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

Computational Design of Phosphatidylinositol 3-Kinase Inhibitors. 磷脂酰肌醇3激酶抑制剂的计算设计。

IF 1.8 4区医学

Assay and drug development technologies Pub Date : 2022-10-01 DOI: 10.1089/adt.2022.057

Isha Rani, Anju Goyal, M Sharma

引用次数: 5

Drug Repurposing Patent Applications March: June 2022. 药物再利用专利申请3月:2022年6月。

IF 1.8 4区医学

Assay and drug development technologies Pub Date : 2022-08-23 DOI: 10.1089/adt.2022.065

H. Mucke

引用次数: 2

A Review on Delivery and Bioavailability Enhancement Strategies of Azithromycin. 阿奇霉素给药及提高生物利用度策略研究进展。

IF 1.8 4区医学

Assay and drug development technologies Pub Date : 2022-08-01 Epub Date: 2022-09-08 DOI: 10.1089/adt.2022.036

Pallavi Swarup, Gopal Prasad Agrawal

引用次数: 1

Dual Acting Immuno-Antibiotics: Computational Investigation on Antibacterial Efficacy of Immune Boosters Against Isoprenoid H Enzyme. 双作用免疫抗生素:免疫增强剂对类异戊二烯H酶抑菌效果的计算研究。

IF 1.8 4区医学

Assay and drug development technologies Pub Date : 2022-07-01 Epub Date: 2022-07-12 DOI: 10.1089/adt.2022.038

Hitesh Jamod, Kajal Mehta, Arpit Sakariya, Shweta Shoukani, Bharat Kumar Reddy Sanapalli, Vidyasrilekha Yele

{"title":"Dual Acting Immuno-Antibiotics: Computational Investigation on Antibacterial Efficacy of Immune Boosters Against Isoprenoid H Enzyme.","authors":"Hitesh Jamod, Kajal Mehta, Arpit Sakariya, Shweta Shoukani, Bharat Kumar Reddy Sanapalli, Vidyasrilekha Yele","doi":"10.1089/adt.2022.038","DOIUrl":"https://doi.org/10.1089/adt.2022.038","url":null,"abstract":"Drug-resistant infections have become a serious threat to human health in the past two decades. Global Antimicrobial Surveillance (GLASS) in January 2018 reported widespread antibiotic resistance among 1.5 million people infected with bacteria across 22 countries. According to prominent economist Jim O'Neil, antimicrobial resistance is estimated to kill ∼10 million people affected by microorganisms each year by 2050. Even though multiple therapeutics are now available to treat the infections, more and more bacterial strains have acquired resistance to these treatments through various techniques. Moreover, the decrease in the pipeline of antibacterial medicines under clinical development has become a significant problem. In this scenario, the development of novel antibiotics that act on untapped pathways is necessary to combat the bacterial infections. Isoprenoid H (IspH) synthetase has become an attractive antibacterial target as there is no human homologue. IspH is an enzyme involved in methyl-d-erythritol phosphate (MEP) pathway of isoprenoid synthesis and is conserved in gram-negative bacteria, mycobacteria, and apicomplexans. Since, IspH is a novel therapeutic target, explorations are only just beginning, and despite the progress made in this area, no single IspH inhibitor is available in the market for therapeutic use. In this article, we have repurposed 35 immune boosters against IspH enzyme using methods such as extra-precision docking and Molecular Mechanics Generalized Born Surface Area (MMGBSA). Among them, 4'-fluorouridine was found to be active because of its glide score and significant binding affinity with IspH enzyme. Furthermore, this study requires more in vitro, in vivo, and molecular dynamics studies to support our findings.","PeriodicalId":8586,"journal":{"name":"Assay and drug development technologies","volume":"20 5","pages":"225-236"},"PeriodicalIF":1.8,"publicationDate":"2022-07-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"40505553","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

Formulation and Characterization of Nanostructured Lipid Carriers of Rizatriptan Benzoate-Loaded In Situ Nasal Gel for Brain Targeting. 苯甲酸利扎曲坦原位鼻凝胶纳米结构脂质载体的制备与表征。

IF 1.8 4区医学

Assay and drug development technologies Pub Date : 2022-07-01 Epub Date: 2022-06-30 DOI: 10.1089/adt.2022.044

Dyandevi Mathure, Hemantkumar Ranpise, Rajendra Awasthi, Atmaram Pawar

{"title":"Formulation and Characterization of Nanostructured Lipid Carriers of Rizatriptan Benzoate-Loaded In Situ Nasal Gel for Brain Targeting.","authors":"Dyandevi Mathure, Hemantkumar Ranpise, Rajendra Awasthi, Atmaram Pawar","doi":"10.1089/adt.2022.044","DOIUrl":"https://doi.org/10.1089/adt.2022.044","url":null,"abstract":"Intranasal route provides large surface area, avoids first-pass metabolism, and results in improved drug absorption. Intranasal delivery targets the drug to the brain for treatment of central nervous diseases viz migraine. The objective of the study was to formulate in situ nasal gel containing rizatriptan benzoate (RB)-loaded nanostructured lipid carriers (NLCs). NLCs were prepared by melt-emulsification ultrasonication method and optimized using 32 factorial design. Optimized NLCs were spherical with particle size of 189 nm, high drug encapsulation efficiency (84.5%), and 83.9% drug release at the end of 24 h. RB-loaded NLCs were incorporated into the liquid Carbopol 934P and Poloxamer 407 liquid gelling system to obtain in situ gel formation. The resultant product was assessed for gelling capacity, viscosity, and mucoadhesive strength. In vivo pharmacokinetic studies revealed significant therapeutic concentration of drug in the brain following intranasal administration with Cmax value of 5.1 ng/mL and area under the curve value of 829 ng/(min·mL). Significantly higher values of nose to brain targeting parameters, namely, drug targeting index (2.76) and nose to brain drug direct transport (63.69%) for RB-NLCs in situ nasal gel, confirmed drug targeting to brain through nasal route. The ex vivo nasal toxicity study showed no sign of toxicity to the nasal mucosa. Thus, the application of lipid carrier-loaded in situ gel proved potential for intranasal delivery of RB over the conventional gel formulations for efficient brain targeting.","PeriodicalId":8586,"journal":{"name":"Assay and drug development technologies","volume":"20 5","pages":"211-224"},"PeriodicalIF":1.8,"publicationDate":"2022-07-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"40572021","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: 7

Nanocarriers for Smart Therapeutic Strategies to Treat Drug-Resistant Tumors: A Review. 纳米载体治疗耐药肿瘤的智能治疗策略综述

IF 1.8 4区医学

Assay and drug development technologies Pub Date : 2022-07-01 DOI: 10.1089/adt.2022.025

Abdulsalam A Alqahtani, Hira Aslam, Shazia Shukrullah, Hareem Fatima, Muhammad Yasin Naz, Saifur Rahman, Mater H Mahnashi, Muhammad Irfan

{"title":"Nanocarriers for Smart Therapeutic Strategies to Treat Drug-Resistant Tumors: A Review.","authors":"Abdulsalam A Alqahtani, Hira Aslam, Shazia Shukrullah, Hareem Fatima, Muhammad Yasin Naz, Saifur Rahman, Mater H Mahnashi, Muhammad Irfan","doi":"10.1089/adt.2022.025","DOIUrl":"https://doi.org/10.1089/adt.2022.025","url":null,"abstract":"Combination therapy has become much more effective in treating cancer because it produces combinatorial anticancer results, lowers specific drug-related toxicities, and inhibits multidrug resistivity through several modes of action. Combined drug delivery (CDD) to cancerous tissues, primarily based on nanotechnology, has developed as a viable method in recent years, surpassing various biomedical, biophysical, and biological obstacles that the body erects to prevent antitumor drugs from reaching their target tissues. In a combined strategy, the prolonged, regulated, and targeted administration of chemotherapeutic medicines improves therapeutic anticancer benefits while reducing drug-related adverse effects. CDD systems have several advantages over traditional drug systems, such as improved solubility, higher permeability for traveling through biomembranes, a significantly longer half-life to expand the treatment time, and low cytotoxicity. CDDs are mostly used to treat neurological, cardiovascular, neoplastic, infectious, and inflammatory diseases. Many CDDs are designed to enhance hydrophilicity to improve transportation inside or across biomembranes, particularly the cornea and skin. CDDs could be delivered to particular cells, organs, or tissues, resulting in increased bioavailability. The most widely utilized nanocarriers for CDDs of anticancer medicines are summarized in this review. This study also covers the chemical or enzymatic decomposition of CDDs and their bioactivity and pharmacokinetics. Additional clinical trials will enhance the usefulness of CDDs in treating drug-resistant tumors.","PeriodicalId":8586,"journal":{"name":"Assay and drug development technologies","volume":"20 5","pages":"191-210"},"PeriodicalIF":1.8,"publicationDate":"2022-07-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"40519121","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

Preparation and Optimization of Leuprolide Acetate Nanoparticles Using Response Surface Methodology: In Vitro and Ex Vivo Evaluation. 响应面法制备醋酸Leuprolide纳米颗粒及其优化:体外和离体评价。

IF 1.8 4区医学

Assay and drug development technologies Pub Date : 2022-07-01 DOI: 10.1089/adt.2022.051

Tosha Pandya, Abhay Dharamsi

{"title":"Preparation and Optimization of Leuprolide Acetate Nanoparticles Using Response Surface Methodology: In Vitro and Ex Vivo Evaluation.","authors":"Tosha Pandya, Abhay Dharamsi","doi":"10.1089/adt.2022.051","DOIUrl":"https://doi.org/10.1089/adt.2022.051","url":null,"abstract":"This study aims to develop optimized leuprolide acetate (LA) nanoparticles (NPs) for intranasal delivery in the treatment of Alzheimer's disease. Box-Behnken Design was used to optimize LA polylactide-co-glycolic acid (PLGA) NPs. The independent variables chosen were PLGA concentration, surfactant concentration, and the ratio of water to oil phase, whereas the dependent variables were particle size and % entrapment efficiency. The optimized NPs were evaluated by in vitro drug release study, ex vivo diffusion study, histopathology study, hemolytic stability study, and stability in simulated nasal fluid (SNF). The optimized NPs had particle size of 182.6 ± 1.5 nm, polydispersity index (0.3), % entrapment efficiency (77.3 ± 0.6), and zeta potential (-5.6 mv ±0.2). The in vitro drug release indicated 96% of pure drug release in 6 h, whereas only 66.35% of the drug was released from the optimized formulation at 48 h. The ex vivo diffusion study indicated an apparent permeability coefficient of 5.0 + 0.3 × 104 for drug-containing NPs, which was higher than for plain drug solution (2.0 + 0.2 × 104). Sheep nasal toxicity and hemolytic study proved the safety of formulation. The optimized NPs were found to be stable in SNF. Thus, nanoparticulate formulation of LA was optimized by quality by design approach.","PeriodicalId":8586,"journal":{"name":"Assay and drug development technologies","volume":"20 5","pages":"237-249"},"PeriodicalIF":1.8,"publicationDate":"2022-07-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"40604409","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

Novel Therapeutics Involving Antibiotic Polymer Conjugates for Treating Various Ailments: A Review. 抗生素聚合物偶联物治疗各种疾病的新疗法：综述。

IF 1.8 4区医学

Assay and drug development technologies Pub Date : 2022-06-07 DOI: 10.1089/adt.2022.031

Abhay Tharmatt, Aashveen Chhina, Muskaan Saini, Karan Trehan, Sahilpreet Singh, Neena Bedi

{"title":"Novel Therapeutics Involving Antibiotic Polymer Conjugates for Treating Various Ailments: A Review.","authors":"Abhay Tharmatt, Aashveen Chhina, Muskaan Saini, Karan Trehan, Sahilpreet Singh, Neena Bedi","doi":"10.1089/adt.2022.031","DOIUrl":"https://doi.org/10.1089/adt.2022.031","url":null,"abstract":"Antibiotic polymer conjugates (APCs) are an essential part of polymer therapeutics. These conjugates have been used as an appealing platform for drug delivery. As a delivery vector, the administration route severely impacts the accessibility of antibiotics to their respective target site and therapeutic index. Furthermore, the physicochemical and biological properties of conjugates also correlate distinctly with the route of administration. The APCs delivery methods that have been disclosed so far suffer from significant constraints due to poor technology and constrained administration routes (mainly injections). Leading to promising directions, which include the development of specific characteristics for each polymer carrier, application of novel biodegradable polymers, expansion of traditional drug administration routes through the development of emerging routes, and the development of a rational and systematic methodology for designing administration routes are yet to be explored widely. This review focuses primarily on recent improvements in various routes of administration (dental, topical, and ocular) employing APCs. The mechanism of action, as well as other perspectives, have also been discussed. Moreover, this innovative technology provides a fresh perspective on pharmaceutical science research and offers unique and potential pathways for designing desired APCs.","PeriodicalId":8586,"journal":{"name":"Assay and drug development technologies","volume":" ","pages":""},"PeriodicalIF":1.8,"publicationDate":"2022-06-07","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"44813104","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 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