pharmaceutics 2023, 15(4), 1121; https://doi.org/10.3390/pharmaceutics15041121 - 31 Mar 2023
Cited by 4 | Viewed by 2612
Abstract
Over the last decades, comprehensive two-dimensional gas chromatography (GC×GC) has emerged as a significant separation tool for high-resolution analysis of disease-associated metabolites and pharmaceutically relevant molecules. This review highlights recent advances of GC×GC with different detection modalities for drug discovery and analysis, which [...] Read more.
Over the last decades, comprehensive two-dimensional gas chromatography (GC×GC) has emerged as a significant separation tool for high-resolution analysis of disease-associated metabolites and pharmaceutically relevant molecules. This review highlights recent advances of GC×GC with different detection modalities for drug discovery and analysis, which ideally improve the screening and identification of disease biomarkers, as well as monitoring of therapeutic responses to treatment in complex biological matrixes. Selected recent GC×GC applications that focus on such biomarkers and metabolite profiling of the effects of drug administration are covered. In particular, the technical overview of recent GC×GC implementation with hyphenation to the key mass spectrometry (MS) technologies that provide the benefit of enhanced separation dimension analysis with MS domain differentiation is discussed. We conclude by highlighting the challenges in GC×GC for drug discovery and development with perspectives on future trends. Full article
(This article belongs to the Special Issue Bioanalysis and Metabolomics, 2nd Edition)
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