Assay and drug development technologies最新文献_第5页

Adjusting the Fitting of Fluorescence-Based Dose-Response Kinase Inhibition Assay to Account for Fluorescent Inhibitors. 调整基于荧光的剂量反应激酶抑制测定的拟合以考虑荧光抑制剂。

IF 1.8 4区医学

Assay and drug development technologies Pub Date : 2023-10-01 Epub Date: 2023-09-28 DOI: 10.1089/adt.2023.044

Guillaume A Petit

引用次数: 0

Determination of the Toxicity Preferences of Ocular Drug Delivery System by Comparing Two Different Toxicity Bioassays. 通过比较两种不同的毒性生物测定法测定眼部给药系统的毒性偏好。

IF 1.8 4区医学

Assay and drug development technologies Pub Date : 2023-10-01 DOI: 10.1089/adt.2023.058

Burcu Uner, Meltem Ezgi Durgun, Samet Ozdemir, Cetin Tas, Melike Uner, Yildiz Ozsoy

{"title":"Determination of the Toxicity Preferences of Ocular Drug Delivery System by Comparing Two Different Toxicity Bioassays.","authors":"Burcu Uner, Meltem Ezgi Durgun, Samet Ozdemir, Cetin Tas, Melike Uner, Yildiz Ozsoy","doi":"10.1089/adt.2023.058","DOIUrl":"10.1089/adt.2023.058","url":null,"abstract":"Ocular drug delivery methods are highly favored for boosting bioavailability, patient compliance, and lower adverse effects and dose frequency. In addition to preventing adverse effects from the active ingredient, the parts of drug delivery systems must be nontoxic and nonallergic as well. Mitochondrial toxicity test (MTT) and Hen's egg chorioallantois membrane (HET-CAM) assay are the most often utilized tests based on this dilemma. The toxicity of loteprednol etabonate loaded solid lipid nanoparticles, lipid nanostructured carriers, and nanoemulsion were compared. Oleic acid, Precirol®ATO5, and Pluronic® F68 were used in the preparation. Their toxicities were evaluated by using two different toxicity tests (MTT and HET-CAM). The results suggest that there are no significant differences between the HET-CAM and MTT assays. It is noteworthy that the HET-CAM assay offers a more cost-effective and environmentally friendly alternative to the MTT assay, as it does not require cell culture and generates less toxic waste. This information may be useful to consider when selecting between the two assays.","PeriodicalId":8586,"journal":{"name":"Assay and drug development technologies","volume":"21 7","pages":"337-343"},"PeriodicalIF":1.8,"publicationDate":"2023-10-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"41189559","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

Illuminating Insights: Clinical Study Harnessing Pharmacoscintigraphy for Permeation Study of Radiolabeled Nimesulide Topical Formulation in Healthy Human Volunteers. 启发性见解：利用药物闪烁扫描在健康人体志愿者中进行放射性标记尼美舒利局部制剂渗透性研究的临床研究。

IF 1.8 4区医学

Assay and drug development technologies Pub Date : 2023-10-01 Epub Date: 2023-10-06 DOI: 10.1089/adt.2023.053

Nitin Sharma, Kushagra Khanna, Neeraj Kumar, Ritu Karwasra, Ashok Kumar Janakiraman, Mogana Sundari Rajagopal

{"title":"Illuminating Insights: Clinical Study Harnessing Pharmacoscintigraphy for Permeation Study of Radiolabeled Nimesulide Topical Formulation in Healthy Human Volunteers.","authors":"Nitin Sharma, Kushagra Khanna, Neeraj Kumar, Ritu Karwasra, Ashok Kumar Janakiraman, Mogana Sundari Rajagopal","doi":"10.1089/adt.2023.053","DOIUrl":"10.1089/adt.2023.053","url":null,"abstract":"An alternative to oral administration for the delivery of therapeutic substances is the topical route, which frequently has comparable efficacy but may have a better tolerability profile. Gamma scintigraphy is a noninvasive technique that involves the application of radioactive substances to conduct biodistribution studies of therapeutic substances delivered through various routes. Nimesulide (NSD) was radiolabeled with technetium pertechnetate (Technetium99m [99mTc]) and this radiolabeled drug complex (99mTc-NSD) was used to prepare a topical gel formulation. The permeation of the radiolabeled drug from the topical gel was determined by gamma scintigraphy on human volunteers. The region of interest was calculated for the quantification of permeated radiolabeled drugs. This was observed that the mean percentage permeation of 99mTc-NSD was found to be 0.32 ± 0.22 to 36.37 ± 2.86 at 5 and 240 min. It was demonstrated that gamma scintigraphy may be a noninvasive and reliable technique for the determination of drug permeation through topical routes.","PeriodicalId":8586,"journal":{"name":"Assay and drug development technologies","volume":" ","pages":"325-330"},"PeriodicalIF":1.8,"publicationDate":"2023-10-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"41103048","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

Formulation and Characterization of Nanoparticulate Drug Carrier System for Lacidipine. 拉西地平纳米药物载体体系的制备与表征。

IF 1.8 4区医学

Assay and drug development technologies Pub Date : 2023-10-01 DOI: 10.1089/adt.2023.023

Ashveta Anant Dessai, Mrunali Navin Kantak, Cleona Elizabeth Mary DCruz, Lalit Kumar, Prashant Jivaji Bhide, Rupesh Kalidas Shirodkar

{"title":"Formulation and Characterization of Nanoparticulate Drug Carrier System for Lacidipine.","authors":"Ashveta Anant Dessai, Mrunali Navin Kantak, Cleona Elizabeth Mary DCruz, Lalit Kumar, Prashant Jivaji Bhide, Rupesh Kalidas Shirodkar","doi":"10.1089/adt.2023.023","DOIUrl":"10.1089/adt.2023.023","url":null,"abstract":"Lacidipine, a calcium channel antagonist, is primarily used to treat hypertension. It is classified as a Biopharmaceutics Classification System Class II drug and exhibits an oral bioavailability of 10% due to its extensive hepatic first-pass metabolism. This research study focused on formulating lacidipine-loaded cubosomal nanovesicles developed into rapidly dissolving oral films as an alternative to overcome the downsides faced by conventional antihypertensive therapy. Lacidipine-loaded cubosomes were prepared utilizing a top-down technique using lipid and surfactant and were further developed into fast dissolving oral films. Box-Behnken design was used for the optimization of process variables to achieve minimum particle size and greater entrapment efficiency of the nanovesicles, and response data were statistically evaluated. The optimized cubosomal dispersions upon characterization reported particle size within nanorange (116.8-341 nm) and an entrapment efficiency of 88.15%-97.1%, with 91.72% of total drug content. Morphological studies revealed uniformly dispersed vesicles with cubic to spherical shape. Oral rapidly dissolving films, after evaluation, were reported to have transparent to opaque appearance with a highly porous nature, which was confirmed by scanning electron microscopic imaging and displayed uniformity in weight and thickness and reported optimum mechanical strength and considerable flexibility, with disintegration time of 37.67 ± 3.68 s and exhibited 91.44% ± 1.65% in vitro drug release after 6 min. Short-term stability studies conducted on films at 25°C ± 2°C and 60% ± 5% relative humidity for 3 months demonstrated no significant variation in morphological and mechanical properties. Therefore, lacidipine-loaded cubosomal rapid dissolving oral films may be a promising formulation approach for the management of hypertension.","PeriodicalId":8586,"journal":{"name":"Assay and drug development technologies","volume":"21 7","pages":"309-324"},"PeriodicalIF":1.8,"publicationDate":"2023-10-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"41189560","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

Development and Method Validation of Design of Experiments-Optimized Tablet Formulation for Simultaneous Detection of Exemestane and Everolimus. 同时检测依西美坦和依维莫司的优化片剂配方实验设计的开发和方法验证。

IF 1.8 4区医学

Assay and drug development technologies Pub Date : 2023-08-01 Epub Date: 2023-09-08 DOI: 10.1089/adt.2023.055

Akshay Kumar, Balak Das Kurmi, Dilpreet Singh

{"title":"Development and Method Validation of Design of Experiments-Optimized Tablet Formulation for Simultaneous Detection of Exemestane and Everolimus.","authors":"Akshay Kumar, Balak Das Kurmi, Dilpreet Singh","doi":"10.1089/adt.2023.055","DOIUrl":"10.1089/adt.2023.055","url":null,"abstract":"The development and analysis of pharmaceutical formulations often involves the determination of multiple active ingredients in a dosage form. The aim of the present study is to develop a convenient method for simultaneous estimation of Exemestane (EXE) and Everolimus (EVE) in bulk and in systemically designed tablet dosage form. Methanol was used as a solvent for developing linear curves and validated in terms of various parameters, such as selectivity, sensitivity, linearity, precision, accuracy, and robustness. Method validation observed that the proposed method is reliable and reproducible, meeting the regulatory requirements for pharmaceutical analysis with a relative standard deviation of <2%. The developed method was found to be sensitive and selective in simultaneous equation method. The unknown concentrations of EVE and EXE were found to be 10.431 and 10.232, respectively. The next step is to systematically design a tablet formulation for EXE and EVE containing β-cyclodextrin as a polymer. Microcrystalline cellulose (X1), sodium starch glycolate (X2), and beta-cyclodextrin (X3) are the critical variables and hardness (Y2) and friability (Y3) were selected as prime responses. Analysis of variance provides significance of the model, and the predicted batch gives a high desirability value of 0.862. In vitro dissolution profiles of optimized batch (OB1) were signified by high drug release profile as 89.47% and 96.00% for EVE and EXE in tablet formulation, as compared with pure API, respectively. This study signifies enhancement in biopharmaceutical attributes of EXE and EVE in tablet formulation and robust simultaneous estimation by the UV method. In a nutshell, this study provides the simultaneous estimation method in tablet dosage form, and further research is crucial for the advancement of pharmaceutical analysis and the formulation of effective medicines.","PeriodicalId":8586,"journal":{"name":"Assay and drug development technologies","volume":"21 6","pages":"273-287"},"PeriodicalIF":1.8,"publicationDate":"2023-08-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"10358250","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

Psoriasis: Striving for Potential Biomarkers. 银屑病：寻找潜在的生物标志物。

IF 1.8 4区医学

Assay and drug development technologies Pub Date : 2023-08-01 Epub Date: 2023-09-05 DOI: 10.1089/adt.2023.014

Deblina Dan, Nimisha Srivastava

{"title":"Psoriasis: Striving for Potential Biomarkers.","authors":"Deblina Dan, Nimisha Srivastava","doi":"10.1089/adt.2023.014","DOIUrl":"10.1089/adt.2023.014","url":null,"abstract":"Psoriasis is a chronic disease that is caused by multiple factors and is identified by itchiness, unpleasant, red, or white scaly patches on the skin, particularly on regularly chafed body regions such as the lateral areas of the limbs. Reports suggest that globally around 2%-3% of the population suffers from psoriasis. In this review, we have discussed the clinical classification of psoriasis and also the ideal characteristics of the biomarkers. An overview regarding the discovery of the biomarker and method for validating the study has been discussed. A growing body of research suggests a link to certain other systemic symptoms such as cardiovascular disorder, metabolic syndrome, and few other comorbidities such as hypertension and nonalcoholic fatty liver disease. Natural killer (NK) cells are lymphocyte cells that concentrate on the destruction of virally infected and malignant cells; these tend to produce a wide range of inflammatory cytokines, some of which are associated with the etiology of psoriasis. Detailed information on the molecular pathogenesis of psoriasis in which interleukin (IL)-17, IL-23, tumor necrosis factor-α (TNF-α), and CCL20 play a very significant role in the development of psoriasis. In this review, we have discussed an overview of the recent state of the biomarkers available for the diagnosis and treatment of psoriasis by emphasizing on the available biomarkers such as epigenomic, transcriptomic, glycomic, and metabolomic. The most recent advancements in molecular-targeted therapy utilizing biologics and oral systemic therapy (methotrexate, apremilast) enable to adequately treat the most serious psoriatic symptoms and also the studies have validated the efficacy of biologic therapy such as TNF-α antagonist (infliximab, adalimumab), IL-23 antagonist (guselkumab, risankizumab), and IL-17 antagonist (secukinumab, ixekizumab). Finally, an overview about the technological opportunities as well as various challenges has been discussed.","PeriodicalId":8586,"journal":{"name":"Assay and drug development technologies","volume":"21 6","pages":"235-257"},"PeriodicalIF":1.8,"publicationDate":"2023-08-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"10307237","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

Correction to: Enhanced Cytotoxic Activity of 6-Mercaptopurine-Loaded Solid Lipid Nanoparticles in Hepatic Cancer Treatment, by Ergin, et al. Assay Drug Dev Technol. 2023;21(5):212-221; doi: 10.1089/adt.2023.007. 修正：6-巯基嘌呤负载固体脂质纳米粒子在癌症治疗中增强的细胞毒性活性，Ergin等人，Assay Drug Dev Technol。2023年；21（5）：212-221；doi:10.1089/日期.2023.007。

IF 1.8 4区医学

Assay and drug development technologies Pub Date : 2023-08-01 Epub Date: 2023-09-06 DOI: 10.1089/adt.2023.007.correx

引用次数: 0

Exploration of the Mechanism of Shengxian Decoction Against Chronic Obstructive Pulmonary Disease Based on Network Pharmacology and Experimental Verification. 基于网络药理学和实验验证的升仙汤抗慢性阻塞性肺疾病作用机制探讨。

IF 1.8 4区医学

Assay and drug development technologies Pub Date : 2023-08-01 Epub Date: 2023-09-08 DOI: 10.1089/adt.2023.006

Yifei Chen, Yiming Wang, Zheng Li, Jing Jing, De Jiang, Xiaoxia Yuan, Fengsen Li

{"title":"Exploration of the Mechanism of Shengxian Decoction Against Chronic Obstructive Pulmonary Disease Based on Network Pharmacology and Experimental Verification.","authors":"Yifei Chen, Yiming Wang, Zheng Li, Jing Jing, De Jiang, Xiaoxia Yuan, Fengsen Li","doi":"10.1089/adt.2023.006","DOIUrl":"10.1089/adt.2023.006","url":null,"abstract":"Shengxian decoction (SXT) is clinically used in chronic obstructive pulmonary disease (COPD) treatment. This study aimed to explore the mechanism and target genes of SXT acting on COPD. Differentially expressed genes (DEGs) between COPD and controls were identified and then performed enrichment analysis. The effective active compounds and corresponding target genes were obtained from the traditional Chinese medicine systems pharmacology database. We also compiled COPD related genes from the GeneCards database. Through the protein-protein interaction (PPI) network and least absolute shrinkage and selection operator (LASSO) regression was performed to identify key genes. Molecular docking was used for docking of key genes and compounds. The expression of key genes was detected by quantitative real-time PCR in COPD patients and bronchial epithelial cells stimulated with cigarette stroke extract (CSE). We identified 1,458 intersected DEGs from GSE47460 and GSE57148 datasets. Compared with intersected DEGs, we obtained 33 SXT target COPD-related genes. PI3K-Akt signaling pathway, MAPK signaling pathway, and focal adhesion were enriched by these 33 genes, as well as intersected DEGs. According to LASSO regression, there were 12 genes considered as signature genes. Then we constructed active compounds and corresponding six target genes. Finally, HIF1A and IL1B were selected as key genes by combining PPI network. HIF1A and IL1B were all upregulated expression in COPD and CSE stimulated cells and recovered in SXT treated CSE stimulated cells. This study provides a scientific basis for the identification of active compounds and target genes of SXT in the treatment of COPD.","PeriodicalId":8586,"journal":{"name":"Assay and drug development technologies","volume":"21 6","pages":"258-272"},"PeriodicalIF":1.8,"publicationDate":"2023-08-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"10297899","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 April-June 2023. 药物再利用专利申请2023年4月至6月。

IF 1.8 4区医学

Assay and drug development technologies Pub Date : 2023-08-01 Epub Date: 2023-09-01 DOI: 10.1089/adt.2023.081

Hermann A M Mucke

引用次数: 0

Rosalind Franklin Society Proudly Announces the 2022 Award Recipient for Assay and Drug Development Technologies. 罗莎琳德·富兰克林协会自豪地宣布了2022年测定和药物开发技术奖获得者。

IF 1.8 4区医学

Assay and drug development technologies Pub Date : 2023-07-01 DOI: 10.1089/adt.2023.29104.rfs2022

Anaelle da Costa

引用次数: 0