An Evaluation of Amoxicillin/Clavulanate Stability in Aqueous Systems, Including Its Suitability for Outpatient Parenteral Antimicrobial Therapy (OPAT).

Purpose: Amoxicillin/clavulanate antibiotic combination is suitable for treating a range of infections, including some suited for Outpatient Parenteral Antimicrobial Therapy (OPAT). The aim of the study was to evaluate shelf-life values of amoxicillin at clinical concentrations in the presence of clavulanate for use in OPAT.

Methods: A stability-indicating HPLC assay was developed and validated.

Synthesis and Structure-Activity Relationship Analysis of 2-Substituted-1,2,4-Triazolo[1,5-a]Pyrimidin-7-Ones and their 6-Carboxylate Derivatives as Xanthine Oxidase Inhibitors.

Hyperuricemia is characterised by high blood levels of uric acid, and it can degenerate into gout when monosodium urate crystals precipitate in joints and other tissues. Uric acid is produced during the catabolism of xanthine by the enzyme xanthine oxidase (XO), which is the primary therapeutic target in gout treatment. Current XO inhibitors approved to treat gout, such as allopurinol and febuxostat, suffer from serious adverse effects, creating the need for new drug molecules.

The therapeutic potential of probucol and probucol analogues in neurodegenerative diseases.

Neurodegenerative disorders present complex pathologies characterized by various interconnected factors, including the aggregation of misfolded proteins, oxidative stress, neuroinflammation and compromised blood-brain barrier (BBB) integrity. Addressing such multifaceted pathways necessitates the development of multi-target therapeutic strategies. Emerging research indicates that probucol, a historic lipid-lowering medication, offers substantial potential in the realm of neurodegenerative disease prevention and treatment.

BinBench: a benchmark for x64 portable operating system interface binary function representations.

In this article we propose the first multi-task benchmark for evaluating the performances of machine learning models that work on low level assembly functions. While the use of multi-task benchmark is a standard in the natural language processing (NLP) field, such practice is unknown in the field of assembly language processing. However, in the latest years there has been a strong push in the use of deep neural networks architectures borrowed from NLP to solve problems on assembly code.

Metabolomics Profiling Reveals the Role of PEDF in Triple-Negative Breast Cancer Cell MDA-MB-231 under Glycaemic Loading.

Pigment epithelium-derived factor (PEDF) is a secreted glycoprotein that belongs to the serine protease inhibitor (serpin) family. An increase in PEDF activity has been shown to be a potent inhibitor of tumour progression and proliferation, suggesting a possible therapeutic target. There is still a great deal to learn about how PEDF controls metabolic pathways in breast cancer and its metastatic form.

Novel Silicone-Grafted Alginate as a Drug Delivery Scaffold: Pharmaceutical Characterization of Gliclazide-Loaded Silicone-Based Composite Microcapsules.

A novel gliclazide-loaded elastomeric carbohydrate pharmaceutical vehicle was successfully developed. This new siliconized alginate platform showed pseudoplastic rheology with a zeta potential ranging from (-43.8 mV to -75.

Novel Self-Nano-Emulsifying Drug Delivery Systems Containing Astaxanthin for Topical Skin Delivery.

Astaxanthin (ASX) is a potent lipophilic antioxidant derived from the natural pigment that gives marine animals their distinctive red-orange colour and confers protection from ultraviolet radiation. Self nano-emulsifying drug delivery systems (SNEDDS) have been successfully developed and evaluated to increase the skin penetration of ASX and target its antioxidant and anti-inflammatory potential to the epidermis and dermis. SNEDDS were prepared using a low-temperature spontaneous emulsification method, and their physical characteristics, stability, antioxidant activity, and skin penetration were characterized.

Compacting oblivious agents on dynamic rings.

In this paper we investigate dynamic networks populated by autonomous mobile agents. Dynamic networks are networks whose topology can change continuously, at unpredictable locations and at unpredictable times. These changes are not considered to be faults, but rather an integral part of the nature of the system.

An investigation of reconstituted terlipressin infusion stability for use in hepatorenal syndrome.

Hepatorenal syndrome (HRS) is a fatal complication of renal dysfunction associated with ascites, liver failure and advanced cirrhosis. Although the best option for long-term survival is liver transplantation, in the critical acute phase, vasoconstrictors are considered first-line supportive agents. Terlipressin is the most widely used vasoconstrictor globally but owing to its short elimination half-life, it is usually administered six hourly by slow intravenous bolus injection.

Quality of benzathine penicillin G: A multinational cross-sectional study.

Benzathine penicillin G (BPG) is used as first-line treatment for most forms of syphilis and as secondary prophylaxis against rheumatic heart disease (RHD). Perceptions that poor quality of BPG is linked to reported adverse effects and therapeutic failure may impact syphilis and RHD control programs. Clinical networks and web-based advertising were used to obtain vials of BPG from a wide range of countries.

Design, synthesis, and biological evaluation of novel arylcarboxamide derivatives as anti-tubercular agents.

Our group has previously reported several indolecarboxamides exhibiting potent antitubercular activity. Herein, we rationally designed several arylcarboxamides based on our previously reported homology model and the recently published crystal structure of the mycobacterial membrane protein large 3 (MmpL3). Many analogues showed considerable anti-TB activity against drug-sensitive (DS) () strain.

Pharmacological Effects of Secondary Bile Acid Microparticles in Diabetic Murine Model.

Aim: Examine bile acids effects in Type 2 diabetes.

Background: In recent studies, the bile acid ursodeoxycholic acid (UDCA) has shown potent antiinflammatory effects in obese patients while in type 2 diabetics (T2D) levels of the pro-inflammatory bile acid lithocholic acid were increased, and levels of the anti-inflammatory bile acid chenodeoxycholic acid were decreased, in plasma.

Objective: Hence, this study aimed to examine applications of novel UDCA microparticles in diabetes.

Oral gavage of nano-encapsulated conjugated acrylic acid-bile acid formulation in type 1 diabetes altered pharmacological profile of bile acids, and improved glycaemia and suppressed inflammation.

Background: Ursodeoxycholic acid (UDCA) is a secondary hydrophilic bile acid, metabolised in the gut, by microbiota. UDCA is currently prescribed for primary biliary cirrhosis, and of recently has shown β-cell protective effects, which suggests potential antidiabetic effects. Thus, this study aimed to design targeted-delivery microcapsules for oral uptake of UDCA and test its effects in type 1 diabetes (T1D).

Modulatory Nano/Micro Effects of Diabetes Development on Pharmacology of Primary and Secondary Bile Acids Concentrations.

Background: Recent studies have suggested that hyperglycaemia influences the bile acid profile and concentrations of secondary bile acids in the gut.

Introduction: This study aimed to measure changes in the bile acid profile in the gut, tissues, and faeces in type 1 Diabetes (T1D) and Type 2 Diabetes (T2D).

Methods: T1D and T2D were established in a mouse model.

Bio-nanotechnological advancement of orally administered insulin nanoparticles: Comprehensive review of experimental design for physicochemical characterization.

Therapeutic proteins are labile macromolecules that are prone to degradation during production, freeze-drying and storage. Recent studies showed that nanoparticles can enhance the stability and oral bioavailability of encapsulated proteins. Several conventional approaches (enzyme inhibitors, mucoadhesive polymers) and novel strategies (surface modification, ligand conjugation, flash nano-complexation, stimuli-responsive drug delivery systems) have been employed to improve the physiochemical properties of nanoparticles such as size, zeta potential, morphology, polydispersity index, drug release kinetics and cell-targeting capacity.

Bile acid-polymer-probucol microparticles: protective effect on pancreatic β-cells and decrease in type 1 diabetes development in a murine model.

Studies in our laboratory have shown potential applications of the anti-atherosclerotic drug probucol (PB) in diabetes due to anti-inflammatory and β-cell protective effects. The anti-inflammatory effects were optimized by incorporation of the anti-inflammatory bile acid, ursodeoxycholic acid (UDCA). This study aimed to test PB absorption, tissue accumulation profiles, effects on inflammation and type 1 diabetes prevention when combined with UDCA.

An investigation of the stability of meropenem in elastomeric infusion devices.

Purpose: To evaluate the stability of meropenem trihydrate in elastomeric infusion devices at a range of selected concentrations (6, 12, 20 and 25 mg/mL) at ambient, refrigeration and freezing temperatures.

Methods: Meropenem Ranbaxy (meropenem trihydrate equivalent to anhydrous meropenem 1 g) vials for injection were reconstituted with 0.9% sodium chloride and adjusted to pH 6.

An in vivo pharmacological study: Variation in tissue-accumulation for the drug probucol as the result of targeted microtechnology and matrix-acrylic acid optimization and stabilization techniques.

Type 2 diabetes (T2D) is characterised by β-cell damage and hyperglycaemia. The lipophilic drug, probucol, has shown significant β-cell protective and potential antidiabetic effects, which were enhanced by hydrophilic bile acid incorporation using taurocholic acid and chenodeoxycholic acid. However, probucol has severe cardiotoxicity and a variable absorption profile, which limit its potential applications in T2D.

Inhibitors of Xanthine Oxidase: Scaffold Diversity and Structure-Based Drug Design.

Xanthine oxidase (XO) is the enzyme responsible for the catabolism of purines and their conversion into uric acid. XO is thus the target for the treatment of hyperuricemia and gout. For more than 50 years the only XO inhibitor drug available on the market was the purine analogue allopurinol.

Evaluation of the stability of linezolid in aqueous solution and commonly used intravenous fluids.

Purpose: The aim was to evaluate the stability of linezolid in commonly used intravenous fluids and in aqueous solution to determine the kinetics of degradation and shelf-life values at alkaline pH values.

Methods: Forced degradation studies were performed on linezolid in solution to develop a validated high-performance liquid chromatography analysis. Sodium chloride 0.