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

On the Recent Changes to Animal Protection Measures in United States Food and Drug Administration Policy. 论美国食品和药物管理局政策中动物保护措施的最新变化。

IF 1.8 4区医学

Assay and drug development technologies Pub Date : 2023-01-01 DOI: 10.1089/adt.2023.29103.bjm

Bruce J Melancon

引用次数: 0

Design, Synthesis, and Biological Evaluation of Novel Dihydropyrimidinone Derivatives as Potential Anticancer Agents and Tubulin Polymerization Inhibitors. 新型二氢嘧啶衍生物抗癌和微管蛋白聚合抑制剂的设计、合成和生物学评价。

IF 1.8 4区医学

Assay and drug development technologies Pub Date : 2023-01-01 DOI: 10.1089/adt.2022.085

Ramkaran Rawal, Praveen K Gupta, Bhupinder Kumar, Rohit Bhatia

{"title":"Design, Synthesis, and Biological Evaluation of Novel Dihydropyrimidinone Derivatives as Potential Anticancer Agents and Tubulin Polymerization Inhibitors.","authors":"Ramkaran Rawal, Praveen K Gupta, Bhupinder Kumar, Rohit Bhatia","doi":"10.1089/adt.2022.085","DOIUrl":"https://doi.org/10.1089/adt.2022.085","url":null,"abstract":"The severity and prevalence of cancer in modern time are a huge global health burden. Continuous efforts are being made toward the development of newer therapeutic candidates to treat and manage this ailment. The dihydropyrimidinone scaffold is one of the key nuclei that have been highly explored and investigated against cancer. It has the potential to combat the consequences of cancer by interacting with several biological targets. Tubulin polymerization inhibition is one such strategy to prevent the progression of cancer. In the presented work, we have synthesized a series of sixteen dihydropyrimidinone derivatives by following a rational drug design. The synthesized compounds have been characterized by 1H NMR and 13C NMR and were further evaluated for cytotoxic activity against breast cancer cell lines (MCF-7 and MDA-MB-231), lung cancer cell lines (A549), and colon cancer cell lines (HCT-116). Compounds 5D and 5P were found most potent and revealed a better cytotoxic activity compared with the standard drug colchicine. Furthermore, the tubulin polymerization inhibition assay revealed that compound 5D showed better inhibition than colchicines, whereas compound 5P revealed an almost equal inhibition to that of colchicine. Furthermore, to investigate the possible mode of action and binding patterns, compounds 5P and 5D were subjected to molecular docking against tubulin (Protein Data Bank ID: ISA0). The results showed that compounds revealed significant interactions and were well occupied inside the cavity of tubulin. The compounds 5D and 5P may serve as new leads in drug development against cancer.","PeriodicalId":8586,"journal":{"name":"Assay and drug development technologies","volume":"21 1","pages":"17-28"},"PeriodicalIF":1.8,"publicationDate":"2023-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"10741939","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

Acknowledgment of Reviewers 2022. 审稿人致谢2022。

IF 1.8 4区医学

Assay and drug development technologies Pub Date : 2023-01-01 DOI: 10.1089/adt.2022.29102.ack

引用次数: 0

Silibinin-Loaded Nanostructured Lipid Carriers for Growth Inhibition of Cisplatin-Resistant Ovarian Cancer Cells. 负载水飞蓟宾的纳米结构脂质载体对顺铂耐药卵巢癌细胞生长的抑制作用。

IF 1.8 4区医学

Assay and drug development technologies Pub Date : 2022-12-01 DOI: 10.1089/adt.2022.060

Sevda Jafari, Atabak Bakhshaei, Morteza Eskandani, Ommoleila Molavi

{"title":"Silibinin-Loaded Nanostructured Lipid Carriers for Growth Inhibition of Cisplatin-Resistant Ovarian Cancer Cells.","authors":"Sevda Jafari, Atabak Bakhshaei, Morteza Eskandani, Ommoleila Molavi","doi":"10.1089/adt.2022.060","DOIUrl":"https://doi.org/10.1089/adt.2022.060","url":null,"abstract":"Cisplatin is the most often used chemotherapy in the treatment of ovarian cancer (OC), however long-term usage leads to drug resistance and treatment failure. Silibinin is a sparingly water-soluble natural compound with well-known anticancer effects. The use of lipid-based delivery systems is a potential approach for enhancing silibinin's water solubility. In this study, nanostructured lipid carriers (NLCs) containing silibinin were prepared and their inhibitory effects were tested in combination with cisplatin against sensitive/resistant A2780 OC cells. Silibinin-loaded NLCs (silibinin-NLCs) were prepared by the hot homogenization method, and their size, shape, zeta potential (ZP), and encapsulation efficiency (EE), as well as their inhibitory effects, were examined in combination with cisplatin against sensitive/resistant A2780 OC cells. Formulation of silibinin-NLCs using cocoa butter led to spherical-shaped NLCs with a size of 95 nm and EE of 98%. The ZP and the dispersion index of the silibinin-NLCs were -27.12 ± 0.13 mv and 0.12 ± 0.04, respectively. The release kinetics of silibinin-NLCs was best fitted with the zero-order model. The combination of cisplatin and silibinin-NLCs sensitized the cisplatin-resistant A2780 OC cells and exhibited a more synergistic inhibitory effect on A2780 cells as compared with the combination of cisplatin and plain silibinin. The optimized silibinin-NLCs can be considered a suitable drug delivery system for the inhibition of cisplatin-resistant OC cells.","PeriodicalId":8586,"journal":{"name":"Assay and drug development technologies","volume":"20 8","pages":"339-348"},"PeriodicalIF":1.8,"publicationDate":"2022-12-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"10412200","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

Development and Validation of Reverse-Phase High-Performance Liquid Chromatography Based Bioanalytical Method for Estimation of Simvastatin in Rat's Plasma. 大鼠血浆中辛伐他汀反相高效液相色谱生物分析方法的建立与验证。

IF 1.8 4区医学

Assay and drug development technologies Pub Date : 2022-12-01 DOI: 10.1089/adt.2022.080

Narendra Kumar Pandey, Sachin Kumar Singh, Bimlesh Kumar, Leander Corrie, Umesh Goutam, Dileep Singh Baghel

{"title":"Development and Validation of Reverse-Phase High-Performance Liquid Chromatography Based Bioanalytical Method for Estimation of Simvastatin in Rat's Plasma.","authors":"Narendra Kumar Pandey, Sachin Kumar Singh, Bimlesh Kumar, Leander Corrie, Umesh Goutam, Dileep Singh Baghel","doi":"10.1089/adt.2022.080","DOIUrl":"https://doi.org/10.1089/adt.2022.080","url":null,"abstract":"Simvastatin (SIM) is known to lower cholesterol levels and is speculated in the pathogenesis of Alzheimer's disease. In this study, the bioanalytical method of SIM SNEDDS was developed and validated for the estimation of SIM in the rat's plasma using reverse-phase high-performance liquid chromatography. C-18 reverse-phase octadecylsilyl column was used to validate the method. Atorvastatin (ATV) was used as an internal standard. Gradient elution was performed using acetonitrile and water in a ratio of 90:10 with a flow rate of 1 mL/min. The chromatogram of these both compounds SIM and ATV was detected at a wavelength of 238 and 244 nm. The drugs were extracted from the plasma samples using the protein precipitation method. The retention time of SIM and ATV was found to be 3.720 and 8.331 min, respectively. The developed method was found to be linear in the range between 50 and 250 ng/mL, with a regression coefficient (r2) of 0.9994. According to ICH M10 guidelines, the method was validated. The percent of drug recovery was more than 95% and the % relative standard deviation was <2% in the replicate studies, which showed that the method was accurate and precise. The limit of detection and limit of quantification were found in rat plasma to be 0.12 and 0.38 ng/mL, respectively. The obtained result indicated that the developed method was successful in estimating SIM in rat plasma and passed all validation test parameters.","PeriodicalId":8586,"journal":{"name":"Assay and drug development technologies","volume":"20 8","pages":"349-358"},"PeriodicalIF":1.8,"publicationDate":"2022-12-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"10762625","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 July-September 2022. 药物再利用专利申请2022年7月至9月。

IF 1.8 4区医学

Assay and drug development technologies Pub Date : 2022-12-01 DOI: 10.1089/adt.2022.097

Hermann A M Mucke

引用次数: 0

Potential Assessment of Topical Felbinac-Loaded Cubosomal Gel in Soft Tissue Injury in Albino Rats. 外用负载felbinac的立方体凝胶治疗白化大鼠软组织损伤的潜力评估。

IF 1.8 4区医学

Assay and drug development technologies Pub Date : 2022-12-01 DOI: 10.1089/adt.2022.063

Snigdha Bhardwaj, Anshul, Praveen Kumar Gaur, Sonam Bhatia

{"title":"Potential Assessment of Topical Felbinac-Loaded Cubosomal Gel in Soft Tissue Injury in Albino Rats.","authors":"Snigdha Bhardwaj, Anshul, Praveen Kumar Gaur, Sonam Bhatia","doi":"10.1089/adt.2022.063","DOIUrl":"https://doi.org/10.1089/adt.2022.063","url":null,"abstract":"Muscle strain is one of the most common injuries with high intermittence rate. Due to diverseness of strain injuries, different experimental animal models are employed to investigate such injuries with reproducible results. Cubosomes, an emerging nano drug delivery tool, are considered ideal carriers for the topical delivery of lipophilic drugs to treat local inflammations with reduced frequency of application for prolonged periods. This work describes the development of Felbinac-loaded cubosomal gel and investigated the treatment of inflammation and tissue injury in vivo. Sciatic Function Index (SFI) is a simple clinical method to observe hind limb recovery in rats after induced injuries. First, cubosomes were fabricated by high-pressure homogenization process and evaluated for in vitro parameters. The optimized cubosome formulation was chosen to develop cubosomal gel and evaluated for in vitro parameters and also investigated time to recovery of SFI after strain induction in tibialis anterior muscles in rats. The cubosome formulation (F4) exhibited low droplet size (51.04 ± 1.37 nm)and polydispersity index (0.085 ± 1.13), and negative zeta potential (-32.8 ± 0.67 mV). In rats, topical application of cubosomal gel formulation (CGF) exhibited significant improvement in skin permeation (402 ± 6.08 μg) and drug flux (15.71 ± 0.82 μg/cm2 h) compared to plain gel. Also, CGF demonstrated significant difference in SFI from first to seventh day. The histology of rat skin showed significant effect for groups treated with Felbinac-loaded CGF compared to a negative control group.","PeriodicalId":8586,"journal":{"name":"Assay and drug development technologies","volume":"20 8","pages":"367-376"},"PeriodicalIF":1.8,"publicationDate":"2022-12-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"10413074","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

Healing Potential of Propolis Extract-Passiflora edulis Seed Oil Emulgel Against Excisional Wound: Biochemical, Histopathological, and Cytokines Level Evidence. 蜂胶提取物-西番莲籽油凝胶对切除伤口的愈合潜力:生化、组织病理学和细胞因子水平证据。

IF 1.8 4区医学

Assay and drug development technologies Pub Date : 2022-10-01 DOI: 10.1089/adt.2022.075

Puneet Gupta, Ashish Singh, Neelam Singh, Faraat Ali, Ayushi Tyagi, Sadish K Shanmugam

{"title":"Healing Potential of Propolis Extract-Passiflora edulis Seed Oil Emulgel Against Excisional Wound: Biochemical, Histopathological, and Cytokines Level Evidence.","authors":"Puneet Gupta, Ashish Singh, Neelam Singh, Faraat Ali, Ayushi Tyagi, Sadish K Shanmugam","doi":"10.1089/adt.2022.075","DOIUrl":"https://doi.org/10.1089/adt.2022.075","url":null,"abstract":"Propolis is rich in natural bioactive compounds, and considering its importance for many skin therapies, emulgel was prepared. This study examines how a propolis extract (PE) and Passiflora edulis seed (PS) oil emulgel affect rat deep skin wound healing. Based on preset criteria of maximum drug content and optimum drug permeation through the stratum corneum along with drug retention in the skin layers, an optimized emulgel formula based on Box-Behnken factorial design was prepared and used for subsequent in vitro and in vivo evaluations. In vivo wound-healing activities of emulgel and control treatments were investigated in a rat model. The optimized emulgel formula exhibited superior healing activity compared with plain PE suspension-treated rats on day 14 of wounding. Histopathological investigations of hematoxylin and eosin and Masson's Trichrome-stained skin sections supported this effect. Emulgel promotes cutaneous wound healing through a variety of mechanisms, including anti-inflammatory through modulation of cytokines tumor necrosis factor-α, interleukin (IL)-1β, and IL-6 production, and promotion of collagen fiber formation, all of which contribute to tissue remodeling. Furthermore, when compared with propolis suspension, emulgel showed significant antioxidant and anti-inflammatory effects. Emulgel significantly increased the skin's hydroxyproline level, antioxidant potential, wound contraction, increased penetration, and localized propolis deposition across the skin. Incorporation of PS oil into the emulgel accelerates the tissue regeneration process. The findings suggest that 5% propolis emulgel could be used as an alternative to treat wounds.","PeriodicalId":8586,"journal":{"name":"Assay and drug development technologies","volume":"20 7","pages":"300-316"},"PeriodicalIF":1.8,"publicationDate":"2022-10-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"40561376","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

Letter to the Editor: 3D Printing Has an Imperative Role in Colitis Management. 致编辑的信:3D打印在结肠炎管理中起着至关重要的作用。

IF 1.8 4区医学

Assay and drug development technologies Pub Date : 2022-10-01 Epub Date: 2022-10-11 DOI: 10.1089/adt.2022.078

Sarmili Sahoo, Amandeep Singh

引用次数: 1

Editor's Response to a Letter on "3D Printing Has an Imperative Role in Colitis Management" by Sahoo and Singh. 编辑对Sahoo和Singh关于“3D打印在结肠炎管理中起着至关重要的作用”的信的回应。

IF 1.8 4区医学

Assay and drug development technologies Pub Date : 2022-10-01 Epub Date: 2022-10-11 DOI: 10.1089/adt.2022.29101.bjm

Bruce J Melancon

引用次数: 0