ADMET and DMPKPub Date : 2022-03-04DOI: 10.5599/admet.1271
V. Gigante, Hatim F Sati, P. Beyer
{"title":"Recent advances and challenges in antibacterial drug development","authors":"V. Gigante, Hatim F Sati, P. Beyer","doi":"10.5599/admet.1271","DOIUrl":"https://doi.org/10.5599/admet.1271","url":null,"abstract":"The abstract is not provided being a short comunication / featured article.","PeriodicalId":7259,"journal":{"name":"ADMET and DMPK","volume":"16 1","pages":"147 - 151"},"PeriodicalIF":2.5,"publicationDate":"2022-03-04","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"82026695","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
ADMET and DMPKPub Date : 2022-02-02eCollection Date: 2022-01-01DOI: 10.5599/admet.1172
Murat Ozdal, Sumeyra Gurkok
{"title":"Recent advances in nanoparticles as antibacterial agent.","authors":"Murat Ozdal, Sumeyra Gurkok","doi":"10.5599/admet.1172","DOIUrl":"https://doi.org/10.5599/admet.1172","url":null,"abstract":"<p><p>Recently, the rapid increase in antibiotic-resistant pathogens has caused serious health problems. Researchers are searching for alternative antimicrobial substances to control or prevent infections caused by pathogens. Different strategies are used to develop effective antibacterial agents, and in this respect, nanoparticles are undoubtedly promising materials. Nanoparticles act by bypassing drug resistance mechanisms in bacteria and inhibiting biofilm formation or other important processes related to their virulence potential. Nanoparticles can penetrate the cell wall and membrane of bacteria and act by disrupting important molecular mechanisms. In combination with appropriate antibiotics, NPs may show synergy and help prevent the developing global bacterial resistance crisis. Furthermore, due to characteristics such as enhanced biocompatibility and biodegradability, polymer-based nanoparticles enable the development of a wide range of medical products. Antibacterial applications of nanoparticles range from antimicrobial synthetic textiles to biomedical and surgical devices when nanoparticles are embedded/loaded/coated into different materials. In this review, the antibacterial mechanisms of nanoparticles and their potential for use in the medical field are discussed.</p>","PeriodicalId":7259,"journal":{"name":"ADMET and DMPK","volume":"10 2","pages":"115-129"},"PeriodicalIF":2.5,"publicationDate":"2022-02-02","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC8957245/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"71419610","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
ADMET and DMPKPub Date : 2022-01-20DOI: 10.5599/admet.1215
Guangshun Wang, A. Mechesso
{"title":"Realistic and critical review of the state of systemic antimicrobial peptides","authors":"Guangshun Wang, A. Mechesso","doi":"10.5599/admet.1215","DOIUrl":"https://doi.org/10.5599/admet.1215","url":null,"abstract":"Antimicrobial peptide research remains active not only because of the growing antibiotic resistance problem but also our desire to understand the role of innate immune peptides in host defense. While numerous peptides are currently under active development for topical use, this article highlights peptides with systemic efficacy. The scaffolds of these peptides range from linear to cyclic forms. The neutropenic mouse model is well established to illustrate antimicrobial efficacy from direct killing. The majority of tests, however, are conducted using normal mice so that both direct antimicrobial and immune regulatory effects can be characterized. These systemic examples underscore the possibility of adding new candidates to the list of the existing peptide antibiotics to more effectively combat antibiotic-resistant bacteria, fungi, and parasites.","PeriodicalId":7259,"journal":{"name":"ADMET and DMPK","volume":"56 1","pages":"91 - 105"},"PeriodicalIF":2.5,"publicationDate":"2022-01-20","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"88823986","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
ADMET and DMPKPub Date : 2022-01-14DOI: 10.5599/admet.1078
S. Berns, J. Isakova, Polina Pekhtereva
{"title":"Therapeutic potential of interferon-gamma in tuberculosis","authors":"S. Berns, J. Isakova, Polina Pekhtereva","doi":"10.5599/admet.1078","DOIUrl":"https://doi.org/10.5599/admet.1078","url":null,"abstract":"Tuberculosis is one of the critical health problems worldwide. The search for ways to improve the results of tuberculosis treatment and overcome drug resistance lies in understanding the pathogenesis of the development of the infectious process. The interferon system, particularly the role of interferon-gamma, has been identified as the main link in the immune response in tuberculosis. The clinical efficacy of interferon-gamma has been studied and evaluated in clinical trials since the end of the last century. There was obtained evidence of the clinical efficacy of interferon-gamma as part of complex therapy. Recent experimental data make it possible to consider interferon-gamma as a promising therapeutic option for the treatment of multidrug-resistant tuberculosis as part of complex therapy worthy of further studies.","PeriodicalId":7259,"journal":{"name":"ADMET and DMPK","volume":"23 1","pages":"63 - 73"},"PeriodicalIF":2.5,"publicationDate":"2022-01-14","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"76162804","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
ADMET and DMPKPub Date : 2022-01-12DOI: 10.5599/admet.1179
A. Bogdanov, O. Tsivileva, A. Voloshina, A. Lyubina, S. Amerhanova, Ekaterina Burtceva, S. Bukharov, Alexander V. Samorodov, V. Pavlov
{"title":"Synthesis and diverse biological activity profile of triethylammonium isatin-3-hydrazones","authors":"A. Bogdanov, O. Tsivileva, A. Voloshina, A. Lyubina, S. Amerhanova, Ekaterina Burtceva, S. Bukharov, Alexander V. Samorodov, V. Pavlov","doi":"10.5599/admet.1179","DOIUrl":"https://doi.org/10.5599/admet.1179","url":null,"abstract":"A series of biorelevant triethylammonium isatin hydrazones containing various substituents in the aromatic fragment have been synthesized. Their structure and composition were confirmed by NMR- and IR-spectroscopies, mass-spectrometry and elemental analysis. It was found that some representatives show activity against Staphylococcus aureus and Bacillus cereus higher or at the level of norfloxacin, including methicillin-resistant Staphylococcus aureus strains. The study also showed low hemo- and cytotoxicity (Chang Liver) and high antiaggregatory and anticoagulant activity of these compounds. The high potential of new ammonium isatin-3-acylhydrazones in the search for antimicrobial activity against phytopathogens of bacterial and fungal nature has been shown for the first time.","PeriodicalId":7259,"journal":{"name":"ADMET and DMPK","volume":"26 1","pages":"163 - 179"},"PeriodicalIF":2.5,"publicationDate":"2022-01-12","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"88276481","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
ADMET and DMPKPub Date : 2022-01-11DOI: 10.5599/admet.1183
S. Amponsah, Joseph A. Boadu, Daniel K. Dwamena, K. F. Opuni
{"title":"Bioanalysis of aminoglycosides using high-performance liquid chromatography","authors":"S. Amponsah, Joseph A. Boadu, Daniel K. Dwamena, K. F. Opuni","doi":"10.5599/admet.1183","DOIUrl":"https://doi.org/10.5599/admet.1183","url":null,"abstract":"Aminoglycosides are broad-spectrum antibiotics used in the treatment of gram-negative bacterial infections. Due to their nephrotoxic and ototoxic potential (narrow therapeutic index), the use of aminoglycoside for clinical indications requires monitoring. The objective of this review was to identify relevant literature reporting liquid chromatographic methods for the bioanalysis of aminoglycosides in both preclinical and clinical settings/experiments. Data on liquid chromatographic methods were collected from articles in an online academic database (PubMed, Science Direct, Scopus, and Google Scholar). All 71 articles published from 1977 to 2020 were included in the review. Reversed-phase liquid chromatography was the most used method for the bioanalysis of aminoglycosides. Fluorescence or ultraviolet detection methods were mostly used from 1977 to 2002 (51 articles), while mass spectrometry was predominantly used as a detector from 2003 to 2020 (15 articles). Sixty-seven articles reported calibration ranges, which varied significantly for the various drugs assayed: some in the range of 0.1-0.5 ng/mL and others 1250-200000 ng/mL. Also, 61 articles reported R2 values (0.964-1.0) for almost all analytes under consideration. Sixty-three articles reported percent recoveries mostly between 61.0 % to 114.0 %, with only two articles reporting recoveries of 4.9 % and 36 %. Out of the 71 reviewed articles, 56 reported intermediate precision values ranging between 0.331 % to 19.76 %, which is within the acceptable limit of 20 %. This review will serve as a guide for research and/or routine clinical monitoring of aminoglycosides in biological matrices.","PeriodicalId":7259,"journal":{"name":"ADMET and DMPK","volume":"56 1","pages":"27 - 62"},"PeriodicalIF":2.5,"publicationDate":"2022-01-11","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"87641306","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
ADMET and DMPKPub Date : 2022-01-07DOI: 10.5599/admet.1164
B. Plotkin, M. Konaklieva
{"title":"Impact of host factors on susceptibility to antifungal agents","authors":"B. Plotkin, M. Konaklieva","doi":"10.5599/admet.1164","DOIUrl":"https://doi.org/10.5599/admet.1164","url":null,"abstract":"An obstacle to drug development, particularly in this era of multiple drug resistance, is the under-appreciation for the role the host environment plays in microbial response to drugs. With the rise in fungal infection and drug resistance, particularly in individuals with co-morbidities, the influence serum and its components have on antimicrobial susceptibility requires assessment. This study examined the impact of physiologically relevant glucose and insulin levels in the presence and absence of 50 % human plasma on MICs for clinical isolates of Candida lusitaniae, Candida parapsilosis, Candida albicans, Candida tropicalis, Candida glabrata, Candida krusei and Cryptococcus neoformans. The addition of insulin or glucose at physiologic levels in RPMI medium alone altered the MIC in either a positive or negative fashion, depending on the organisms and drug tested, with C. glabrata most significantly altered with a 40, >32- and 46-fold increase in MIC for amphotericin B, itraconazole and miconazole, respectively. The addition of candida-antibody negative plasma also affected MIC, with the addition of glucose and insulin having a tandem effect on MIC. These findings indicate that phenotypic resistance of Candida and Cryptococcus can vary depending on the presence of insulin with glucose and plasma. This modulation of resistance may help explain treatment failures in the diabetic population and facilitate the development of stable drug-resistant strains. Furthermore, these findings indicate the need for a precision approach in the choice of drug treatment and drug development.","PeriodicalId":7259,"journal":{"name":"ADMET and DMPK","volume":"106 1","pages":"153 - 162"},"PeriodicalIF":2.5,"publicationDate":"2022-01-07","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"74345043","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
ADMET and DMPKPub Date : 2022-01-01DOI: 10.5599/admet.1427
Nanami Nakatani, Kiyohiko Sugano
{"title":"Effect of divalent and trivalent metal ions on artificial membrane permeation of fluoroquinolones.","authors":"Nanami Nakatani, Kiyohiko Sugano","doi":"10.5599/admet.1427","DOIUrl":"https://doi.org/10.5599/admet.1427","url":null,"abstract":"<p><p>The purpose of the present study was to evaluate the predictability of PAMPA for the effect of metal ions on the bioavailability of fluoroquinolones (FQ). Eleven FQs and seven metal ions were employed in this study. The PAMPA membrane consisted of a 10 % soybean lecithin (SL) - decane solution. A drug solution in MES buffer with or without a metal ion (added as a chloride salt) was added to the donor compartment. In the absence of metal ions, FQ showed relatively high permeability (> 5 × 10<sup>-6</sup> cm/sec) in SL-PAMPA despite their hydrophilic and zwitterionic properties. As the PAMPA permeability ratio with/without metal ions became smaller, the urinary excretion and AUC ratios tended to be smaller, suggesting that SL-PAMPA is a suitable in vitro model to evaluate the potential effect of metal ions on the bioavailability of FQ. However, the reduction in AUC and urinary excretion was overestimated for low solubility metal ion formulations (dried aluminum hydroxide gel and La<sub>2</sub>(CO<sub>3</sub>)<sub>3</sub>・8H<sub>2</sub>O). In such cases, the dissolution of the metal ion formulations and the permeation of FQs should be simultaneously evaluated.</p>","PeriodicalId":7259,"journal":{"name":"ADMET and DMPK","volume":"10 4","pages":"289-297"},"PeriodicalIF":2.5,"publicationDate":"2022-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC9793463/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"10800157","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
ADMET and DMPKPub Date : 2022-01-01DOI: 10.5599/admet.1568
Alex Avdeef
{"title":"Thickness of the aqueous boundary layer in stirred microtitre plate permeability assays (PAMPA and Caco-2), based on the Levich equation.","authors":"Alex Avdeef","doi":"10.5599/admet.1568","DOIUrl":"https://doi.org/10.5599/admet.1568","url":null,"abstract":"The stirring frequency exponent of -1/2 in the theoretical Levich expression appears to apply to PAMPA and Caco-2 assays, where efficient individual-well magnetic stirring ( > 20 RPM) is used. If a single molecule is used as a stirring calibrant, then scaling suggested by Eq. (5) with microtitre plate data may be used. The error in calculating hABL based on unscaled hABLref can be as high as 30%. This is of practical importance in PAMPA, and perhaps cellular assays as well.","PeriodicalId":7259,"journal":{"name":"ADMET and DMPK","volume":"10 4","pages":"249-252"},"PeriodicalIF":2.5,"publicationDate":"2022-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC9793457/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"10800156","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
ADMET and DMPKPub Date : 2022-01-01DOI: 10.5599/admet.1140
Marilyn N. Martinez, M. Papich, R. Fahmy
{"title":"Impact of gastrointestinal differences in veterinary species on the oral drug solubility, in vivo dissolution, and formulation of veterinary therapeutics","authors":"Marilyn N. Martinez, M. Papich, R. Fahmy","doi":"10.5599/admet.1140","DOIUrl":"https://doi.org/10.5599/admet.1140","url":null,"abstract":"Many gaps exist in our understanding of species differences in gastrointestinal (GI) fluid composition and the associated impact of food intake and dietary composition on in vivo drug solubilization. This information gap can lead to uncertainties with regard to how best to formulate pharmaceuticals for veterinary use or the in vitro test conditions that will be most predictive of species-specific in vivo oral product performance. To address these challenges, this overview explores species-specific factors that can influence oral drug solubility and the formulation approaches that can be employed to overcome solubility-associated bioavailability difficulties. These discussions are framed around some of the basic principles associated with drug solubilization, reported species differences in GI fluid composition, types of oral dosage forms typically given for the various animal species, and the effect of prandial state in dogs and cats. This basic information is integrated into a question-and-answer section that addresses some of the formulation issues that can arise in the development of veterinary medicinals.","PeriodicalId":7259,"journal":{"name":"ADMET and DMPK","volume":"19 1","pages":"1 - 25"},"PeriodicalIF":2.5,"publicationDate":"2022-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"85821208","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}