Assay and drug development technologies最新文献_第10页

Formulation and Characterization of Raloxifene Nanostructured Lipid Carriers for Permeability and Uptake Enhancement Applications. 雷洛昔芬纳米结构脂质载体的制备和表征，用于渗透和吸收增强应用。

IF 1.8 4区医学

Assay and drug development technologies Pub Date : 2022-05-26 DOI: 10.1089/adt.2022.004

Anju Sharma, Jarriaun Streets, Priyanka Bhatt, Pranav Patel, V. Sutariya, Sheeba Varghese Gupta

{"title":"Formulation and Characterization of Raloxifene Nanostructured Lipid Carriers for Permeability and Uptake Enhancement Applications.","authors":"Anju Sharma, Jarriaun Streets, Priyanka Bhatt, Pranav Patel, V. Sutariya, Sheeba Varghese Gupta","doi":"10.1089/adt.2022.004","DOIUrl":"https://doi.org/10.1089/adt.2022.004","url":null,"abstract":"Raloxifene (RLX), a biopharmaceutical classification system (BCS) class II drug, is a selective estrogen receptor modulator (SERM) having an estrogenic effect on the bone and an antiestrogenic effect on the endometrium and breast. Low solubility, high permeability, high metabolism, and low bioavailability are the characteristics of raloxifene. Although 60% is absorbed orally, raloxifene shows extremely poor bioavailability (2%) owing to its low solubility and extensive (>90%) intestinal/hepatic first-pass metabolism. Hence, it becomes important to increase the solubility of raloxifene to enhance its bioavailability. In this study, raloxifene nanostructured lipid carriers (RNLCs) were prepared using the melt dispersion ultrasonication method. The prepared RNLCs were characterized, and the in vitro studies were carried out in the human epithelial breast cancer cell line (MCF-7). The RNLCs had a size of 114.8 ± 0.98 nm and a zeta potential of +9.21 ± 0.58 mV. Transmission electron microscopy (TEM) images showed particle size ranging from 65 to 120 nm. With an entrapment efficiency of 75.04% ± 2.75%, the RNLCs showed sustained release over 7 days compared with the raloxifene drug solution. The prepared RNLCs were successfully taken up by the MCF-7 cells in a time-dependent manner, and the RNLCs showed increased cell cytotoxicity compared with the raloxifene drug. Using the parallel artificial membrane permeability assay (PAMPA), the permeability rate for raloxifene solution was calculated to be 8 × 10-6 cm/s, and for the RNLCs, it was calculated to be 17.8 × 10-6 cm/s. Hence, from the permeability rate calculated, we could conclude that raloxifene, when formulated as nanostructured lipid carriers, showed increased permeability. Overall, the prepared RNLCs were found to be superior to the raloxifene drug as such.","PeriodicalId":8586,"journal":{"name":"Assay and drug development technologies","volume":" ","pages":""},"PeriodicalIF":1.8,"publicationDate":"2022-05-26","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"46391558","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: 2

Drug Repurposing Patent Applications January-March 2022. 药物再利用专利申请2022年1月至3月。

IF 1.8 4区医学

Assay and drug development technologies Pub Date : 2022-05-24 DOI: 10.1089/adt.2022.033

H. Mucke

引用次数: 0

Correction to: A New Spectral Shift-Based Method to Characterize Molecular Interactions, by Langer, et al. Assay Drug Dev Technol. 2022;20(2):83-94; doi: 10.1089/adt.2021.133. 修正:一种新的基于光谱位移的方法来表征分子相互作用，由Langer等人。检测药物开发技术，2022;20(2):83-94;doi: 10.1089 / adt.2021.133。

IF 1.8 4区医学

Assay and drug development technologies Pub Date : 2022-04-07 DOI: 10.1089/adt.2021.133.correx

引用次数: 0

Call for Special Issue Papers: New Modalities in Chemical Probes and Pharmacological Tools in Drug Discovery. 特刊论文征集：药物发现中化学探针和药理学工具的新模式。

IF 1.8 4区医学

Assay and drug development technologies Pub Date : 2022-04-01 DOI: 10.1089/adt.2022.29098.cfp

M. Kostic, B. Melancon

引用次数: 0

Developmental Cardiotoxicity and Hepatotoxicity of Flurbiprofen Axetil to Zebrafish Embryo. 氟比洛芬酯对斑马鱼胚胎的发育性心脏毒性和肝毒性。

IF 1.8 4区医学

Assay and drug development technologies Pub Date : 2022-04-01 DOI: 10.1089/adt.2021.127

Yuping Wang, Min Zhou, Jing Wang, Chu-Fang Lin, Xiang-li Gao, Li Zhang, Wenshui Yao, Longxin Zhang

{"title":"Developmental Cardiotoxicity and Hepatotoxicity of Flurbiprofen Axetil to Zebrafish Embryo.","authors":"Yuping Wang, Min Zhou, Jing Wang, Chu-Fang Lin, Xiang-li Gao, Li Zhang, Wenshui Yao, Longxin Zhang","doi":"10.1089/adt.2021.127","DOIUrl":"https://doi.org/10.1089/adt.2021.127","url":null,"abstract":"Flurbiprofen axetil (FA) is a nonsteroidal targeted analgesic and widely used for postoperative analgesia and cancer analgesia. Extensive works have been done in the evaluation of FA's clinical analgesic effect on adults. Along with the increase of FA usage, the potential toxicity and molecular mechanism in embryo development need to be better understood. In this article, multiple embryonic development indexes of zebrafish were introduced to evaluate the FA toxicity to provide clinical guidance for gravidas medicine. We performed a zebrafish embryo toxicity (ZFET) test by exposing embryos to a series of concentration gradients of FA medium starting from 24 hours postfertilization (hpf). The mortality rate, hatching rate, and malformation rate of drug-treated zebrafish were assessed at 72, 96, and 120 hpf. Effects of ≤10% lethal concentration (LC10) of FA on embryogenesis were evaluated by eye area, body length, and yolk sac area. A 0.5 μg/mL or fewer FA treatment did not show any adverse effects, but the LC10 FA significantly caused zebrafish malformation. Organ disorders, including slow heart rate, enlarged pericardium, and liver atrophy, were found in the dysplasia individuals when compared with control. TUNEL assay suggested that apoptotic cells in malformation embryos were produced by FA and the increasing dosage exacerbated apoptosis. Quantitative real-time polymerase chain reaction revealed that expressions of cardiac development-associated transcription factors, liver development-related genes, and apoptosis regulating genes were aberrant. These results indicate that the ZFET can be applied in the FA toxicity test, and a low lethal dose of FA is harmful to zebrafish embryogenesis, especially in embryo carcinogenesis and hepatogenesis.","PeriodicalId":8586,"journal":{"name":"Assay and drug development technologies","volume":"20 3 1","pages":"125-135"},"PeriodicalIF":1.8,"publicationDate":"2022-04-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"42987879","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

引用次数: 1

Call for Special Issue Papers: Chemical Probes and Pharmacological Tools for Imaging Applications. 特刊论文征集：用于成像应用的化学探针和药理学工具。

IF 1.8 4区医学

Assay and drug development technologies Pub Date : 2022-04-01 DOI: 10.1089/adt.2022.29099.cfp

M. Kostic, B. Melancon

引用次数: 0

Interview with Craig W. Lindsley, PhD. Craig W. Lindsley博士访谈

IF 1.8 4区医学

Assay and drug development technologies Pub Date : 2022-03-31 DOI: 10.1089/adt.2022.29097.bjm

B. Melancon

引用次数: 0

Forging Ahead with ASSAY. 与化验携手前行。

IF 1.8 4区医学

Assay and drug development technologies Pub Date : 2022-03-30 DOI: 10.1089/adt.2022.29100.bjm

B. Melancon

引用次数: 0

Drug Repurposing Patent Applications October: December 2021. 药物再利用专利申请10月:2021年12月

IF 1.8 4区医学

Assay and drug development technologies Pub Date : 2022-02-09 DOI: 10.1089/adt.2022.002

H. Mucke

引用次数: 0

Modifications to the Transwell Migration/Invasion Assay Method That Eases Assay Performance and Improves the Accuracy. 对Transwell迁移/入侵分析方法的改进，简化了分析性能并提高了准确性。

IF 1.8 4区医学

Assay and drug development technologies Pub Date : 2022-02-01 DOI: 10.1089/adt.2021.140

Heidi Marie Stoellinger, Arshak R Alexanian

{"title":"Modifications to the Transwell Migration/Invasion Assay Method That Eases Assay Performance and Improves the Accuracy.","authors":"Heidi Marie Stoellinger, Arshak R Alexanian","doi":"10.1089/adt.2021.140","DOIUrl":"https://doi.org/10.1089/adt.2021.140","url":null,"abstract":"Migration is a key property of live cells and critical for normal development, immune response, and disease processes such as cancer metastasis and inflammation. Methods to examine cell migration are especially useful and important for a wide range of biomedical research such as cancer biology, immunology, vascular biology, cell biology, and developmental biology. In vitro assays are excellent approaches to extrapolate to in vivo situations and study live cells behavior. The aim of this article is to discuss the existing methods for transwell migration/invasion studies, the problems associated with this assay, and proposed modifications to this methodological approach that makes it simple to perform and improve the assay accuracy. Results of our studies demonstrated that the count of cells that had grown on top of the membrane is important to accurately evaluate the percentage of migrated/invaded cells. The results also showed that the transparent transwell insert with 4',6-diamidino-2-phenylindole (DAPI) stained cells is the best approach to ease the analysis of cell numbers on top of the membranes. In addition, the overlay of bright light (representing membrane pores) and DAPI images can further improve the accuracy of cell count. All these modifications in combination simplify the assay performance and improve the accuracy of the transwell migration assay method.","PeriodicalId":8586,"journal":{"name":"Assay and drug development technologies","volume":"20 2","pages":"75-82"},"PeriodicalIF":1.8,"publicationDate":"2022-02-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC8968842/pdf/adt.2021.140.pdf","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"10819806","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: 4