{"title":"Modulation of Anti-Inflammatory Activity via Diclofenac Sodium-Based Nanostructured-Lipid Carriers: Physical Characterization and <i>In Vivo</i> Assessment.","authors":"Alok Pratap Singh, Dinesh Puri, Iti Chauhan, Amulya Jindal, Jayendra Kumar, Nitish Kumar, Madhu Verma, Mohd Yasir, Sonakshi Antal, Priya Dhiman, Prasoon Kumar Saxena","doi":"10.1089/adt.2025.004","DOIUrl":"https://doi.org/10.1089/adt.2025.004","url":null,"abstract":"<p><p>\u0000 <i>Diclofenac sodium (DS) is categorized under the nonsteroidal anti-inflammatory class of drugs that also belongs to biopharmaceutical classification system (BCS) class II. It has limited dissolution parameters which also resist the total bioavailability but it has a good transdermal permeability characteristic and the pharmacokinetic parameters of DS make it suitable for the formulation of nanostructured-lipid carrier (NLC)-based gel transdermal delivery. The research aimed to design and develop a drug-delivery system (DDS), i.e., DS-NLCs incorporated in gel to modulate its anti-inflammatory action via skin. The formulation was optimized using Taguchi's approach and the resultant NLCs were thoroughly characterized, including assessments for viscosity, zeta potential, particle size, and morphological evaluation. Furthermore, particular investigations were carried out for DS-NLCs, including drug encapsulation efficiency, <i>ex vivo</i> release properties in Phosphate Buffer Saline at pH 7.4, and an <i>in vivo</i> skin irritation test. 5-FUNLCs had a mean size of 339 ± 25 nm and were spherical-shaped particles. With an encapsulation effectiveness of 84%, the NLCs were found to have effectively loaded drugs. Moreover, these NLCs demonstrated a sustained release characteristic that persisted for a maximum of 24 h, suggesting their potential for gradual and regulated drug release. Lipid components demonstrated good stability over 90 days and were biocompatible with the DS. Furthermore, compared with the usual formulation, topical gel loaded with NLC (GNLC) containing DS considerably suppresses edema in the <i>in vivo</i> result, suggesting that the developed formulation has superior anti-inflammatory efficacy. These NLCs provide prolonged release and better drug solubility, both of which boost therapeutic outcomes and control the drug's anti-inflammatory potential. The study's conclusion emphasizes DS-NLC's potential as a cutting edge and effective medication delivery technology. The results indicate the need for more preclinical research, which presents an effective direction for developing a more potent and well-tolerated therapeutic strategy.</i>\u0000 </p>","PeriodicalId":8586,"journal":{"name":"Assay and drug development technologies","volume":" ","pages":""},"PeriodicalIF":1.6,"publicationDate":"2025-06-12","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"144274122","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":"<i>Letter:</i> Addressing False Positives in High-Throughput Screening: A Call for Better Predictive Models.","authors":"Dilpreet Singh","doi":"10.1089/adt.2025.035","DOIUrl":"https://doi.org/10.1089/adt.2025.035","url":null,"abstract":"","PeriodicalId":8586,"journal":{"name":"Assay and drug development technologies","volume":" ","pages":""},"PeriodicalIF":1.6,"publicationDate":"2025-05-28","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"144156053","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}
Hrushikesh S Dhande, Jayshree B Taksande, Nishant B Awandekar, Sushil S Burle, Milind J Umekar, Swati N Lade
{"title":"Pharmacodynamic and Physicochemical Evaluation of Intranasal Zolmitriptan-Loaded Nanostructured Lipid Carriers: for Enhanced Antimigraine Potential.","authors":"Hrushikesh S Dhande, Jayshree B Taksande, Nishant B Awandekar, Sushil S Burle, Milind J Umekar, Swati N Lade","doi":"10.1089/adt.2025.016","DOIUrl":"https://doi.org/10.1089/adt.2025.016","url":null,"abstract":"<p><p>\u0000 <i>Migraine is a debilitating neuromuscular disorder marked by severe, one-sided headaches. Triptans, such as Zolmitriptan (ZMP), act as serotonin receptor agonists and are commonly used in migraine treatment. However, ZMP, classified under Bio-pharmaceutics Classification System Class III, suffers from low oral bioavailability (<4%), limiting its therapeutic efficacy. To address this, intranasal delivery using nanostructured lipid carriers (NLCs) has emerged as a promising strategy to enhance bioavailability and enable targeted brain delivery. The study aimed to improve the bioavailability of ZMP by developing intranasal NLCs and evaluating their potential for targeted brain delivery in migraine treatment. ZMP-loaded NLCs (ZMP-NLCs) were formulated using the hot melt emulsification method with high-speed stirring. The NLCs were optimized based on particle size, zeta potential, entrapment efficiency (EE), and drug release over 8 h. The optimized formulation consisted of 1% Glycerol Monostearate (solid lipid), 1% Capmul MCM (liquid lipid), and 1.5% Tween 80 (surfactant). The NLCs were characterized using Fourier transmission infrared (FTIR) spectroscopy, powder X-ray diffraction (XRD), and scanning electron microscopy (SEM) to confirm drug incorporation and particle morphology. Pharmacodynamic studies were conducted to assess brain delivery and antimigraine efficacy. The optimized NLC formulation exhibited a particle size of 233 ± 9.07 nm, a polydispersity index of 0.257 ± 0.03, a zeta potential of -42.8 ± 0.5 mV, an EE of 89.35 ± 0.9%, and a drug release of 87.1 ± 1.03% after 8 h. FTIR and XRD analyses confirmed the successful incorporation of ZMP into the NLCs without significant chemical interactions. SEM revealed uniform, spherical particles. Pharmacodynamic studies demonstrated effective brain delivery of ZMP, bypassing the blood-brain barrier, and significantly enhancing its antimigraine potential. This study highlights the potential of ZMP-NLCs for intranasal delivery. NLCs offer improved bioavailability and targeted brain therapy for effective migraine management. The findings suggest that NLCs are a promising approach for enhancing the therapeutic efficacy of ZMP.</i>\u0000 </p>","PeriodicalId":8586,"journal":{"name":"Assay and drug development technologies","volume":" ","pages":""},"PeriodicalIF":1.6,"publicationDate":"2025-05-26","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"144141255","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":"https://doi.org/10.1089/adt.2025.010","url":null,"abstract":"<p><p>\u0000 <i>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.</i>\u0000 </p>","PeriodicalId":8586,"journal":{"name":"Assay and drug development technologies","volume":" ","pages":""},"PeriodicalIF":1.6,"publicationDate":"2025-05-12","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}
{"title":"Recent Trends in Drug Delivery Systems.","authors":"Omnia Mohamed Sarhan","doi":"10.1089/adt.2025.031","DOIUrl":"https://doi.org/10.1089/adt.2025.031","url":null,"abstract":"<p><p>\u0000 <i>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.</i>\u0000 </p>","PeriodicalId":8586,"journal":{"name":"Assay and drug development technologies","volume":" ","pages":""},"PeriodicalIF":1.6,"publicationDate":"2025-05-07","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":"Elucidating Genetic and Immunological Pathways Mediated by Sodium-Glucose Transporter 2 Inhibitors in Reducing Gout Risk: A Two-Step Mendelian Randomization Study.","authors":"Huiqiong Zeng, Zebo Cai, Junda Lai, Zhijun Chen, Wei Liu, Ye Zhang","doi":"10.1089/adt.2024.137","DOIUrl":"https://doi.org/10.1089/adt.2024.137","url":null,"abstract":"<p><p>\u0000 <i>While sodium-glucose transporter 2 inhibitors (SGLT2i) demonstrate urate-lowering effects, their causal role in Gout prevention remains controversial. This study employs advanced Mendelian randomization (MR) techniques to dissect immune-mediated mechanisms underlying this relationship. Using bidirectional two-sample MR and mediation analysis, we analyzed genetic instrument variables for SGLT2i (10 single-nucleotide polymorphisms, F-statistic >20), Gout risk (6,810 cases/477,788 controls), and 731 immune cell phenotypes. Pleiotropy and heterogeneity were also assessed to ensure robustness. The study confirmed a significant indirect effect of SGLT2i, which exhibited a 2.6% reduced Gout risk (Odds Ratio [OR]: 0.9738, 95% confidence interval [CI] = 0.9623, 0.9854, P = 1.12e-05). Thirty-five immune cell phenotypes were identified as significantly affecting Gout development, with key phenotypes such as CD86 on myeloid Dendritic cell (DC) (OR: 0.9966; 95% CI = 0.9930, 0.9995), contributing to 12.8% of the overall mediation effect. No evidence of heterogeneity or pleiotropy was detected and reverse-direction MR corroborated these findings. Our study first established SGLT2i as Gout-protective agents through DC-mediated immunomodulation, offering mechanistic insights for targeted prevention strategies in clinical practice.</i>\u0000 </p>","PeriodicalId":8586,"journal":{"name":"Assay and drug development technologies","volume":" ","pages":""},"PeriodicalIF":1.6,"publicationDate":"2025-05-07","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143957934","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}
Sachin Joshi, Priya Jindal, Shreastha Gautam, Charanjeet Singh, Preeti Patel, Ghanshyam Das Gupta, Balak Das Kurmi
{"title":"Mini Review on the Lyophilization: A Basic Requirement for Formulation Development and Stability Modifier.","authors":"Sachin Joshi, Priya Jindal, Shreastha Gautam, Charanjeet Singh, Preeti Patel, Ghanshyam Das Gupta, Balak Das Kurmi","doi":"10.1089/adt.2024.122","DOIUrl":"10.1089/adt.2024.122","url":null,"abstract":"<p><p>\u0000 <i>Freeze-drying is popular for producing pharmaceutical formulations with structurally complicated active components and drug delivery system carriers. It is the process of eliminating water from ice crystals through the sublimation mechanism. Some formulations may require drug-specific excipients such as stabilizers, buffers, and bulking agents to maintain the appearance and assure the long-term stability of the drug product. This approach is utilized for therapeutic compounds that are moisture sensitive, thermolabile, and degrade in the atmosphere. Freezing and primary and secondary drying are critical processes in the lyophilization process because they directly impact the end result. This approach is effective for producing a variety of dosage forms, including oral, inhalation, and parenteral. As a result, lyophilization may be an important method for improving the therapeutic efficacy and delivery of various dosage forms delivered via different routes. Additionally, lyophilization is used in pharmacological research to preserve biological samples, stabilize reference/standards, and increase the solubility and bioavailability of poorly soluble drugs. Thus, lyophilization is critical for maintaining the stability, efficacy, and safety of pharmaceutical products throughout their development and lifecycles. This article includes a broad overview of the lyophilization process, principle, excipients for lyophilized medicine compositions, and new lyophilization technologies as well as their applications in a variety of fields.</i>\u0000 </p>","PeriodicalId":8586,"journal":{"name":"Assay and drug development technologies","volume":" ","pages":"180-194"},"PeriodicalIF":1.6,"publicationDate":"2025-05-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143497615","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}
Gabriel Atampugbire, Eureka Emefa Ahadjie Adomako, Osbourne Quaye
{"title":"<i>In Vitro</i> Antiviral Assays: A Review of Laboratory Methods.","authors":"Gabriel Atampugbire, Eureka Emefa Ahadjie Adomako, Osbourne Quaye","doi":"10.1089/adt.2024.075","DOIUrl":"10.1089/adt.2024.075","url":null,"abstract":"<p><p>\u0000 <i>Viral diseases remain a significant challenge for global health with rising fatalities each year. In vitro assays are crucial techniques that have been utilized by researchers in the quest to develop antiviral therapies. These assays mimic the internal conditions of a living system and make it possible to study how antiviral compounds interact with such systems in a laboratory setting. Thus, the importance of in vitro assays cannot be overemphasized, as they provide an accurate means for assessing the efficacy of potential antiviral compounds. This review offers an overview of in vitro antiviral assays, the different types of cell lines used, and emerging techniques and applications that have been developed in recent times. The current review also assesses challenges that are encountered in antiviral drug research, as well as emerging technologies like microfluidics and three-dimensional cell cultures. The integration of computational models and multiparametric assays into antiviral research was noted to significantly improve antiviral drug development process.</i>\u0000 </p>","PeriodicalId":8586,"journal":{"name":"Assay and drug development technologies","volume":" ","pages":"165-179"},"PeriodicalIF":1.6,"publicationDate":"2025-05-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142969514","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}
Yujiao Hou, Yuesheng Zhao, Jun Liu, Yanan Bao, Njolibimi Mosesmanaanye, Chunjie Zhao, Wenjing Li, Bo Hong
{"title":"Optimization of Docetaxel-Zedoary Turmeric Oil Magnetic Solid Lipid Nanoparticle Preparation by Central Composite Design-Response Surface Methodology.","authors":"Yujiao Hou, Yuesheng Zhao, Jun Liu, Yanan Bao, Njolibimi Mosesmanaanye, Chunjie Zhao, Wenjing Li, Bo Hong","doi":"10.1089/adt.2024.120","DOIUrl":"10.1089/adt.2024.120","url":null,"abstract":"<p><p><i>To optimize the formulation of docetaxel-zedoary oil magnetic solid lipid nanoparticles (DTX-ZTO-MSLN) using central composite design-response surface methodology. First, the formulation and preparation process of DTX-ZTO-MSLN were optimized</i> via <i>design-response surface methodology. The appearance, particle size, thermogravimetric, pH, iron content, magnetic strength, and</i> in vitro <i>drug release of DTX-ZTO-MSLN were subsequently examined. Finally, the antitumor effect of DTX-ZTO-MSLN on MCF-7 breast cancer cells was measured</i> via <i>the 3-[4,5-dimethylthiazol-2-yl]-2,5 diphenyl tetrazolium bromide (MTT) assay. The optimized formulation was as follows: the mass ratio of soybean phospholipid to poloxamer 188 was 0.34, the mass ratio of DTX-ZTO to glycerol monostearate was 3.23, and 29.42 mL of water was used. The DTX-ZTO-MSLN prepared by the optimized method was clear and transparent, with good stability, with an iron content of 7.38%, and a saturation magnetization intensity of 7.05 A·m<sup>2</sup>·kg<sup>-1</sup>. The</i> in vitro <i>drug release was consistent with the Weibull model (R<sup>2</sup> = 0.9992). Compared with zedoary turmeric oil and docetaxel, DTX-ZTO-MSLN had a much greater inhibitory effect on MCF-7 cells (p < 0.05).</i> <i>The optimized DTX-ZTO-MSLN meets the quality requirements for nanoemulsions. This study provides a theoretical basis for developing and applying DTX-ZTO-MSLN</i>.</p>","PeriodicalId":8586,"journal":{"name":"Assay and drug development technologies","volume":" ","pages":"195-211"},"PeriodicalIF":1.6,"publicationDate":"2025-05-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142943401","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":"<i>Letter:</i> New Horizons in Biomarker Discovery: Assay Technologies for Personalized Drug Development.","authors":"Dilpreet Singh","doi":"10.1089/adt.2025.015","DOIUrl":"10.1089/adt.2025.015","url":null,"abstract":"","PeriodicalId":8586,"journal":{"name":"Assay and drug development technologies","volume":" ","pages":"212-215"},"PeriodicalIF":1.6,"publicationDate":"2025-05-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143647067","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}