Assay and drug development technologies最新文献

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Formulation Design, Optimization, and In Vitro Evaluation of Palbociclib-Loaded Polymeric Nanoparticles. 帕博西尼负载聚合物纳米颗粒的配方设计、优化及体外评价。
IF 1.8 4区 医学
Assay and drug development technologies Pub Date : 2026-05-01 Epub Date: 2026-03-10 DOI: 10.1177/1540658X261429246
Nurjamal Hoque, Ananta Choudhury
{"title":"Formulation Design, Optimization, and <i>In Vitro</i> Evaluation of Palbociclib-Loaded Polymeric Nanoparticles.","authors":"Nurjamal Hoque, Ananta Choudhury","doi":"10.1177/1540658X261429246","DOIUrl":"10.1177/1540658X261429246","url":null,"abstract":"<p><p>\u0000 <i>Palbociclib (PLB), an advanced breast cancer drug, shows limited success in clinical scenarios due to toxicity and resistant antitumor activities. The article aimed at preparing folic acid-modified chitosan-based polymeric nanoparticles (PNS) for controlled and targeted release of PLB. PLB-loaded nanoparticles were prepared via solvent evaporation. Central composite design was adopted in optimizing the formulation, with concentration levels of chitosan and polyvinyl alcohol (PVA) making responses of size and zeta potential (ZP) its independent variables. Mean particle size (MPS) ranged from 376 to 412 nm, and ZP ranged from 29.87 to 36.76 mV. Quadratic models were significant for both responses (MPS: <i>F</i> = 9.81, <i>p</i> = 0.0128; ZP: <i>F</i> = 5.24, <i>p</i> = 0.0466), with a nonsignificant lack of fit, confirming model adequacy. Particle size was significantly influenced by chitosan and PVA quadratic terms, while ZP was primarily affected by PVA. Optimization predicted a formulation with 63.35 mg of chitosan, 20 mg of PVA, an MPS of 389.1 nm, and a ZP of 31.2 mV, closely matching experimental observations (MPS of 237.8 ± 1.76 nm and ZP of 32.09 ± 3.38 mV). Entrapment efficiency and drug loading were 81.21 ± 1.80% and 40.79 ± 1.98%, respectively. PLB-PNS exhibited sustained, pH-responsive release, releasing 70.48% at pH 5.4 and 50.77% at pH 7.4 at 12 h, while free drug released 97.20% and 91.52%, respectively, confirming controlled and tumor-microenvironment-responsive drug delivery. Drug release followed Korsmeyer-Peppas kinetics, indicating diffusion-controlled release. Scanning electron microscope analysis revealed smooth, spherical nanoparticles. These developed PLB-loaded nanoparticles were indicated as an attractive tumor microenvironment-responsive drug-delivery carrier system capable of achieving enhanced therapeutic outcomes in breast cancer therapy.</i>\u0000 </p>","PeriodicalId":8586,"journal":{"name":"Assay and drug development technologies","volume":" ","pages":"296-311"},"PeriodicalIF":1.8,"publicationDate":"2026-05-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"147389049","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
Neprilysin Inhibitor and Angiotensin Receptor Blocker Attenuate Ischemic Brain Injury: Unveiling the Kinin-Mediated Pathway. Neprilysin抑制剂和血管紧张素受体阻滞剂减轻缺血性脑损伤:揭示激肽介导的途径。
IF 1.8 4区 医学
Assay and drug development technologies Pub Date : 2026-05-01 Epub Date: 2026-03-10 DOI: 10.1177/1540658X261429243
Geetika Mehta, Monika Sachdeva, Abul Kalam Najmi
{"title":"Neprilysin Inhibitor and Angiotensin Receptor Blocker Attenuate Ischemic Brain Injury: Unveiling the Kinin-Mediated Pathway.","authors":"Geetika Mehta, Monika Sachdeva, Abul Kalam Najmi","doi":"10.1177/1540658X261429243","DOIUrl":"10.1177/1540658X261429243","url":null,"abstract":"<p><p>\u0000 <i>Kinin peptides play a key role in regulating blood vessel tone, renal function, and protection against ischemia-reperfusion injury. Neprilysin is one of the primary enzymes responsible for degrading several vasoactive peptides including bradykinin. Concurrent inhibition of neprilysin and angiotensin II receptors leads to elevated bradykinin levels by reducing its breakdown, potentially enhancing its interaction with bradykinin receptor complexes. It has therefore been hypothesized that increased bradykinin generation may contribute to the neuroprotective effect of neprilysin inhibitors and angiotensin receptor blockers against global cerebral ischemia-reperfusion injury (GCI/R). GCI/R was induced in mice by transient occlusion of bilateral common carotid arteries. A combination of Sacubitril/Valsartan (30/50 mg/kg and 60/100 mg/kg, PO) was administered for 7 days before subjecting to ischemia. Behavioral changes were assessed using the beam walk test for motor coordination and passive avoidance and Y-maze tests for spatial memory, which were further supported by biochemical and histopathological assessment. Our results demonstrated that prophylactic treatment with Sacubitril/Valsartan led to a dose-dependent improvement in neurological deficits, a reduction in oxidative stress and inflammation, and an increased number of intact neurons in the hippocampus and cortex of GCI/R mice. Interestingly, immunohistochemical analysis revealed upregulation of bradykinin B2 receptors accompanied by changes in eNOS and NFκB expression. However, coadministration of the bradykinin B2 receptor antagonist, Icatibant, attenuated the neuroprotective effects of Sacubitril/Valsartan. Our findings suggest that the neuroprotective effects of Sacubitril/Valsartan may be mediated by the endogenous accumulation of vasodilatory bradykinin. Thus, concurrent inhibition of neprilysin and angiotensin II receptors represents a promising therapeutic target for stroke management.</i>\u0000 </p>","PeriodicalId":8586,"journal":{"name":"Assay and drug development technologies","volume":" ","pages":"312-322"},"PeriodicalIF":1.8,"publicationDate":"2026-05-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"147389136","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
Spatiotemporal Nanocarriers for Circadian-Aligned Drug Delivery: Advances, Challenges, and Future Directions. 时空纳米载体用于昼夜节律药物递送:进展、挑战和未来方向。
IF 1.8 4区 医学
Assay and drug development technologies Pub Date : 2026-04-01 Epub Date: 2026-01-13 DOI: 10.1177/1540658X251410476
Dilpreet Singh, Akshay Thakur
{"title":"Spatiotemporal Nanocarriers for Circadian-Aligned Drug Delivery: Advances, Challenges, and Future Directions.","authors":"Dilpreet Singh, Akshay Thakur","doi":"10.1177/1540658X251410476","DOIUrl":"10.1177/1540658X251410476","url":null,"abstract":"<p><p>Circadian rhythms orchestrate a wide array of physiological processes that critically influence drug absorption, distribution, metabolism, and excretion. Misalignment between drug administration and biological timing can compromise therapeutic efficacy, increase adverse effects, and lead to therapeutic failure in diseases with established diurnal variation. Chronotherapy seeks to align pharmacologic interventions with these endogenous rhythms; however, traditional drug delivery systems lack the ability to adapt dynamically to circadian cues. Recent advances in nanotechnology have enabled the development of spatiotemporal nanocarrier systems capable of both anatomical targeting and time-synchronized drug release. These smart nanocarriers leverage internal stimuli (<i>e.g.</i>, pH, redox state, enzyme activity) or external triggers (<i>e.g.</i>, light, temperature, magnetic fields) to optimize therapeutic action at specific circadian windows. This review provides a comprehensive analysis of circadian biology relevant to drug delivery, current clinical applications of chronotherapy, and emerging preclinical evidence for chrono-responsive nanosystems, enabling technologies such as wearable biosensors, organ-on-chip platforms, and artificial intelligence. We also discuss the translational barriers and future directions in realizing patient-specific, feedback-controlled chrono-nanomedicine. The convergence of circadian pharmacology and intelligent nanocarrier design represents a transformative approach toward achieving precision medicine that targets not only the right site but also the right time.</p>","PeriodicalId":8586,"journal":{"name":"Assay and drug development technologies","volume":"24 3","pages":"189-205"},"PeriodicalIF":1.8,"publicationDate":"2026-04-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"147670151","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
Terpenes Encapsulated Polycaprolactone Nanoparticles for Topical Delivery of Hydrocortisone: In Vitro Study and In Vivo Appraisal. 萜烯封装的聚己内酯纳米颗粒局部递送氢化可的松:体外研究和体内评价。
IF 1.8 4区 医学
Assay and drug development technologies Pub Date : 2026-04-01 Epub Date: 2026-01-13 DOI: 10.1177/1540658X251410481
Khaled Shalaby, Mohammed Elmowafy, Mohammed H Elkomy, Omar Awad Alsaidan, Mohamed A Abdelgawad, Ehab M Mostafa, Ayman Salama, Abdulsalam M Kassem, Mohamed F Ibrahim
{"title":"Terpenes Encapsulated Polycaprolactone Nanoparticles for Topical Delivery of Hydrocortisone: <i>In Vitro</i> Study and <i>In Vivo</i> Appraisal.","authors":"Khaled Shalaby, Mohammed Elmowafy, Mohammed H Elkomy, Omar Awad Alsaidan, Mohamed A Abdelgawad, Ehab M Mostafa, Ayman Salama, Abdulsalam M Kassem, Mohamed F Ibrahim","doi":"10.1177/1540658X251410481","DOIUrl":"10.1177/1540658X251410481","url":null,"abstract":"<p><p>This work aimed to develop and assess terpene encapsulated polycaprolactone (PCL) nanoparticles for topical delivery of hydrocortisone (HC). Formulations were designed to investigate the effect of terpene/PCL ratio and concentration of surfactant on physicochemical characteristics. Structural analyses were studied using differential scanning calorimetry (DSC) and Fourier-transform infrared spectroscopy techniques. <i>Ex vivo</i> skin permeation and anti-inflammatory activity of HC were also appraised. Results showed that the physicochemical characteristics were particularly influenced by terpene/PCL ratio and concentration of surfactant. The selected formulation (F6) showed core-shell structure and good encapsulation of HC in less crystalline state. Higher skin flux (366.11 ± 32.8 µg/cm<sup>2</sup>/h) and permeability coefficient (17.57 ± 2.6 × 10<sup>2</sup> cm/h) of HC from gel based on F6 were observed when compared with crude drug gel. Anti-inflammatory activity of HC was significantly improved and showed sustained therapeutic action when using gel based on F6. Collectively, these findings suggest that terpene encapsulated PCL nanoparticles can potentially deliver HC through the skin.</p>","PeriodicalId":8586,"journal":{"name":"Assay and drug development technologies","volume":"24 3","pages":"237-249"},"PeriodicalIF":1.8,"publicationDate":"2026-04-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"147670068","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 Kir2.1 Inhibitors from a High-Throughput Screen. 高通量筛选鉴定Kir2.1抑制剂
IF 1.8 4区 医学
Assay and drug development technologies Pub Date : 2026-04-01 Epub Date: 2026-02-17 DOI: 10.1177/1540658X261415763
Jacob L Bouchard, Pedro de Andrade Horn, Yu Nishio, Emily L Days, Liangping Li, Roman M Lazarenko, Snehal Sant, Sichen Chang, Joshua A Bauer, Jerod S Denton, Olivier Boutaud, Masahito Abe, Craig W Lindsley
{"title":"Identification of Kir2.1 Inhibitors from a High-Throughput Screen.","authors":"Jacob L Bouchard, Pedro de Andrade Horn, Yu Nishio, Emily L Days, Liangping Li, Roman M Lazarenko, Snehal Sant, Sichen Chang, Joshua A Bauer, Jerod S Denton, Olivier Boutaud, Masahito Abe, Craig W Lindsley","doi":"10.1177/1540658X261415763","DOIUrl":"10.1177/1540658X261415763","url":null,"abstract":"<p><p>The inward-rectifier potassium channel (Kir) 2.x family is an important family of ion channels in the context of human health. These potassium channels are involved in processes such as cardiac action potential, formation of skeletal muscle, bone development, vasodilation, and neuronal activity and are expressed centrally and peripherally. Given their importance, they are an attractive target for the development of tool compounds. The high homology between the members of the Kir family has made isoform selectivity challenging. In an effort to discover novel chemical matter related to this intriguing target, we performed a high-throughput screen utilizing compounds from the Vanderbilt Institute of Chemical Biology Discovery Collection. This screen of over 20,000 compounds resulted in 48 verified hits consisting of six novel chemical scaffolds. Of these hits, VU0523203 and VU0606851 were selected as promising starting points for initial medicinal chemistry optimization to improve potency and distribution, metabolism, and pharmacokinetic (DMPK) properties. These efforts resulted in the discovery of VU6073995, a compound with modest potency at Kir2.1 and improved DMPK properties compared with ML133.</p>","PeriodicalId":8586,"journal":{"name":"Assay and drug development technologies","volume":" ","pages":"265-273"},"PeriodicalIF":1.8,"publicationDate":"2026-04-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC13535541/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"146212059","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Network Pharmacology Combined with Experimental Validation to Investigate the Mechanism of Huxinkang Tablets in Treating Atherosclerosis by Modulating Macrophages. 网络药理学结合实验验证探讨护心康片调节巨噬细胞治疗动脉粥样硬化的作用机制。
IF 1.8 4区 医学
Assay and drug development technologies Pub Date : 2026-04-01 Epub Date: 2026-01-13 DOI: 10.1177/1540658X251404889
Zhengke Yu, Guobing Zhou, Kaili Wang, Qi Zhao, Xiaojing Zhu, Wenbo Zhao, Zhihong Chen
{"title":"Network Pharmacology Combined with Experimental Validation to Investigate the Mechanism of Huxinkang Tablets in Treating Atherosclerosis by Modulating Macrophages.","authors":"Zhengke Yu, Guobing Zhou, Kaili Wang, Qi Zhao, Xiaojing Zhu, Wenbo Zhao, Zhihong Chen","doi":"10.1177/1540658X251404889","DOIUrl":"10.1177/1540658X251404889","url":null,"abstract":"<p><p>Huxinkang tablets (HXKT) is the formula prescription of Traditional Chinese Medicine for treating atherosclerosis (AS), but its underlying mechanisms remain unclear. Network pharmacology and experimental verification were integrated to explore the therapeutic effects and key targets of HXKT in macrophage-associated genes in vulnerable AS plaques. Our findings indicated that a total of 75 candidate targets of HXKT against vulnerable AS were acquired. Furthermore, five core targets were identified including STAT3, HIF1A, EGFR, ESR1, and BCL2. KEGG pathway analysis demonstrated that these targets participated in the advanced glycation end product - receptor for advanced glycation end-product (AGE-RAGE) signaling pathway associated with diabetic complications, lipid metabolism, AS, and human cytomegalovirus infection. Molecular docking results indicated that the ESR1-miltirone complex exhibited the highest binding affinity. <i>In vitro</i> experiments demonstrated that HXKT inhibited oxidized low-density lipoprotein-induced macrophage injury, reversed abnormal expression of key targets, and reduced inflammation and lipid accumulation. Overexpression of STAT3 partially attenuated the protective effects of HXKT, confirming its role as a critical target while underscoring the multi-target mechanism of HXKT. In conclusion, HXKT stabilizes vulnerable atherosclerotic plaques by regulating macrophage function through a multi-component, multi-target mechanism, with STAT3 signaling playing a pivotal role.</p>","PeriodicalId":8586,"journal":{"name":"Assay and drug development technologies","volume":"24 3","pages":"216-227"},"PeriodicalIF":1.8,"publicationDate":"2026-04-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"147670094","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
Computational Prediction and In Vitro Validation of Potential Molecular Targets Associated with Adverse Reactions of Antimicrobial Drugs in Neonates. 新生儿抗菌药物不良反应相关潜在分子靶点的计算预测和体外验证。
IF 1.8 4区 医学
Assay and drug development technologies Pub Date : 2026-04-01 Epub Date: 2026-04-14 DOI: 10.1177/1540658X251413074
Xiaojuan He, Rui Jing, Na Wu, Xiaojing Li, Shasha Qiao, Zhaojuan Yang, Ying Zhang, Yuanyuan Han
{"title":"Computational Prediction and <i>In Vitro</i> Validation of Potential Molecular Targets Associated with Adverse Reactions of Antimicrobial Drugs in Neonates.","authors":"Xiaojuan He, Rui Jing, Na Wu, Xiaojing Li, Shasha Qiao, Zhaojuan Yang, Ying Zhang, Yuanyuan Han","doi":"10.1177/1540658X251413074","DOIUrl":"10.1177/1540658X251413074","url":null,"abstract":"<p><p>Neonates are particularly susceptible to a range of adverse reactions when administered antimicrobial drugs, including allergic reactions, gastrointestinal discomfort, and hepatic or renal dysfunction. These adverse reactions can have significant long-term impacts on neonatal health. This study aimed to investigate the common molecular targets associated with these adverse reactions using reverse target identification and molecular dynamics (MD) simulations, and to experimentally assess the inhibitory effects of selected drugs on these targets. We initially identified adverse reactions associated with commonly used antimicrobial drugs such as Ceftazidime, Meropenem, Levofloxacin, Cefdinir, and Avibactam through DrugBank. Potential targets for these drugs were predicted using SwissTargetPrediction software, and common targets were identified using a Venn diagram. Molecular docking and MD simulations were conducted to assess the binding affinity and stability of the drug-target interactions. Finally, the inhibitory potential of selected antimicrobial drugs on the target proteins was evaluated through <i>in vitro</i> bioactivity assays. The study identified AKR1B1 and Neprilysin as common potential off-targets. Bioactivity assays confirmed that the tested antimicrobial drugs exhibited significant inhibitory effects on these two proteins, with inhibitory concentration at 50% (IC<sub>50</sub>) values generally in the micromolar range. MD simulations indicated that the complexes of these drugs with the target proteins maintained relatively stable root mean square deviation (RMSD) values throughout the simulation period. Analysis of intermolecular forces revealed key attractive charge interactions and hydrogen bonds between the drugs and target proteins. This study systematically analyzed the molecular targets associated with antimicrobial drug adverse reactions in neonates by integrating computational and experimental approaches. The findings suggest that these drugs may cause adverse reactions by affecting the function of specific off-target proteins. This discovery provides valuable molecular insights into the mechanisms of adverse reactions and establishes a scientific basis for the rational design of safer drug analogs and for informing future antimicrobial treatment research for neonates.</p>","PeriodicalId":8586,"journal":{"name":"Assay and drug development technologies","volume":"24 3","pages":"250-264"},"PeriodicalIF":1.8,"publicationDate":"2026-04-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"147670157","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
Ultrafast Detection of Environmental Pollutants and Pharmaceutical Residues Using a CuFe Nanozyme-Enhanced Sensing Platform. 利用CuFe纳米酶增强传感平台超快检测环境污染物和药物残留。
IF 1.7 4区 医学
Assay and drug development technologies Pub Date : 2026-04-01 Epub Date: 2025-09-11 DOI: 10.1177/1540658X251378353
Dilpreet Singh
{"title":"Ultrafast Detection of Environmental Pollutants and Pharmaceutical Residues Using a CuFe Nanozyme-Enhanced Sensing Platform.","authors":"Dilpreet Singh","doi":"10.1177/1540658X251378353","DOIUrl":"10.1177/1540658X251378353","url":null,"abstract":"<p><p>The aim of this study was to develop a novel CuFe nanozyme-enhanced sensing platform for the ultrafast detection of trace analytes, specifically targeting environmental pollutants and heavy metals. The objectives of the research included evaluation of the platform's sensitivity, selectivity, and real-world applicability for detecting trace analytes in environmental and biological samples. We synthesized the CuFe nanozyme using a co-precipitation method with metal-organic precursors and a reducing agent. The sensing platform was fabricated using conductive electrodes and immobilized nanozymes. The turnover frequency was calculated under optimized conditions (e.g., temperature, pH, and substrate concentration). Equipment utilized included an X-ray diffraction analyzer, transmission electron microscope, electrochemical workstation, and UV-Vis spectrophotometer. This CuFe nanozyme demonstrated a turnover frequency of 125 s<sup>-1</sup>, 3.5 times higher than natural peroxidase enzymes, as determined using a colorimetric assay with 3,3',5,5'-Tetramethylbenzidine. The sensing platform exhibited ultrafast detection with a response time of 5 s, determined through real-time monitoring of analyte interaction via the electrochemical method. The detection limit was established at 0.1 nM for target analytes, as measured by the electrochemical method with calibration curves constructed for each analyte in the concentration range of [0.1 nM-X nM]. Importantly, the system was successfully validated in real-world environmental water samples and spiked clinical fluids, showing high recovery rates (98%-102%). The CuFe nanoenzyme-based electrochemical sensing platform demonstrated high accuracy, precision, and recovery in environmental water and spiked biological fluid samples. This study presents a robust, ultrafast nanozyme-based sensing platform with superior sensitivity and selectivity.</p>","PeriodicalId":8586,"journal":{"name":"Assay and drug development technologies","volume":" ","pages":"206-215"},"PeriodicalIF":1.7,"publicationDate":"2026-04-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"145032717","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
Building a State-of-the-Art Automation Platform to Support High-Throughput 96-Well Caco-2 Permeability Assay. 建立最先进的自动化平台,支持高通量96井Caco-2渗透率测定。
IF 1.7 4区 医学
Assay and drug development technologies Pub Date : 2026-04-01 Epub Date: 2025-12-26 DOI: 10.1177/1540658X251408742
Xianmei Cai, Gregory Barker, Shivani Patel, Anthony Paiva, Yongnian Sun, Chunli Huang, David Connors, Peter Chase, Nicole Diaz, Mary Ellen Cvijic, Wilson Shou
{"title":"Building a State-of-the-Art Automation Platform to Support High-Throughput 96-Well Caco-2 Permeability Assay.","authors":"Xianmei Cai, Gregory Barker, Shivani Patel, Anthony Paiva, Yongnian Sun, Chunli Huang, David Connors, Peter Chase, Nicole Diaz, Mary Ellen Cvijic, Wilson Shou","doi":"10.1177/1540658X251408742","DOIUrl":"10.1177/1540658X251408742","url":null,"abstract":"<p><p><i>Automation plays a crucial role in enhancing efficiency and increasing capacity for <i>in vitro</i> absorption, distribution, metabolism, and excretion profiling in early drug discovery. Building an automation platform requires a careful balance of innovation and practical considerations to align assay needs with technological capabilities. In this study, we present a state-of-the-art automation system designed to support the miniaturization of the Caco-2 permeability assay from the 24-well to the 96-well format. This platform integrates advanced infrastructure for cell culture and assay execution, along with several key features, including innovative cleaning protocols, cutting-edge plate tracking, and dynamic scheduling capabilities. The fully automated 96-well platform delivers significant efficiency gains, increased capacity, and faster turnaround for permeability assay support while maintaining high predictive accuracy. It correctly classified 94% of 50 literature compounds, demonstrating strong concordance with the established 24-well format. Moreover, the platform enables large-scale permeability data generation, advancing our \"predict-first\" modeling paradigm, in which predictive models guide experimental design and compound prioritization</i>.</p>","PeriodicalId":8586,"journal":{"name":"Assay and drug development technologies","volume":" ","pages":"228-236"},"PeriodicalIF":1.7,"publicationDate":"2026-04-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"145861907","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
Reversed-Phase High-Performance Liquid Chromatography Assisted Simultaneous Estimation and Validation as per ICHQ2(R2) Guidelines: Application of Method in Quantification of Paclitaxel and Berberine in Liposomes-Based Delivery System. 根据ICHQ2(R2)指南:应用反相高效液相色谱法定量脂质体中紫杉醇和小檗碱的含量。
IF 1.7 4区 医学
Assay and drug development technologies Pub Date : 2026-03-01 Epub Date: 2025-08-13 DOI: 10.1177/1540658X251365254
Debanjan Mukherjee, Raj Kamal, Akshay Kumar Lunawat, Tarun Sharma, Nitish Kumar, Ankit Awasthi, Shubham Thakur
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