Assay and drug development technologies最新文献_第9页

Drug Repurposing Patent Applications January-March 2023. 药物再利用专利申请2023年1月至3月。

IF 1.8 4区医学

Assay and drug development technologies Pub Date : 2023-05-01 DOI: 10.1089/adt.2023.030

Hermann A M Mucke

引用次数: 0

In-Silico Design, Synthesis, and Pharmacological Evaluation of Oxadiazole-Based Selective Cyclo-oxygenase-2 Inhibitors. 基于噁二唑的选择性环氧合酶-2 抑制剂的硅内设计、合成和药理评估。

IF 1.8 4区医学

Assay and drug development technologies Pub Date : 2023-05-01 DOI: 10.1089/adt.2022.090

Manish Kumar, Isha Rani, Somdutt Mujwar, Rakesh Narang, Manish Devgun, Sukhbir Lal Khokra

{"title":"In-Silico Design, Synthesis, and Pharmacological Evaluation of Oxadiazole-Based Selective Cyclo-oxygenase-2 Inhibitors.","authors":"Manish Kumar, Isha Rani, Somdutt Mujwar, Rakesh Narang, Manish Devgun, Sukhbir Lal Khokra","doi":"10.1089/adt.2022.090","DOIUrl":"10.1089/adt.2022.090","url":null,"abstract":"A series of oxadiazole-based five-membered heterocyclic derivatives was designed and synthesized with the intent of exclusive cyclo-oxygenase-2 (COX-2) inhibition to acquire anti-inflammatory activity without the presence of gastric toxicity. Oxadiazole-based novel analogs were designed by using bioisosteric substitutions and were screened against the macromolecular target by using docking-based virtual screening to identify their potential inhibitors. These selective COX-2 inhibitors were further evaluated for their stability within the binding cavity of macromolecular complex by performing molecular dynamic simulation for 100 ns. Selected compounds were synthesized by using Naphthalene-2-yl-acetic acid as a starting material based on the fundamental structure of naphthalene. The naphthalene ring and methylene bridge of naphthalene-2-yl-acetic acid were retained in the rational molecular design by replacing the carboxyl group with biologically significant groups like 1,3,4-oxadiazoles, with the goal of obtaining a novel, superior, and relatively safe anti-inflammatory molecule with better efficacy and optimized pharmacokinetics. Anti-inflammatory as well as analgesic properties of the compounds were evaluated experimentally for their pharmacological efficiency.","PeriodicalId":8586,"journal":{"name":"Assay and drug development technologies","volume":"21 4","pages":"166-179"},"PeriodicalIF":1.8,"publicationDate":"2023-05-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"9645392","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

引用次数: 0

Losartan Plays a Fungistatic and Fungicidal Activity Against Candida albicans Biofilms: Drug Repurposing for Localized Candidosis. 洛沙坦对白色念珠菌生物膜具有抑菌和杀菌作用：针对局部念珠菌病的药物再利用。

IF 1.8 4区医学

Assay and drug development technologies Pub Date : 2023-05-01 Epub Date: 2023-05-25 DOI: 10.1089/adt.2023.013

Vanessa Soares Lara, Rafaela Alves da Silva, Tatiane Ponteado Ferrari, Carlos Ferreira Dos Santos, Sandra Helena Penha de Oliveira

{"title":"Losartan Plays a Fungistatic and Fungicidal Activity Against Candida albicans Biofilms: Drug Repurposing for Localized Candidosis.","authors":"Vanessa Soares Lara, Rafaela Alves da Silva, Tatiane Ponteado Ferrari, Carlos Ferreira Dos Santos, Sandra Helena Penha de Oliveira","doi":"10.1089/adt.2023.013","DOIUrl":"10.1089/adt.2023.013","url":null,"abstract":"Candidosis is one of the most frequent opportunistic infections and exhibits variable clinical presentations, including oral localized forms. Drugs affecting the renin-angiotensin system targets inhibit secreted aspartic proteases from Candida albicans. The objective of the study was to evaluate whether losartan has antimicrobial action against C. albicans biofilms. Biofilms were treated with losartan or aliskiren (for comparison) for 24 h. Metabolic activity of viable cells and growth inhibition of C. albicans biofilms were assessed using XTT [2,3-Bis(2-Methoxy-4-Nitro-5-Sulfophenyl)-5-[(Phenyl-Amino)Carbonyl]-2H-Tetrazolium Hydroxide] and colony-forming unit assays, respectively. In addition, the cytotoxicity of the drugs on human cells was evaluated using the AlamarBlue assay. Both drugs decreased fungal viability at all concentrations. In addition, all concentrations of losartan inhibited the growth of C. albicans biofilm, ranging from 47% to 88.5%, whereas aliskiren showed inhibition from 1 to 10 mg/mL, which ranged from 16% to 97.6%. Furthermore, at certain concentrations, these drugs maintained the viability of human cells. Losartan and aliskiren have fungistatic and fungicidal action against C. albicans biofilms and are compatible with human cells. Therefore, these antihypertensive drugs can be repurposed to interfere with the metabolism and development of Candida biofilms, which are widely associated with clinical forms of candidosis, including oral localized forms such as denture stomatitis.","PeriodicalId":8586,"journal":{"name":"Assay and drug development technologies","volume":"21 4","pages":"157-165"},"PeriodicalIF":1.8,"publicationDate":"2023-05-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"10024903","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

引用次数: 0

Doxorubicin Conjugates: An Efficient Approach for Enhanced Therapeutic Efficacy with Reduced Side Effects. 多柔比星共轭物：提高疗效、减少副作用的有效方法。

IF 1.8 4区医学

Assay and drug development technologies Pub Date : 2023-05-01 Epub Date: 2023-04-20 DOI: 10.1089/adt.2022.102

Pallavi Sandal, Lakshmi Kumari, Preeti Patel, Amrinder Singh, Dilpreet Singh, Ghanshyam Das Gupta, Balak Das Kurmi

{"title":"Doxorubicin Conjugates: An Efficient Approach for Enhanced Therapeutic Efficacy with Reduced Side Effects.","authors":"Pallavi Sandal, Lakshmi Kumari, Preeti Patel, Amrinder Singh, Dilpreet Singh, Ghanshyam Das Gupta, Balak Das Kurmi","doi":"10.1089/adt.2022.102","DOIUrl":"10.1089/adt.2022.102","url":null,"abstract":"Continuous drug delivery modification is the scientific approach and is a basic need for the efficient therapeutic efficacy of active drug molecules. Polymer-drug conjugates have long been a hallmark of the drug delivery sector, with various conjugates on the market or in clinical trials. Improved drug solubilization, extended blood circulation, decreased immunogenicity, controlled release behavior, and increased safety are the advantages of conjugating drugs to the polymeric carrier like polyethylene glycol (PEG). Polymer therapies have evolved over the last decade, resulting in polymer-drug conjugates with diverse topologies and chemical properties. Traditional nondegradable polymeric carriers like PEG and hydroxy propyl methacrylate have been clinically employed to fabricate polymer-drug conjugates. Still, functionalized polymer-drug conjugates are increasingly being used to increase localized drug delivery and ease of removal. Researchers have developed multifunctional carriers that can \"see and treat\" patients using medicinal and diagnostic chemicals. This review focused on the various conjugation approaches for attaching the doxorubicin to different polymers to achieve enhanced therapeutic efficacy, that is, increased bioavailability and reduced adverse effects.","PeriodicalId":8586,"journal":{"name":"Assay and drug development technologies","volume":"21 4","pages":"137-156"},"PeriodicalIF":1.8,"publicationDate":"2023-05-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"10022334","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

引用次数: 0

High-Throughput Ultra Performance Liquid Chromatography-Tandem Mass Spectrometry Method Validation for the Estimation of Atorvastatin and Active Metabolites in Human Plasma. 高通量超高效液相色谱-串联质谱法测定人血浆中阿托伐他汀及其活性代谢物的验证。

IF 1.8 4区医学

Assay and drug development technologies Pub Date : 2023-04-01 DOI: 10.1089/adt.2022.113

Nikhil Agrawal, Amit Mittal

{"title":"High-Throughput Ultra Performance Liquid Chromatography-Tandem Mass Spectrometry Method Validation for the Estimation of Atorvastatin and Active Metabolites in Human Plasma.","authors":"Nikhil Agrawal, Amit Mittal","doi":"10.1089/adt.2022.113","DOIUrl":"https://doi.org/10.1089/adt.2022.113","url":null,"abstract":"A highly selective, sensitive, rugged, and rapid ultra high-performance liquid chromatography-tandem mass spectrometry method (UPLC-MS/MS) is optimized and validated for reliable quantification of atorvastatin (ATR) and its active metabolites, 2-hydroxy atorvastatin (2-ATR) and 4-hydroxy atorvastatin (4-ATR) in human plasma using atorvastatin-D5 (ATR-D5), 2-hydroxy atorvastatin-D5 (2-ATR-D5), and 4-hydroxy atorvastatin-D5 (4-ATR-D5) as deuterium-labeled internal standards (ISTDs), respectively. Isocratic mode chromatographic separation was used with a reverse-phase C18 Symmetry Shield (150 × 4.6 mm, 5.0 μm) column and a mobile phase of acetonitrile:2 mM ammonium formate (pH-3.0) [65:35%v/v] at a flow rate of 0.7 mL/min. Electrospray ionization technique with positive ion mode polarity was applied to achieve the best signal intensity and stable response. Solid-phase extraction by direct elution method was applied to extract the drugs from the plasma sample. The calibration curve range was validated from a concentration range of 0.500-250 ng/mL for ATR and 2-ATR and 0.200-20 ng/mL for 4-ATR. The within-batch and between-batch precision and accuracy were found to be consistent and reproducible for all the analytes across the validation. Extraction recoveries were >80% for all analytes and ISTDs. All peaks of analytes and the respective ISTDs were eluted within 5.2 min. In this validated method, selective multivariate analytical approaches were utilized such as best fit linearity range for different strength formulations, preventive measures for in vivo and ex vivo autodegradation of metabolites, and shorter analysis time. This validated method can be useful for challenging quantification of ATR and its active metabolites for therapeutic drug monitoring and in high-throughput clinical study sample analysis.","PeriodicalId":8586,"journal":{"name":"Assay and drug development technologies","volume":"21 3","pages":"110-125"},"PeriodicalIF":1.8,"publicationDate":"2023-04-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"9515874","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

引用次数: 0

Validation of a Novel Supercritical Fluid Extractor/Dryer Combo Instrument. 一种新型超临界流体萃取/干燥组合仪器的验证。

IF 1.8 4区医学

Assay and drug development technologies Pub Date : 2023-04-01 DOI: 10.1089/adt.2023.005

Mritunjay Kumar, Yash Sharma, Kanak Chahar, Lakshmi Kumari, Lopamudra Mishra, Preeti Patel, Dilpreet Singh, Balak Das Kurmi

{"title":"Validation of a Novel Supercritical Fluid Extractor/Dryer Combo Instrument.","authors":"Mritunjay Kumar, Yash Sharma, Kanak Chahar, Lakshmi Kumari, Lopamudra Mishra, Preeti Patel, Dilpreet Singh, Balak Das Kurmi","doi":"10.1089/adt.2023.005","DOIUrl":"https://doi.org/10.1089/adt.2023.005","url":null,"abstract":"The current pharmaceutical manufacturing scenario involves different techniques for the processing of materials. For example, the extraction unit is one of the essential aspects of plant-based pharmaceuticals. Recently, various kinds of extraction techniques have been used for analytical and preparative scales; among them, a supercritical fluid extractor (SCFE) is the most widely used technique for extraction. It is used for an extensive range of crude drugs and can be possible with the help of SCFE by varying temperature/pressure. Notably, it uses carbon dioxide (CO2) for extraction instead of other solvents. Simultaneously, lyophilization is an important technique used at different processing steps along with other methods. In lyophilization, CO2 is used as a cooling agent in the shelves of lyophilized equipment. It behaves as a supercritical fluid at critical pressure (Pc) of 72.7 atm and critical temperature (Tc) of 31°C. Considering the criteria mentioned earlier, there is a possibility that liquid CO2 or supercritical carbon dioxide (SC-CO2) can be used as a cooling agent in a lyophilizer and extraction solvent in SCFE. This review presents a brief outline for the possible validation parameters of the proposed novel processor; that is, SCFE/Dryer combo instrument containing Design Qualification, Installation Qualification, Operational Qualification, and Performance Qualification.","PeriodicalId":8586,"journal":{"name":"Assay and drug development technologies","volume":"21 3","pages":"126-136"},"PeriodicalIF":1.8,"publicationDate":"2023-04-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"9566772","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

引用次数: 1

Oral Gastroretentive Film of Lacidipine for the Treatment of Gastroparesis. 口服拉西地平胃保留膜治疗胃轻瘫。

IF 1.8 4区医学

Assay and drug development technologies Pub Date : 2023-04-01 DOI: 10.1089/adt.2022.091

Mrunali Navin Kantak, Lalit Kumar, Prashant Jivaji Bhide, Rupesh Kalidas Shirodkar

{"title":"Oral Gastroretentive Film of Lacidipine for the Treatment of Gastroparesis.","authors":"Mrunali Navin Kantak, Lalit Kumar, Prashant Jivaji Bhide, Rupesh Kalidas Shirodkar","doi":"10.1089/adt.2022.091","DOIUrl":"https://doi.org/10.1089/adt.2022.091","url":null,"abstract":"The research work was aimed to formulate and evaluate gastroretentive mucoadhesive film of calcium channel blocker, Lacidipine for treatment of gastroparesis. Box-Behnken design was used for preparation of optimized formulation using solvent casting method. In this design, different concentrations of mucoadhesive polymers HPMC E15, Eudragit RL100, and Eudragit RS100 were considered as independent variables and its effect on responses like percent drug release, swelling index at 12 h, and folding endurance of the film were examined. Drug and polymer compatibility studies were performed using Fourier transform infrared spectroscopy and differential scanning calorimetry. Optimized formulation was evaluated for organoleptic properties, weight variation, thickness, swelling index, folding endurance, drug content, tensile strength, percent elongation, drug release, and percent moisture loss. The results revealed that the film possessed considerable flexibility and smoothness, and in vitro drug release was found to be 95.22% ± 0.93% at the end of 12 h. Scanning electron microscopy imaging of film displayed smooth, uniform, and porous surface texture. The dissolution followed Higuchi's model and Hixson Crowell model displayed non-Fickian drug release mechanism. Furthermore, the film was incorporated in capsule and the presence of capsule showed no effect on the drug release profile. In addition, no change was observed in the appearance, drug content, swelling index, folding endurance, and drug release upon storage at 25°C ± 2°C and 60% ± 5% relative humidity for 3 months. Collectively, the study revealed that gastroretentive mucoadhesive film of Lacidipine could serve as an effective and alternate site-specific targeted delivery in the management of gastroparesis.","PeriodicalId":8586,"journal":{"name":"Assay and drug development technologies","volume":"21 3","pages":"97-109"},"PeriodicalIF":1.8,"publicationDate":"2023-04-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"9566760","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

引用次数: 0

Identification of Potent, Selective, and Peripherally Restricted Serotonin Receptor 2B Antagonists from a High-Throughput Screen. 通过高通量筛选鉴定强效、选择性和外周限制性羟色胺受体 2B 拮抗剂

IF 1.6 4区医学

Assay and drug development technologies Pub Date : 2023-04-01 Epub Date: 2023-03-17 DOI: 10.1089/adt.2022.116

Aaron M Bender, Michael S Valentine, Joshua A Bauer, Emily Days, Craig W Lindsley, W David Merryman

引用次数: 0

Pharmaceutical Methods for Enhancing the Dissolution of Poorly Water-Soluble Drugs. 提高难水溶性药物溶出度的药学方法。

IF 1.8 4区医学

Assay and drug development technologies Pub Date : 2023-02-01 DOI: 10.1089/adt.2022.119

Tahir Mahmood, Rai M Sarfraz, Asmara Ismail, Muhammad Ali, Abdur Rauf Khan

{"title":"Pharmaceutical Methods for Enhancing the Dissolution of Poorly Water-Soluble Drugs.","authors":"Tahir Mahmood, Rai M Sarfraz, Asmara Ismail, Muhammad Ali, Abdur Rauf Khan","doi":"10.1089/adt.2022.119","DOIUrl":"https://doi.org/10.1089/adt.2022.119","url":null,"abstract":"\u0000 Low water solubility is the main hindrance in the growth of pharmaceutical industry. Approximately 90% of newer molecules under investigation for drugs and 40% of novel drugs have been reported to have low water solubility. The key and thought-provoking task for the formulation scientists is the development of novel techniques to overcome the solubility-related issues of these drugs. The main intention of present review is to depict the conventional and novel strategies to overcome the solubility-related problems of Biopharmaceutical Classification System Class-II drugs. More than 100 articles published in the last 5 years were reviewed to have a look at the strategies used for solubility enhancement. pH modification, salt forms, amorphous forms, surfactant solubilization, cosolvency, solid dispersions, inclusion complexation, polymeric micelles, crystals, size reduction, nanonization, proliposomes, liposomes, solid lipid nanoparticles, microemulsions, and self-emulsifying drug delivery systems are the various techniques to yield better bioavailability of poorly soluble drugs. The selection of solubility enhancement technique is based on the dosage form and physiochemical characteristics of drug molecules.\u0000 ","PeriodicalId":8586,"journal":{"name":"Assay and drug development technologies","volume":"21 2","pages":"65-79"},"PeriodicalIF":1.8,"publicationDate":"2023-02-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"9512702","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

引用次数: 0

Drug Repurposing Patent Applications October-December 2022. 药物再利用专利申请2022年10月至12月。

IF 1.8 4区医学

Assay and drug development technologies Pub Date : 2023-02-01 DOI: 10.1089/adt.2023.008

Hermann A M Mucke

引用次数: 0