Written by David J. Snodin
Published on Vol 4 , 2024
Over the past decade, significant changes have occurred in the approach to drug impurity profiling, as reflected in pharmacopeial and regulatory standards. This review provides an in-depth exploration of impurity profiling, focusing on the regulatory requirements. It offers detailed insights into various impurities such as residual solvents, water impurities, elemental contaminants, and carcinogenic substances, with special attention to genotoxic impurities. To meet the required quality standard
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The chemical entities quinazolinone and piperazine are highly valued in organic chemistry due to their broad spectrum of therapeutic and biological activities. To explore their potential applications, researchers developed a novel set of compounds combining quinazolinone and piperazine structures. These compounds, featuring the N-(4-oxo-2-(4-(4-(4-(2-(substituted phenylamino) acetyl) piperazin-1-yl) phenyl) quinazolin-3(4H)-yl) benzamide framework, were synthesized in high yields. Characterizati
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Controlled-release drug delivery systems regulate the plasma drug concentrations through predefined release patterns over a specified period. The release rate directly affects drug absorption and systemic levels. These formulations help in reducing the frequency of daily dosing. This review examines the essential criteria, advantages, characteristics, and strategies for the development of controlled-release formulations to enhance drug delivery. These systems ensure the administration of the dru
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Written by Oscar A. Anunziata
Published on Vol 4 , 2024
This research focuses on the development and validation of cyclophosphamide-loaded microspheres for drug delivery. Cyclophosphamide, which is widely used in cancer therapy and immunosuppression, was analyzed using a newly established method with water as a diluent. The maximum absorption wavelength (λmax) was identified at 263 nm. Various analytical parameters, including linearity, precision, accuracy, limits of detection, robustness, and ruggedness, were assessed. The drug showed linearity over
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Written by Claudia Iftode
Published on Vol 4 , 2024
Repurposing existing drugs for new therapeutic applications offers significant advantages over conventional drug development. Since these drugs have already passed safety evaluations, their failure rate is significantly reduced. In addition, leveraging pre-existing clinical data and established manufacturing methods accelerates the development process and reduces costs. While bringing a new drug to market typically requires 10-17 years and $2-3 billion, repurposed drugs can become available in 3
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WNK (With No Lysine [K]) kinases are serine/threonine kinases implicated in familial hyperkalemic hypertension (FHHt). Beyond blood pressure regulation, WNKs are emerging therapeutic targets for stroke and certain cancers, including triple-negative breast cancer and glioblastoma. In this study, we aimed to identify and characterize novel inhibitors of WNK kinases. A high-throughput screening of approximately 210,000 compounds was performed, followed by compound re-acquisition, secondary assays,
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This study aimed to elucidate the therapeutic mechanisms of Sancao Yuyang Decoction (SCYYD) in managing oral mucositis (OM) through a combination of computational and experimental approaches.Bioactive compounds in SCYYD and their potential molecular targets, along with OM-associated targets, were collected from public databases. Protein–protein interaction (PPI) networks, Gene Ontology (GO), and KEGG pathway analyses were employed to identify core targets and signaling pathways involved in SCYYD
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Written by Frederik Olsen
Published on Vol 4 , 2024
This study aimed to evaluate the protective effects of roxadustat against hypoxia-induced injury during rapid ascent to high altitude. BALB/C mice were randomly assigned to receive roxadustat at doses of 7.8, 15.6, or 31.2 mg/kg, or to control groups. The anti-hypoxic efficacy of roxadustat at the recommended dose was assessed using a controlled atmospheric pressure hypoxia model. Additionally, Wistar rats were randomly allocated to groups exposed to normal oxygen, hypoxia, acetazolamide, or rox
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The mammalian target of rapamycin (mTOR) is a major regulator of cell growth, proliferation, and the cell cycle. The primary component of mTORC2 is markedly upregulated in prostate cancer cells that have developed resistance to docetaxel. However, its specific molecular effects in prostate cells have not been fully defined.
A docetaxel-resistant prostate cancer cell line (PC-3/DTX) was established to examine the function of mTORC2 in drug resistance. Lentiviral vectors were used to silence Ricto
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Oral absorption of poorly water-soluble drugs like simvastatin is often limited. Self-emulsifying drug-delivery systems (SEDDSs) offer a strategy to enhance solubility and bioavailability. This study aimed to develop and evaluate SEDDS-based tablets of simvastatin using castor and olive oils as the lipid phase and Tween 60 as the surfactant.Liquid SEDDS formulations were adsorbed onto microcrystalline cellulose and compressed into tablets using 10.5 mm shallow concave punches. The tablets were t
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Written by Amelie Dubois
Published on Vol 4 , 2024
Paclitaxel is a key drug in cancer therapy, yet its clinical benefit is often constrained by pronounced toxicity and the development of resistance. 10-Gingerol (10-G), a naturally occurring ginger-derived molecule with known anti-inflammatory and antiproliferative actions, has been proposed as a potential chemosensitizer. However, its influence on the response of triple-negative breast cancer (TNBC) to paclitaxel has not been clearly defined. This work investigates whether 10-G can improve pacli
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Written by Gabriel Johansen
Published on Vol 4 , 2024
Vancomycin (VCM) is commonly used to treat infections caused by Gram-positive bacteria. However, over the past decades, VCM overdose has increasingly been linked to kidney damage. The mechanisms driving this nephrotoxicity remain incompletely understood. This study aimed to investigate how VCM induces renal injury.Kidney tissues from mice were analyzed for the expression of Ki67, DDX5, PTGS2, GPX4, and SLC7A11 using immunohistochemistry, RT-qPCR, and Western blot. In parallel, HK-2 cells were as
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Written by Hiroshi Tanaka
Published on Vol 4 , 2024
This research aimed to elucidate the mechanisms through which the Zuogui Jiangtang Shuxin formula (ZGJTSXF) alleviates diabetic cardiomyopathy (DCM) using a combined approach of serum pharmacochemistry, network pharmacology, and experimental validation.Following oral administration of ZGJTSXF in rats, serum compounds were analyzed using UPLC-Q-Exactive-Orbitrap-MS. A network linking bioactive components of ZGJTSXF to DCM-associated targets was established with Cytoscape. Functional enrichment an
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Sichen (SC) formula, a well-known Tibetan medicinal preparation, has been traditionally applied to treat respiratory ailments in Tibet due to its anti-inflammatory potential. This study aimed to systematically investigate its anti-inflammatory effects and the molecular mechanisms involved.The chemical profile of SC was analyzed using HPLC. An acute lung injury (ALI) model in mice was established by intratracheal administration of lipopolysaccharide (LPS), with subsequent collection of bronchoalv
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Written by Caroline Fischer
Published on Vol 4 , 2024
Glucocorticoids (GCs) are the primary treatment for ulcerative colitis (UC), but their long-term use is associated with severe systemic toxicity and side effects. Local delivery via enema can enhance GC concentrations at the site of inflammation in the distal colon while minimizing systemic exposure. However, frequent diarrhea in UC patients often shortens colonic residence time, limiting the therapeutic efficacy of GCs.This study aimed to develop mucoadhesive nanoparticles (NPs) carrying differ
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Click chemistry provides a powerful method for selectively linking diverse molecular building blocks to create sophisticated molecules efficiently. Here, we report the use of copper(I)-catalyzed biorthogonal cycloaddition between alkynes and azides for the indirect incorporation of fluorine-18 into an estradiol-based compound, aimed at imaging estrogen receptors. The synthesis protocol was entirely established and refined using an automated module, with parameters adjusted to deliver the target
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Written by Thomas Berger
Published on Vol 4 , 2024
Breast cancer originates in breast tissue cells and primarily affects women. It typically begins in the cells lining the milk ducts or the lobules that produce milk, with the potential to invade surrounding tissues and metastasize to distant parts of the body. In 2020, approximately 2.3 million women worldwide were diagnosed with the disease, resulting in an estimated 685,000 deaths. Furthermore, 7.8 million women were alive with a breast cancer diagnosis, establishing it as the fifth leading ca
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Written by Maria Gonzalez
Published on Vol 4 , 2024
Due to the rising incidence of diabetes mellitus and the drawbacks of existing therapies, there is an urgent demand for new therapeutic agents targeting this condition. This research concentrates on developing novel compounds with potent alpha-glucosidase inhibitory activity, a key enzyme in managing diabetes. A series of 33 triazole derivatives was subjected to comprehensive QSAR analysis to determine the critical factors affecting their α-glucosidase inhibitory potency. Based on the multiple l
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Written by Anders Nilsson
Published on Vol 4 , 2024
The purpose of this research was to create a binary nanodrug-delivery platform functionalized with aptamers (APs) and transferrin (Tf), and encapsulating daunorubicin (Drn) and luteolin (Lut) for leukemia therapy. Oligonucleotide ligands containing APs and Tf were designed and synthesized independently. AP-functionalized nanoparticles loaded with Drn (AP-Drn NPs) and Tf-functionalized nanoparticles loaded with Lut (Tf-Lut NPs) were fabricated through self-assembly. A binary nanodrug-delivery sys
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A series of diterpenoid 1,3-aminoalcohol derivatives was synthesised from isosteviol through stereoselective transformations. Isosteviol was obtained via acid-catalysed hydrolysis and rearrangement of natural stevioside and subsequently converted to the key methyl ester intermediate. A 1,3-aminoalcohol library was then constructed by reductive amination of the 3-hydroxyaldehyde intermediate derived from isosteviol in a two-step process. To evaluate the influence of the carboxylate ester at posit
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