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α-Tocopherol Polyethylene Glycol 1000 Succinate-Based Cationic Liposome for the Intracellular Delivery of Doxorubicin in MDA-MB-231 Triple-Negative Breast Cancer Cell Line. Assay Drug Dev. Technol. (IF 1.8) Pub Date : 2023-11-21 Pallavi Sandal,Preeti Patel,Dilpreet Singh,Ghanshyam Das Gupta,Balak Das Kurmi
Present research work reports the development of doxorubicin (DOX) loaded α-tocopherol polyethylene glycol 1000 succinate (TPGS)-coated cationic liposomes. The developed formulation was evaluated for its anticancer potential and intracellular uptake against the MDA-MB-231 breast cancer cell line. Moreover, hemocompatibility studies were also done on human blood red blood cells for the determination
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A Short Appraisal of Biomimetic Hydrogels to Improve Penetration of Poorly Permeable Drugs. Assay Drug Dev. Technol. (IF 1.8) Pub Date : 2023-11-21 Dilpreet Singh,Sahil Arora,Vimal Arora
Effective drug delivery to target sites is critical for achieving desired therapeutic outcomes. However, the poor permeability of certain drugs poses significant challenges in achieving adequate drug concentrations at the desired locations. Biomimetic hydrogels have emerged as a promising approach to enhance the penetration of poorly permeable drugs. These hydrogels, designed to mimic natural biological
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Letter to the Editor: Concerns Regarding Ethical Issues in Reviewer Recommendations for Citations. Assay Drug Dev. Technol. (IF 1.8) Pub Date : 2023-11-15 Rajendra Awasthi
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Letter to the Editor: Repurposing Tafenoquine as a Potential Inhibitor Against Severe Acute Respiratory Syndrome Coronavirus 2 Main Protease via a Fluorescence Polarization Assay. Assay Drug Dev. Technol. (IF 1.8) Pub Date : 2023-11-07 Rui Zhang,Haohao Yan,Gangan Yan,Xiaoping Liu,Yunyu Chen
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Illuminating Insights: Clinical Study Harnessing Pharmacoscintigraphy for Permeation Study of Radiolabeled Nimesulide Topical Formulation in Healthy Human Volunteers. Assay Drug Dev. Technol. (IF 1.8) Pub Date : 2023-10-06 Nitin Sharma,Kushagra Khanna,Neeraj Kumar,Ritu Karwasra,Ashok Kumar Janakiraman,Mogana Sundari Rajagopal
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)
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Formulation and Characterization of Nanoparticulate Drug Carrier System for Lacidipine. Assay Drug Dev. Technol. (IF 1.8) Pub Date : 2023-10-01 Ashveta Anant Dessai,Mrunali Navin Kantak,Cleona Elizabeth Mary DCruz,Lalit Kumar,Prashant Jivaji Bhide,Rupesh Kalidas Shirodkar
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
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Determination of the Toxicity Preferences of Ocular Drug Delivery System by Comparing Two Different Toxicity Bioassays. Assay Drug Dev. Technol. (IF 1.8) Pub Date : 2023-10-01 Burcu Uner,Meltem Ezgi Durgun,Samet Ozdemir,Cetin Tas,Melike Uner,Yildiz Ozsoy
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
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Quality by Design Approach for Optimization of Microbial and pH-Triggered Colon-Targeted Tablet Formulation Using Carboxymethyl Tamarind Gum. Assay Drug Dev. Technol. (IF 1.8) Pub Date : 2023-10-01 Jaymin Patel,Kaushika Patel,Shreeraj Shah
ABSTRACT The purpose of this study was to apply the quality by design (QbD) approach in the development of a microbial and pH-triggered colon-targeted budesonide tablet. A retrospective research strategy was used to select various polysaccharide-based natural gums such as tamarind gum, gellan gum, karaya gum, gum ghutti, and khaya gum, which were then evaluated for their effectiveness in microbial
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Adjusting the Fitting of Fluorescence-Based Dose-Response Kinase Inhibition Assay to Account for Fluorescent Inhibitors. Assay Drug Dev. Technol. (IF 1.8) Pub Date : 2023-09-28 Guillaume A Petit
Fluorescence is routinely used to monitor kinase inhibition in commercial assays. Occasionally fluorescent compounds can interfere with the fluorescent reading. To address this issue, the problematic data are usually truncated to improve the fit, however, this approach raises ethical and reproducibility concerns. Instead, it is suggested to adjust the fitting formula, to account for the autofluorescence
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Exploration of the Mechanism of Shengxian Decoction Against Chronic Obstructive Pulmonary Disease Based on Network Pharmacology and Experimental Verification. Assay Drug Dev. Technol. (IF 1.8) Pub Date : 2023-09-08 Yifei Chen,Yiming Wang,Zheng Li,Jing Jing,De Jiang,Xiaoxia Yuan,Fengsen Li
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
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Development and Method Validation of Design of Experiments-Optimized Tablet Formulation for Simultaneous Detection of Exemestane and Everolimus. Assay Drug Dev. Technol. (IF 1.8) Pub Date : 2023-09-08 Akshay Kumar,Balak Das Kurmi,Dilpreet Singh
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
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Design, Synthesis, Molecular Docking, and Biological Evaluation of Isatin-Based Fused Heterocycles As Epidermal Growth Factor Receptor Inhibitors. Assay Drug Dev. Technol. (IF 1.8) Pub Date : 2023-07-12 Ankush Kumar,Bhupinder Kumar,Rohit Bhatia
A series of isatin-based fused heterocycles were designed, synthesized, and evaluated for anticancer activity against four cancer cell lines: MCF-7, MDA-MB-231, A549, and HL-60. Among them, Q3 and T4 were found to be potent anticancer agents. Furthermore, two compounds Q3 and T4 were selected for epidermal growth factor receptor (EGFR) inhibitory activity. Two compounds Q3 and T4 were found to be most
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TWIST1 Promotes Colorectal Carcinoma Stemness and Oxaliplatin Resistance by Activating Microfibrillar-Associated Protein 2. Assay Drug Dev. Technol. (IF 1.8) Pub Date : 2023-07-10 Ying Liu,Minhan Chen,Bo Wu
Colorectal carcinoma (CRC) is a fatal disease and ranks as the third most prevalent cancer globally. Stemness and drug resistance are the main causes of tumor recurrence in CRC. This study attempted to probe the impact of TWIST1 on CRC stemness and resistance to oxaliplatin and to uncover the underlying regulatory mechanism of TWIST1. mRNA expression data from The Cancer Genome Atlas-CRC were subjected
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Enhanced Cytotoxic Activity of 6-Mercaptopurine-Loaded Solid Lipid Nanoparticles in Hepatic Cancer Treatment. Assay Drug Dev. Technol. (IF 1.8) Pub Date : 2023-07-07 Ahmet Doğan Ergin,Çağatay Oltulu,Büşra Koç
6-Mercaptopurine (6-MCP) is an antiproliferative purine analog used in acute lymphoblastic leukemia, non-Hodgkin lymphoma, and inflammatory bowel disease (Crohn's disease, ulcerative colitis). Although 6-MCP has the great therapeutic potential for cancer and immunosuppressant-related diseases, 6-MCP is not readily soluble in water, presents a high first-pass effect, short half-life (0.5-1.5 h), and
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Biosensor Assays Types and Their Roles Toward Ligand-Receptor Interactions in Drug Discovery. Assay Drug Dev. Technol. (IF 1.8) Pub Date : 2023-06-06 Garima Gupta,Kanupriya Jha,Sarika Chaudhary
Ligand-receptor interactions (LRIs) are the basis for all the biological processes taking place in living cells and have been exploited to develop and implement in medical field a number of highly sensitive biosensors for the detection of various biomarkers in complex biological fluids. Drug-target interactions, one of the LRIs, are important to understand the biological processes that further help
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Losartan Plays a Fungistatic and Fungicidal Activity Against Candida albicans Biofilms: Drug Repurposing for Localized Candidosis. Assay Drug Dev. Technol. (IF 1.8) Pub Date : 2023-05-25 Vanessa Soares Lara,Rafaela Alves da Silva,Tatiane Ponteado Ferrari,Carlos Ferreira Dos Santos,Sandra Helena Penha de Oliveira
Candidosis is one of the most frequent opportunistic infections and exhibits variable clinical presentations, including oral localized forms. Drugs affecting the renin-angiotensin system targets inhibit secreted aspartic proteases from Candida albicans. The objective of the study was to evaluate whether losartan has antimicrobial action against C. albicans biofilms. Biofilms were treated with losartan
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Doxorubicin Conjugates: An Efficient Approach for Enhanced Therapeutic Efficacy with Reduced Side Effects. Assay Drug Dev. Technol. (IF 1.8) Pub Date : 2023-04-20 Pallavi Sandal,Lakshmi Kumari,Preeti Patel,Amrinder Singh,Dilpreet Singh,Ghanshyam Das Gupta,Balak Das Kurmi
Continuous drug delivery modification is the scientific approach and is a basic need for the efficient therapeutic efficacy of active drug molecules. Polymer-drug conjugates have long been a hallmark of the drug delivery sector, with various conjugates on the market or in clinical trials. Improved drug solubilization, extended blood circulation, decreased immunogenicity, controlled release behavior
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High-Throughput Ultra Performance Liquid Chromatography-Tandem Mass Spectrometry Method Validation for the Estimation of Atorvastatin and Active Metabolites in Human Plasma. Assay Drug Dev. Technol. (IF 1.8) Pub Date : 2023-04-01 Nikhil Agrawal,Amit Mittal
A highly selective, sensitive, rugged, and rapid ultra high-performance liquid chromatography-tandem mass spectrometry method (UPLC-MS/MS) is optimized and validated for reliable quantification of atorvastatin (ATR) and its active metabolites, 2-hydroxy atorvastatin (2-ATR) and 4-hydroxy atorvastatin (4-ATR) in human plasma using atorvastatin-D5 (ATR-D5), 2-hydroxy atorvastatin-D5 (2-ATR-D5), and 4-hydroxy
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Validation of a Novel Supercritical Fluid Extractor/Dryer Combo Instrument. Assay Drug Dev. Technol. (IF 1.8) Pub Date : 2023-03-30 Mritunjay Kumar,Yash Sharma,Kanak Chahar,Lakshmi Kumari,Lopamudra Mishra,Preeti Patel,Dilpreet Singh,Balak Das Kurmi
The current pharmaceutical manufacturing scenario involves different techniques for the processing of materials. For example, the extraction unit is one of the essential aspects of plant-based pharmaceuticals. Recently, various kinds of extraction techniques have been used for analytical and preparative scales; among them, a supercritical fluid extractor (SCFE) is the most widely used technique for
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Oral Gastroretentive Film of Lacidipine for the Treatment of Gastroparesis. Assay Drug Dev. Technol. (IF 1.8) Pub Date : 2023-03-28 Mrunali Navin Kantak,Lalit Kumar,Prashant Jivaji Bhide,Rupesh Kalidas Shirodkar
The research work was aimed to formulate and evaluate gastroretentive mucoadhesive film of calcium channel blocker, Lacidipine for treatment of gastroparesis. Box-Behnken design was used for preparation of optimized formulation using solvent casting method. In this design, different concentrations of mucoadhesive polymers HPMC E15, Eudragit RL100, and Eudragit RS100 were considered as independent variables
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Identification of Potent, Selective, and Peripherally Restricted Serotonin Receptor 2B Antagonists from a High-Throughput Screen. Assay Drug Dev. Technol. (IF 1.8) Pub Date : 2023-03-17 Aaron M Bender,Michael S Valentine,Joshua A Bauer,Emily Days,Craig W Lindsley,W David Merryman
Antagonists of the serotonin receptor 2B (5-HT2B) have shown great promise as therapeutics for the treatment of pulmonary arterial hypertension, valvular heart disease, and related cardiopathies. Herein, we describe a high-throughput screen campaign that led to the identification of highly potent and selective 5-HT2B antagonists. Furthermore, selected compounds were profiled for their predicted ability
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Pharmaceutical Methods for Enhancing the Dissolution of Poorly Water-Soluble Drugs. Assay Drug Dev. Technol. (IF 1.8) Pub Date : 2023-01-01 Tahir Mahmood,Rai M Sarfraz,Asmara Ismail,Muhammad Ali,Abdur Rauf Khan
Low water solubility is the main hindrance in the growth of pharmaceutical industry. Approximately 90% of newer molecules under investigation for drugs and 40% of novel drugs have been reported to have low water solubility. The key and thought-provoking task for the formulation scientists is the development of novel techniques to overcome the solubility-related issues of these drugs. The main intention
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A Sojourn on Liposomal Delivery System: Recent Advances and Future Prospects. Assay Drug Dev. Technol. (IF 1.8) Pub Date : 2023-02-28 Simranjeet Kaur,Dilpreet Singh
Liposomes are unique novel drug delivery carriers that favor the effective transportation of pharmaceuticals. These vesicles acquire one or more phospholipid bilayer membranes, and an inner aqueous core can carry both aqueous and lipid drugs. While hydrophilic molecules can be confined in the aqueous core, hydrophobic molecules are injected into the bilayer membrane. Liposomes have many benefits as
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A Critical Sojourn of Polymeric Micelles: Technological Concepts, Recent Advances, and Future Prospects. Assay Drug Dev. Technol. (IF 1.8) Pub Date : 2023-02-28 Princi Verma,G D Gupta,Tanmay S Markandeywar,Dilpreet Singh
Poorly soluble drug molecules/phytoconstituents are still a growing concern for biopharmaceutical delivery in the body. Polymeric micelles are the amphiphilic block copolymers and have been widely investigated as targeted nanocarriers for the treatment of various ailments. The versatility of nanocarriers is the self-assembling properties in the aqueous medium and forms a stable isotropic system in
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Preparation and Optimization of Liposome Containing Thermosensitive In Situ Nasal Hydrogel System for Brain Delivery of Sumatriptan Succinate Assay Drug Dev. Technol. (IF 1.8) Pub Date : 2023-01-17 Dyandevi Mathure, Ashish Dilip Sutar, Hemantkumar Ranpise, Atmaram Pawar, Rajendra Awasthi
Drug absorption is improved by the intranasal route's wide surface area and avoidance of first-pass metabolism. For the treatment of central nervous system diseases such as migraine, intranasal administration delivers the medication to the brain. The study's purpose was to develop an in situ nasal hydrogel that contained liposomes that were loaded with sumatriptan succinate (SS). A thin-film hydration
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Design, Synthesis, and Biological Evaluation of Novel Dihydropyrimidinone Derivatives as Potential Anticancer Agents and Tubulin Polymerization Inhibitors Assay Drug Dev. Technol. (IF 1.8) Pub Date : 2023-01-17 Ramkaran 1 , Ravindra K. Rawal, Praveen K. Gupta, Bhupinder Kumar, Rohit Bhatia
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
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In-Silico Design, Synthesis, and Pharmacological Evaluation of Oxadiazole-Based Selective Cyclo-oxygenase-2 Inhibitors. Assay Drug Dev. Technol. (IF 1.8) Pub Date : 2023-01-01 Manish Kumar,Isha Rani,Somdutt Mujwar,Rakesh Narang,Manish Devgun,Sukhbir Lal Khokra
A series of oxadiazole-based five-membered heterocyclic derivatives was designed and synthesized with the intent of exclusive cyclo-oxygenase-2 (COX-2) inhibition to acquire anti-inflammatory activity without the presence of gastric toxicity. Oxadiazole-based novel analogs were designed by using bioisosteric substitutions and were screened against the macromolecular target by using docking-based virtual
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On the Recent Changes to Animal Protection Measures in United States Food and Drug Administration Policy. Assay Drug Dev. Technol. (IF 1.8) Pub Date : 2023-01-01 Bruce J Melancon
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Silibinin-Loaded Nanostructured Lipid Carriers for Growth Inhibition of Cisplatin-Resistant Ovarian Cancer Cells Assay Drug Dev. Technol. (IF 1.8) Pub Date : 2022-12-15 Sevda Jafari, Atabak Bakhshaei, Morteza Eskandani, Ommoleila Molavi
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
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Development and Validation of Reverse-Phase High-Performance Liquid Chromatography Based Bioanalytical Method for Estimation of Simvastatin in Rat's Plasma Assay Drug Dev. Technol. (IF 1.8) Pub Date : 2022-12-15 Hardeep, Narendra Kumar Pandey, Sachin Kumar Singh, Bimlesh Kumar, Leander Corrie, Umesh Goutam, Dileep Singh Baghel
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
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Potential Assessment of Topical Felbinac-Loaded Cubosomal Gel in Soft Tissue Injury in Albino Rats Assay Drug Dev. Technol. (IF 1.8) Pub Date : 2022-12-15 Snigdha Bhardwaj, Anshul, Praveen Kumar Gaur, Sonam Bhatia
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
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Healing Potential of Propolis Extract–Passiflora edulis Seed Oil Emulgel Against Excisional Wound: Biochemical, Histopathological, and Cytokines Level Evidence Assay Drug Dev. Technol. (IF 1.8) Pub Date : 2022-10-17 Puneet Gupta, Ashish Singh, Neelam Singh, Faraat Ali, Ayushi Tyagi, Sadish K. Shanmugam
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
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Computational Design of Phosphatidylinositol 3-Kinase Inhibitors Assay Drug Dev. Technol. (IF 1.8) Pub Date : 2022-10-17 Isha Rani, Anju Goyal, M. Sharma
One of the most sought-after therapeutic targets for treating human cancers is the phosphoinositide 3-kinase; PI3k is an integral part of the PI3K/protein kinase B signaling arcade. This pathway is frequently activated in malignancies. Drug resistance and dose-limiting adverse effects are currently associated challenges with the existing anticancer chemotherapy. Therefore, in this research, a series
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Editor's Response to a Letter on "3D Printing Has an Imperative Role in Colitis Management" by Sahoo and Singh. Assay Drug Dev. Technol. (IF 1.8) Pub Date : 2022-10-11 Bruce J Melancon
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Letter to the Editor: 3D Printing Has an Imperative Role in Colitis Management. Assay Drug Dev. Technol. (IF 1.8) Pub Date : 2022-10-11 Sarmili Sahoo,Amandeep Singh
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PEGylation of Nanoemulsion Using Spontaneous Emulsification Method Assay Drug Dev. Technol. (IF 1.8) Pub Date : 2022-09-14 S.K. Janani, S.P. Dhanabal, R. Sureshkumar, Sai Surya Nikitha Upadhyayula
Nanoemulsion (NE), a lipid-based drug delivery system, plays an important role in delivering drugs and enhancing bioavailability. They are mainly taken up by the reticuloendothelial system, because of which their bioavailability is diminished, leading to poor therapeutic activity. It is important to protect this delivery system using a coating agent. Thus, we have coated o/w type NE using polyethylene
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A Review on Delivery and Bioavailability Enhancement Strategies of Azithromycin Assay Drug Dev. Technol. (IF 1.8) Pub Date : 2022-09-14 Pallavi Swarup, Gopal Prasad Agrawal
Azithromycin (AZI) belongs to the class of macrolide antibiotics that has limited water solubility and belongs to Biopharmaceutical Classification System Class II. Dissolution is the rate-limiting step in the absorption process of AZI. Several approaches have been investigated for enhancing the bioavailability of poorly soluble drugs. This review intends to explore the various strategies that have
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Solubility Enhancement of Ebastine by Formulating Microemulsion Using D-Optimal Mixture Design: Optimization and Characterization Assay Drug Dev. Technol. (IF 1.8) Pub Date : 2022-09-14 Apoorva Ratnakar Barve, Gauri Ramchandra Kapileshwari, Cleona Elizabeth Mary DCruz, Lalit Kumar, Prashant Jivaji Bhide, Anand Avinash Mahajan, Asmita Sunil Arondekar, Rupesh Kalidas Shirodkar
Ebastine, a histamine H1 antagonist, nonsedating, belonging to BCS class II is used in the treatment of allergic rhinitis and chronic idiopathic urticaria. The current study was intended in augmenting the aqueous solubility and dissolution rate of ebastine, by formulating a microemulsion system using oleic acid, Transcutol® HP, and Tween®80 as oily phase, cosurfactant, and surfactant, respectively
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Nanocarriers for Smart Therapeutic Strategies to Treat Drug-Resistant Tumors: A Review Assay Drug Dev. Technol. (IF 1.8) Pub Date : 2022-07-18 Abdulsalam A. Alqahtani, Hira Aslam, Shazia Shukrullah, Hareem Fatima, Muhammad Yasin Naz, Saifur Rahman, Mater H. Mahnashi, Muhammad Irfan
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
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Formulation and Characterization of Nanostructured Lipid Carriers of Rizatriptan Benzoate-Loaded In Situ Nasal Gel for Brain Targeting Assay Drug Dev. Technol. (IF 1.8) Pub Date : 2022-07-18 Dyandevi Mathure, Hemantkumar Ranpise, Rajendra Awasthi, Atmaram Pawar
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
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Dual Acting Immuno-Antibiotics: Computational Investigation on Antibacterial Efficacy of Immune Boosters Against Isoprenoid H Enzyme Assay Drug Dev. Technol. (IF 1.8) Pub Date : 2022-07-18 Hitesh Jamod, Kajal Mehta, Arpit Sakariya, Shweta Shoukani, Bharat Kumar Reddy Sanapalli, Vidyasrilekha Yele
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
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Preparation and Optimization of Leuprolide Acetate Nanoparticles Using Response Surface Methodology: In Vitro and Ex Vivo Evaluation Assay Drug Dev. Technol. (IF 1.8) Pub Date : 2022-07-18 Tosha Pandya, Abhay Dharamsi
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
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Novel Therapeutics Involving Antibiotic Polymer Conjugates for Treating Various Ailments: A Review Assay Drug Dev. Technol. (IF 1.8) Pub Date : 2022-06-16 Abhay Tharmatt, Aashveen Chhina, Muskaan Saini, Karan Trehan, Sahilpreet Singh, Neena Bedi
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
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Evolution of Solid Dispersion Technology: Solubility Enhancement Using Hydroxypropyl Methylcellulose Acetate Succinate: Myth or Reality? Assay Drug Dev. Technol. (IF 1.8) Pub Date : 2022-06-16 N. Raveendra Babu, Dheeraj Nagpal, Dhawal Ankola, Rajendra Awasthi
Poorly aqueous soluble active pharmaceutical ingredients are highly risky development candidates and remain a concern of pharmaceutical industries in drug discovery and development processes. Pharmaceutical industries are putting significant efforts into the target identification and lead candidate development using combinatorial chemistry. About 40% of compounds arising from combinatorial screening
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Formulation and Characterization of Raloxifene Nanostructured Lipid Carriers for Permeability and Uptake Enhancement Applications Assay Drug Dev. Technol. (IF 1.8) Pub Date : 2022-06-16 Anju Sharma, Jarriaun Streets, Priyanka Bhatt, Pranav Patel, Vijaykumar Sutariya, Sheeba Varghese Gupta
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
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Rapid High-Throughput Assay Identified Gemcitabine and Derivatives As Potent Inhibitors Against Multidrug-Resistant Staphylococcus aureus Assay Drug Dev. Technol. (IF 1.8) Pub Date : 2022-06-16 Zhao Chen, Jinxiu Li, Yue Wan, Ruisong Bai, Wenjuan Wang, Xuan Gao, Di Li, Qingfeng Hu, Yong Li, Benfang Helen Ruan
Methicillin-resistant Staphylococcus aureus (MRSA) are challenging pathogenic bacteria that can cause severe infection leading to high mortality rates. We found that both the oxacillin- and cefoxitin-resistant S. aureus strains isolated from clinic showed multidrug-resistant (MDR) characteristics. Through rapid high-throughput screen (HTS) of a compound library, gemcitabine and selen compounds were
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Development of a High-Throughput Screening Assay for Small-Molecule Inhibitors of Androgen Receptor Splice Variants Assay Drug Dev. Technol. (IF 1.8) Pub Date : 2022-04-18 Amy E. Monaghan, Alison Porter, Irene. Hunter, Angus Morrison, Stuart P. McElroy, Iain J. McEwan
The role of the androgen receptor (AR) in the progression of prostate cancer (PCa) is well established and competitive inhibition of AR ligand binding domain (LBD) has been the mainstay of antiandrogen therapies for advanced and metastatic disease. However, the efficacy of such drugs is often limited by the emergence of resistance, mediated through point mutations and receptor splice variants lacking
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Developmental Cardiotoxicity and Hepatotoxicity of Flurbiprofen Axetil to Zebrafish Embryo Assay Drug Dev. Technol. (IF 1.8) Pub Date : 2022-04-18 Yuping Wang, Min Zhou, Jing Wang, Chuantao Lin, Xiang Gao, Li Zhang, Wenshui Yao, Longxin Zhang
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
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Call for Special Issue Papers: Chemical Probes and Pharmacological Tools for Imaging Applications Assay Drug Dev. Technol. (IF 1.8) Pub Date : 2022-04-01 Milka Kostic,Bruce J. Melancon
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Call for Special Issue Papers: New Modalities in Chemical Probes and Pharmacological Tools in Drug Discovery. Assay Drug Dev. Technol. (IF 1.8) Pub Date : 2022-04-01 Milka Kostic,Bruce J Melancon
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Interview with Craig W. Lindsley, PhD. Assay Drug Dev. Technol. (IF 1.8) Pub Date : 2022-03-31 Bruce J Melancon
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Modifications to the Transwell Migration/Invasion Assay Method That Eases Assay Performance and Improves the Accuracy Assay Drug Dev. Technol. (IF 1.8) Pub Date : 2022-03-08 Heidi Marie Stoellinger, Arshak R. Alexanian
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
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A New Spectral Shift-Based Method to Characterize Molecular Interactions Assay Drug Dev. Technol. (IF 1.8) Pub Date : 2022-03-08 Andreas Langer, Tanja Bartoschik, Ondrej Cehlar, Stefan Duhr, Philipp Baaske, Werner Streicher
There are many fluorescence-based applications that can be used to characterize molecular interactions. However, available methods often depend on site-specific labeling techniques or binding-induced changes in conformation or size of the probed target molecule. To overcome these limitations, we applied a ratiometric dual-emission approach that quantifies ligand-induced spectral shifts with sub-nanometer
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Automated Assays to Identify Modulators of Transcription Factor EB Translocation and Autophagy Assay Drug Dev. Technol. (IF 1.8) Pub Date : 2022-03-08 Anaelle da Costa, Christèle Picoli, Franck Mouthon, Mathieu Charvériat
Autophagy is a process leading to the degradation of cellular material, in organelles called lysosomes, to supply energy or generate building blocks for the synthesis of new materials. Over the past decades, its role has been evidenced in several indications, notably in neurodegenerative disorders and orphan diseases called lysosomal storage disorders and its modulation is largely envisioned as a therapeutic
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Drug Repurposing Patent Applications October: December 2021 Assay Drug Dev. Technol. (IF 1.8) Pub Date : 2022-03-01 Hermann A.M. Mucke
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Call for Special Issue Papers: Chemical Probes and Pharmacological Tools for Kinase Signaling Assay Drug Dev. Technol. (IF 1.8) Pub Date : 2022-02-03 Milka Kostic,Bruce J. Melancon
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Call for Special Issue Papers: Special Issue on High-throughput Technologies for the Discovery and Development of Chemical Probes and Pharmacological Tools Assay Drug Dev. Technol. (IF 1.8) Pub Date : 2022-02-03 Milka Kostic,Bruce J. Melancon