Assay and drug development technologies最新文献

{"title":"Precision Targeting in Gastric Cancer: AI-Driven Discovery of MET, ADORA2A, CDK5R1, and ADORA1.","authors":"Tiantian Tuo, Mengchan Wang","doi":"10.1177/1540658X251372072","DOIUrl":"10.1177/1540658X251372072","url":null,"abstract":"<p><p>In this study, we integrated computational and experimental approaches to identify novel therapeutic targets and candidate compounds for gastric cancer (GC). Through <i>in silico</i> analyses, including target prediction, pathway enrichment, and molecular docking, four key proteins-MET, ADORA2A, CDK5R1, and ADORA1-were identified as critical regulators of tumor proliferation, metastasis, and drug resistance pathways (e.g., Semaphorin interactions and NTRK1 signaling). Molecular docking and dynamics simulations revealed strong binding affinities and structural stability between selected compounds and these targets, prioritizing ADORA1 as a promising therapeutic node. To validate these findings, we synthesized compound 3 via a two-step chemical route, yielding a white solid product with 63% overall efficiency. Structural characterization by High-Resolution Mass Spectrometry (HRMS) and ¹H Nuclear Magnetic Resonance (NMR) confirmed its identity. <i>In vitro</i> inhibition assays demonstrated that compound 3 exhibited potent activity against ADORA1, with a mean Half-Maximal Inhibitory Concentration (IC₅₀) of 0.23 nM-approximately twofold more effective than the positive control antagonist Dipropylcyclopentylxanthine (DPCPX) (IC₅₀ = 0.46 nM). These results highlight compound 3 as a promising lead compound for further development in GC therapy, with potential to modulate ADORA1-mediated signaling pathways.</p>","PeriodicalId":8586,"journal":{"name":"Assay and drug development technologies","volume":" ","pages":"149-164"},"PeriodicalIF":1.7,"publicationDate":"2026-03-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"145032701","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}

{"title":"Advances in Capsaicin-Based Nanocarriers: Bridging Mechanistic Insights with Therapeutic Potential and Clinical Outcomes.","authors":"Kiran Patil, Meghanath B Shete, Tulshidas Patil, Harshada Mahajan, Tejas Mahajan, Nilakshi Maind, Rohan Mehta, Yogeeta Agrawal, Sameer Goyal, Abdulla Sherikar","doi":"10.1177/1540658X251366755","DOIUrl":"10.1177/1540658X251366755","url":null,"abstract":"<p><p>Capsaicin (CAP), a bioactive compound from chili peppers, possesses a wide range of therapeutic properties, including antiobesity, anticancer, anti-inflammatory, analgesic, and cardioprotective effects. However, its clinical application has been limited due to poor aqueous solubility, low bioavailability, rapid metabolism, and potential side effects with high doses. Recent advancements in nanotechnology have addressed these challenges by enhancing CAP's solubility, stability, and targeted delivery through innovative nanoformulations. This review provides an in-depth analysis of various nanocarrier systems such as solid lipid nanoparticles, nanostructured lipid carriers, liposomes, polymeric nanoparticles, nanoemulsions, and nanocrystals, all of which have demonstrated improved therapeutic efficacy of CAP in preclinical studies. These nanoformulations not only protect CAP from degradation but also enable controlled release, reduce side effects, and improve patient compliance. The therapeutic potential of CAP-loaded nanocarriers has been investigated in a variety of diseases, including cancer, neurodegenerative disorders, and chronic pain, with promising results. This review highlights the latest innovations in CAP nanotechnology and discusses the future directions for clinical applications, paving the way for more effective CAP-based therapies in modern medicine.</p>","PeriodicalId":8586,"journal":{"name":"Assay and drug development technologies","volume":" ","pages":"85-112"},"PeriodicalIF":1.7,"publicationDate":"2026-03-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"144940306","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}

{"title":"Identification of Selective Small Molecule Modulators of mRNA Processing Using a Multiplexed QuantiGene High-Throughput Screening Platform.","authors":"Sarah Sirin, Nirodhini S Siriwardana, Michael Wood, James Mills, Dominic J Reynolds, Frédéric H Vaillancourt","doi":"10.1177/1540658X251366782","DOIUrl":"10.1177/1540658X251366782","url":null,"abstract":"<p><p>High-throughput screening (HTS) approaches incorporating multiplexed, cell-based assays are increasingly common for identifying novel modulators of complex biological processes. To enable the discovery of small molecule modulators of mRNA processing, we developed a multiplexed, bead-based, high-throughput QuantiGene assay, leveraging the Luminex platform that is capable of simultaneously quantifying transcript levels of multiple independent target genes within a single HTS campaign. To address plate variability and potential screening artifacts, a pragmatic hit-calling pipeline was implemented utilizing both plate- and well-based normalization strategies. This dual-normalization approach reduced false negatives and produced consistent hit confirmation rates. Application of this methodology led to the identification of unique compounds selectively modulating individual target genes. Strikingly, among the three exemplary genes, only 5% of primary actives demonstrated activity across all three target genes, underscoring the assay's capacity for detecting selective mRNA modulators. Chemical motif analysis of confirmed actives recovered known RNA privileged scaffolds as well as novel scaffolds that are uniquely enriched for individual targets screened. Validation screening using an orthogonal, four-point concentration-response real-time PCR (qPCR) assay in a disease-relevant cell line demonstrated high validation rates, supporting the robustness and translational relevance of this multiplexed HTS platform. These findings establish a scalable and reliable strategy for identifying selective small molecule modulators of mRNA processing, with broad applicability in early drug discovery.</p>","PeriodicalId":8586,"journal":{"name":"Assay and drug development technologies","volume":" ","pages":"138-148"},"PeriodicalIF":1.7,"publicationDate":"2026-03-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"144940350","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}

{"title":"Validation of an Reverse Phase High Performance Liquid Chromatography Method for <i>In Vitro</i> Quantification and Degradation Analysis of Naphthol AS-E Phosphate in Bulk Drugs and Nanoparticles.","authors":"Kangkan Sarma, Md Habban Akhter, Maha Alsunbul, Abdul-Hamid Emwas, Mariusz Jaremko","doi":"10.1177/1540658X251377978","DOIUrl":"10.1177/1540658X251377978","url":null,"abstract":"<p><p>\u0000 <i>This study presents the first validated High-performance liquid chromatography (HPLC) technique for quantifying naphthol AS-E phosphate (NASEP) in bulk drugs and nanoparticle formulation. A C18 HPLC cartridge (250 × 4.6 mm, 5 µm particle size) served as the stationary phase for quantification. The mobile phase consisted of Milli-Q water with 0.1% trifluoroacetic acid (TFA) in pump A and acetonitrile with 0.1% TFA in pump B, with a flow rate ranging from 0.8 to 1.2 mL/min. A 3² factorial design was employed to evaluate the robustness of the proposed method, using mobile phase composition (X₁), flow rate (X₂), and column temperature (X₃) as independent variables and peak area (R₁), retention time (R₂), and percent recovery (R₃) as response variables. The calibration range curve (10-500 µg/mL) was best fitted by quadratic regression. The linearity was reported in the above-mentioned range. The accuracy was 99.952% ± 0.961% at the 75% level, 99.58% ± 1.483% at the 100% level, and 99.789% ± 1.936% at the 125% level. The coefficient of variation was below 2% for both intraday and interday measurements, and the limits of detection and quantification were 0.038 and 0.115 µg/mL, respectively. The NASEP solution was stable (99.04% ± 0.0251%) for 48 h at 8°C. The forced degradation study also revealed that the NASEP solution remained stable in an acidic environment for 48 h at 40°C but degraded at 80°C (<i>p</i> < 0.046) in a time-dependent manner. In contrast, it was unstable in an alkaline medium, independent of temperature, and degraded in the presence of strong oxidizing agents (<i>p</i> < 0.039). Furthermore, NASEP encapsulated in a Gly-Arg-Gly-Asp-Ser pentapeptide and low-molecular-weight heparin functionalized metal-organic framework exhibited sustained drug release at acidic pH 5.4. The proposed NASEP quantification method was validated and is suitable for routine analysis in pharmaceutical formulations.</i>\u0000 </p>","PeriodicalId":8586,"journal":{"name":"Assay and drug development technologies","volume":" ","pages":"165-182"},"PeriodicalIF":1.7,"publicationDate":"2026-03-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"145079574","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}

{"title":"Nanoengineering of Exosomal Surfaces for Precision Targeting and Payload Delivery at the Molecular Level.","authors":"Dilpreet Singh, Satvir Singh, Nitin Tandon","doi":"10.1177/1540658X251369691","DOIUrl":"10.1177/1540658X251369691","url":null,"abstract":"<p><p>Exosomes, nano-sized extracellular vesicles secreted by almost all cell types, have emerged as biologically compatible vehicles for targeted drug delivery, gene therapy, and molecular diagnostics. Their innate ability to traverse biological barriers and deliver diverse cargoes with minimal immunogenicity has catalyzed intense interest in their therapeutic exploitation. However, the intrinsic heterogeneity and limited targeting specificity of native exosomes necessitate advanced engineering strategies to fulfill their clinical potential. This review focuses on the molecular-level nanoengineering of exosomal surfaces to enhance specificity, loading efficiency, and release control of therapeutic payloads. We systematically examine current methodologies, including genetic modification of parental cells, covalent and non-covalent surface conjugation, lipid insertion, click chemistry, and hybrid vesicle fusion. We further detail the quantitative performance of targeting ligands-such as peptides, aptamers, nanobodies, and glycans-in relation to receptor affinity, conjugation efficiency, and biological outcomes. Payload loading techniques, both endogenous and exogenous, are critically analyzed based on loading yield and membrane preservation. Additionally, we highlight disease-specific applications in oncology, neurology, cardiology, and immunotherapy, supported by preclinical and translational case studies. Emerging technologies such as microfluidics, synthetic biology, artificial intelligence-guided modeling, and multi-omics are discussed as integral components of the next generation of precision exosome platforms. Finally, we address key challenges related to scalability, regulatory frameworks, and standardization. This review provides a comprehensive and quantitative framework to guide the design of molecularly engineered exosomes for future translational and clinical success.</p>","PeriodicalId":8586,"journal":{"name":"Assay and drug development technologies","volume":" ","pages":"113-125"},"PeriodicalIF":1.7,"publicationDate":"2026-03-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"144990956","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}

{"title":"Neuroprotective Potential of Saroglitazar Against Cerebral Ischemia/Reperfusion Injury in Sprague Dawley Rats: Targeting HMGB-1/NF-κB Pathway.","authors":"Prachi Mistry, Sanjiv Prajapati, Paridhi Vadher, Jhanvi Soni, Vijay Kevlani","doi":"10.1177/1540658X251370044","DOIUrl":"10.1177/1540658X251370044","url":null,"abstract":"<p><p>Stroke is an intricate oxidative and inflammatory response resulting from cerebral ischemia followed by reperfusion injury. The complex pathophysiology of stroke poses challenges for treatment. Peroxisome proliferated-activated receptor (PPAR) expression in the rat hippocampus is markedly elevated post cerebral ischemia/reperfusion injury (I/R injury). Hence, Saroglitazar, a dual PPAR-α/γ agonist, was investigated against cerebral I/R injury in rats. Male Sprague Dawley rats were subjected to bilateral common carotid artery occlusion for 30 min and reperfusion for 3 days. During the reperfusion, animals were treated with vehicle or Saroglitazar once a day for 3 days. The behavioral parameters were assessed, and animals were sacrificed to measure oxidative markers (Malondialdehyde, Superoxide dismutase, catalase, and reduced glutathione), inflammatory markers (interleukin-6, tumor necrosis factor-α, nuclear factor kappa-light chain enhancer of activated B cells [NF-κB], and high mobility group box 1 protein [HMGB-1]), infarction, and histopathology changes. Following I/R injury, antioxidant enzymes were reduced, while nitric oxide and inflammatory markers were increased in the disease group. In the rat hippocampus, these changes led to neurobehavioral impairment and cerebral infarction. Saroglitazar improved the levels of antioxidants and reduced inflammation. 2,3,5-triphenyltetrazolium chloride staining and histopathological analysis revealed the neuroprotective effect of Saroglitazar in the hippocampus region. The neuroprotective effects of Saroglitazar were attributed to its activation of both PPAR-α and PPAR-γ. It improved antioxidant levels and inhibited pro-inflammatory cytokines by suppressing the HMGB-1/NF-κB signaling pathway. These findings underscore the potential of Saroglitazar in mitigating cerebral I/R injury.</p>","PeriodicalId":8586,"journal":{"name":"Assay and drug development technologies","volume":" ","pages":"1540658X251370044"},"PeriodicalIF":1.7,"publicationDate":"2026-02-19","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"144940463","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}

{"title":"Recent Trends in Drug Delivery Systems.","authors":"Omnia Mohamed Sarhan","doi":"10.1089/adt.2025.031","DOIUrl":"10.1089/adt.2025.031","url":null,"abstract":"<p><p>Drug delivery systems are now being advanced by integrating sophisticated nanotechnologies to enhance therapeutic efficacy. Tremendous advancement has been achieved in the field of cancer therapy through the utilization of hyaluronic acid-based nanocarriers, which are well-acknowledged for their capacity to transport medication precisely to targeted regions. Quantum dots exhibit unique optical properties that allow for precise drug administration and monitoring capabilities. Carbon nanotubes provide a large surface area and exceptional strength, allowing for precise manipulation of drug delivery patterns. Dendrimers are versatile structures that can transport many drugs simultaneously, whereas mesoporous silica-functionalized nanoparticles allow exact manipulation of the release rate of pharmaceuticals. Polymer-lipid hybrid nanoparticles synergistically integrate the durability of polymers with the compatibility of lipids, hence augmenting the availability of drugs within the body. Hexagonal boron nitride nanosheets are becoming more recognized as favorable carriers due to their biocompatibility and potential for tailored administration. These achievements demonstrate the changes happening in the field of pharmaceutical administration, where nanotechnology is used to tackle issues such as restricted bioavailability and unanticipated adverse effects. This ultimately enhances the effectiveness of medicines and improves patient outcomes. Future investigations will focus on improving these technologies for broader therapeutic applications.</p>","PeriodicalId":8586,"journal":{"name":"Assay and drug development technologies","volume":" ","pages":"2-29"},"PeriodicalIF":1.8,"publicationDate":"2026-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143975336","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}

{"title":"Neuroprotective Potential of Saroglitazar Against Cerebral Ischemia/Reperfusion Injury in Sprague-Dawley Rats: Targeting HMGB-1/NF-κB Pathway.","authors":"Prachi Mistry, Sanjiv Prajapati, Paridhi Vadher, Jhanvi Soni, Vijay Kevlani","doi":"10.1089/adt.2025.057","DOIUrl":"10.1089/adt.2025.057","url":null,"abstract":"<p><p>Stroke is an intricate oxidative and inflammatory response resulting from cerebral ischemia followed by reperfusion injury. Complex pathophysiology of stroke poses challenges for treatment. Peroxisome proliferator-activated receptor (PPAR) expression in the rat hippocampus is markedly elevated post cerebral ischemia/reperfusion (I/R) injury. Hence, saroglitazar, a dual PPAR-α/γ agonist, was investigated against cerebral I/R injury in rats. Male Sprague-Dawley rats were subjected to bilateral common carotid artery occlusion for 30 min and reperfusion for 3 days. During the reperfusion, animals were treated with vehicle or saroglitazar once a day for 3 days. The behavioral parameters were assessed, and animals were sacrificed to measure oxidative markers (malondialdehyde, superoxide dismutase, catalase, and reduced glutathione), inflammatory markers (interleukin-6, tumor necrosis factor-α, nuclear factor kappa-light chain enhancer of activated B cells (NF-κB), and high mobility group box 1 (HMGB-1) protein, infarction, and histopathology changes. Following I/R injury, antioxidant enzymes were reduced, while nitric oxide and inflammatory markers were increased in the disease group. In the rat hippocampus, these changes led to neurobehavioral impairment and cerebral infarction. Saroglitazar improved the levels of antioxidants and reduced inflammation; 2,3,5-triphenyltetrazolium chloride stain and histopathological analysis revealed the neuroprotective effect of saroglitazar in the hippocampus region. The neuroprotective effects of saroglitazar were attributed to its activation of both PPAR-α and PPAR-γ. It improved antioxidant levels and inhibited proinflammatory cytokines by suppressing the HMGB-1/NF-κB signaling pathway. These findings underscore the potential of saroglitazar in mitigating cerebral I/R injury.</p>","PeriodicalId":8586,"journal":{"name":"Assay and drug development technologies","volume":" ","pages":"65-80"},"PeriodicalIF":1.8,"publicationDate":"2026-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"144582937","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}

{"title":"One Year as Editor-in-Chief: Building on a New Chapter.","authors":"Kevin W-H Lo","doi":"10.1177/1540658X261420558","DOIUrl":"https://doi.org/10.1177/1540658X261420558","url":null,"abstract":"","PeriodicalId":8586,"journal":{"name":"Assay and drug development technologies","volume":"24 1","pages":"1"},"PeriodicalIF":1.7,"publicationDate":"2026-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"146206698","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}

{"title":"Development and Fabrication of Emodin-Loaded Patches Using Geraniol as a Penetration Enhancer for Transdermal Delivery.","authors":"Suhas Shivaji Siddheshwar, Sandhya Jadhav, Someshwar Dattatraya Mankar, Arti Changdev Ghorpade","doi":"10.1089/adt.2025.010","DOIUrl":"10.1089/adt.2025.010","url":null,"abstract":"<p><p>Diabetes management necessitates innovative approaches to enhance treatment efficacy and patient adherence. The study aimed to develop a transdermal patch loaded with emodin, hypothesized to provide a noninvasive treatment option that circumvents complications of oral administration. To optimize the formulation, a full factorial experimental design was employed, focusing on the concentrations of hydroxypropyl methylcellulose K15 and geraniol. Compatibility and mechanical characteristics were investigated using Fourier-transform infrared spectroscopy and differential scanning calorimetry. The patch's drug release profile was assessed via <i>in vitro</i> studies, while its stability was tested under accelerated conditions. The antidiabetic efficacy was evaluated in diabetic rats using an <i>in vivo</i> model. The optimized patch (batch SF7) released 94.57% of the drug over 12 h. Under accelerated stability conditions, the patch showed a minor decline in folding endurance from 396 ± 1.50 to 369 ± 2.63 folds and drug content uniformity from 98.70% ± 0.02% to 98.14% ± 0.23%. The <i>in vivo</i> antidiabetic study demonstrated a considerable decrease in blood glucose levels in SF7-treated rats from 245.83 ± 3.25 mg/dL to 120.86 ± 4.24 mg/dL over 12 h (<i>p</i>-value < 0.001), comparable with the standard drug glibenclamide. The emodin-loaded transdermal patch displayed consistent drug release, maintained stability, and demonstrated significant antidiabetic activity, suggesting that it is a promising noninvasive therapy for diabetes management.</p>","PeriodicalId":8586,"journal":{"name":"Assay and drug development technologies","volume":" ","pages":"30-48"},"PeriodicalIF":1.8,"publicationDate":"2026-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143957539","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}