Effects of chronic marijuana use on driving performance.

Objectives: The effects of marijuana on driving pose a significant public health concern. More studies on chronic marijuana use in driving are needed. The study objectives were to (1) assess differences in the Standardized Field Sobriety Test (SFST) and driving performance outcomes between chronic medical marijuana users and nonusers and (2) identify a cutoff tetrahydrocannabinol (THC) concentration above which chronic medical marijuana users demonstrate driving impairment.

Safety and performance of current abuse-deterrent formulations.

Prescription opioid abuse is now an epidemic that has forced the government and industries to take initiatives. These include developing abuse-deterrent formulations (ADFs), issuing regulatory guidances and allocating massive budgets to ensure the safety and effectiveness of these medications. Areas covered: This review covers the regulatory guidance on evaluation and labeling of the branded and generic ADFs.

Angiotensin II type 1 receptor blockers prevent aortic arterial stiffness in elderly patients with hypertension.

: Increased arterial stiffness may increase cardiovascular morbidity and mortality. Angiotensin II type 1 receptor blockers (ARBs) are potentially useful in controlling the central blood pressure and arterial stiffness in mild to moderate essential hypertension, while the effects of ARBs in aged patients with essential hypertension are not entirely investigated. : The carotid-femoral arterial pulse wave velocity (PWV) was measured in aged patients with essential hypertension.

Penicindopene A, a new indole diterpene from the deep-sea fungus sp. YPCMAC1.

A new indole diterpene, named penicindopene A (), together with seven known compounds (-), was isolated from the deep-sea fungus sp. YPCMAC1. The structure of penicindopene A was elucidated by extensive spectroscopic analyses (1 D and 2 D NMR, and HRESIMS data), in addition to the ECD calculations for the assignments of its absolute configuration.

An indole diterpenoid isolated from the fungus sp. and its antimicrobial activity.

One new indole diterpenoid, drechmerin I (), was isolated from the fermentation broth of sp. isolated from the root of . Its structure was elucidated based on 1 D and 2 D nuclear magnetic resonance (NMR), high resolution electrospray ionization mass spectrum (HRESIMS), and electronic circular dichroism (ECD) spectroscopic analyses as well as TD DFT calculations of ECD spectra.

Pharmacokinetic modeling and simulation of etodolac following single oral administration in dogs.

Etodolac is a nonsteroidal anti-inflammatory drug with selective cyclooxygenase-2 inhibition to treat pain and inflammation associated with osteoarthritis in humans and dogs. The aim of the study was to investigate the pharmacokinetics of etodolac following single oral administration of 200 mg to 10 healthy beagle dogs. The plasma concentrations of etodolac were detected using liquid chromatography-tandem mass spectrometry.

Physical properties and solubility studies of Nifedipine-PEG 1450/HPMCAS-HF solid dispersions.

Low-order high-energy nifedipine (NIF) solid dispersions (SDs) were generated by melt solvent amorphization with polyethylene glycol (PEG) 1450 and hypromellose acetate succinate (HPMCAS-HF) to increase NIF solubility while achieving acceptable physical stability. HPMCAS-HF was used as a crystallization inhibitor. Individual formulation components, their physical mixtures (PMs), and SDs were characterized by differential scanning calorimetry, powder X-ray diffraction, and Fourier transform infrared spectroscopy (FTIR).

Development and in vitro characterization of chitosan-coated polymeric nanoparticles for oral delivery and sustained release of the immunosuppressant drug mycophenolate mofetil.

Objective: To develop an oral sustained release formulation of mycophenolate mofetil (MMF) for once-daily dosing, using chitosan-coated polylactic acid (PLA) or poly(lactic-co-glycolic) acid (PLGA) nanoparticles. The role of polymer molecular weight (MW) and drug to polymer ratio in encapsulation efficiency (EE) and release from the nanoparticles was explored in vitro.

Methods: Nanoparticles were prepared by a single emulsion solvent evaporation method where MMF was encapsulated with PLGA or PLA at various polymer MW and drug: polymer ratios.

Genetic engineering and characterisation of chlorotoxin-fused gelonin for enhanced glioblastoma therapy.

Despite substantial advances in its treatment, brain cancer remains a life-threatening disease with a poor survival rate. The main challenges for the conventional chemotherapy include an insufficient efficacy of drugs and toxicity caused by their nonselective mode of action. Recently, great attention has been paid to highly potent macromolecules such as gelonin, a type 1 ribosome-inactivating protein that inhibits protein translation.

Polyelectrolyte Complex Nanoparticles Based on Methoxy Poly(Ethylene Glycol)-B-Poly (ε-Caprolactone) Carboxylates and Chitosan for Delivery of Tolbutamide.

In this study, a novel chitosan (CS)-modified nanoparticles (NPs) were developed to orally deliver tolbutamide (TOL). Methoxy poly(ethylene glycol)- b-poly(ε-caprolactone) carboxylates (mPEG-b-PCL) was synthesized via an esterification reaction. CS-modified mPEG-b-PCL-COOH NPs (CS@NPs) were fabricated by injecting mPEG-b-PCL-COOH NPs suspension (1.

Novel revaprazan-loaded gelatin microsphere with enhanced drug solubility and oral bioavailability.

To develop a novel revaprazan-loaded gelatine microsphere with enhanced solubility and oral bioavailability, numerous gelatine microspheres were prepared using a spray-drying technique. The impact of gelatine amount on drug solubility in the gelatine microspheres was investigated. The physicochemical properties of the selected gelatine microsphere, such as shape, particle size and crystallinity, were evaluated.

Isolation of tyrosinase and melanogenesis inhibitory flavonoids from Juniperus chinensis fruits.

A new biflavonoid, amentoflavone-7-O-β-D-glucoside, and thirteen known flavonoids were isolated from the fruits of Juniperus chinensis using a bioactivity-guided method and their tyrosinase inhibitory effects were tested using a mushroom tyrosinase bioassay. Two isolates, hypolaetin-7-O-β-D-glucoside and quercetin-7-O-α-L-rhamnoside, were found to reduce tyrosinase activity at a concentration of 50 μM. Quercetin-7-O-α-L-rhamnoside attenuated cellular tyrosinase activity and melanogenesis in α-MSH plus IBMX-stimulated B16F10 melanoma cells.

The effects of phenolic glycosides from Betula platyphylla var. japonica on adipocyte differentiation and mature adipocyte metabolism.

Betula platyphylla var. japonica (Betulaceae) has been used traditionally in Asian countries for the treatment of inflammatory diseases. A recent study has reported a phenolic compound, platyphylloside from B.

Scavenger receptor class BI (SR-BI) mediates uptake of CPX-351 into K562 leukemia cells.

Purpose: CPX-351 is a liposomal formulation of cytarabine and daunorubicin encapsulated at a 5:1 molar ratio, for the treatment of acute myeloid leukemia. The Scavenger Receptor class B type I (SR-BI) plays an important role in mediating the uptake of high-density lipoproteins. The purpose of this study is to assess the role of the cell surface lipoprotein receptor SR-BI in the uptake of CPX-351 liposomes (Jazz Pharmaceuticals) into K562 leukemia cells.

Pharmacokinetic evaluation of meropenem and vaborbactam for the treatment of urinary tract infection.

Meropenem/vaborbactam (M/V) represents the first carbapenem and β-lactamase inhibitor combination approved for treatment of complicated urinary tract infections (cUTIs), including pyelonephritis. Vaborbactam is a novel boronic acid, β-lactamase inhibitor with a high affinity for serine β-lactamases, including Klebsiella pneumoniae carbapenemase (KPC). This combination, Vabomere™, was approved in August 2017 by the United States Food and Drug Administration for the treatment of cUTIs in patients 18 years or older, including pyelonephritis, caused by the following susceptible microorganisms: Escherichia coli, K.

Phytochemical Analysis and Antidepressant Activity of Extracts in Experimental Models of Depression in Mice.

Objectives: The present study aims to assess the antidepressant activity of extracts in mice and phytochemical analysis of the active extract by GC-MS.

Materials And Methods: After oral administration of extracts, tail suspension test (TST), force swim tests (FST), and open field tests (OFT) were performed to assess the antidepressant activity. GC-MS analysis of methanol extract of was performed to ascertain the chemical constituents in the bioactive extract.

Upcycling of jellyfish (Nemopilema nomurai) sea wastes as highly valuable reducing agents for green synthesis of gold nanoparticles and their antitumor and anti-inflammatory activity.

Due to its tentacle poison and huge body, giant jellyfish (Nemopilema nomurai) poses challenging issues to the environment and ecosystems. Here we developed, upcycling a giant jellyfish extract as a reducing agent, a green synthetic method of gold nanoparticles (JF-AuNPs) which possess biological activities. The colloidal solutions of JF-AuNPs were blue, violet, purple and pink depending on the extract concentration.

Economic impact of tolvaptan treatment vs. fluid restriction based on real-world data among hospitalized patients with heart failure and hyponatremia.

Objectives: To estimate the cost difference associated with tolvaptan treatment vs. fluid restriction (FR) among hospitalized patients with heart failure (HF) and hyponatremia (HN) based on a real-world registry of HN patients.

Methods: An Excel-based economic model was developed to evaluate the cost impact of tolvaptan treatment vs.

Controlled formation of polylysinized inner pores in injectable microspheres of low molecular weight poly(lactide-co-glycolide) designed for efficient loading of therapeutic cells.

This study aimed to develop porous microspheres with a suitable porous structure and mechanical property for cell delivery using a comparatively low molecular weight (MW) poly(lactide-co-glycolide) (PLGA) having a weak mechanical strength and fast degradation rate, which could be potentially used for treatment of corneal endothelial diseases. Porous microspheres of 30 kDa PLGA with different pore sizes were prepared by varying preparation conditions, and the microspheres with mean pore diameters approximately 0.5, 1, 2 and 3 times that of a single green fluorescent protein-expressing human embryonic kidney 293 cell, used as a model cell, were chosen for cell loading study.

Investigation on the effect of nanoparticle size on the blood-brain tumour barrier permeability by in situ perfusion via internal carotid artery in mice.

The blood-brain barrier (BBB) is a limiting factor in nanoparticle drug delivery to the brain, and various attempts have been made to overcome it for efficient drug delivery. Nowadays, it was considered as further issue for brain-drug delivery that the nanoparticle delivered to brain through the BBB reach cancer cells in tumour tissue. In this study, we investigated the effect of nanoparticle size on blood-brain tumour barrier (BBTB) permeation of fluorescence-labelled gold nanoparticles (AuNPs) in a mouse model of orthotopic glioblastoma multiforme (GBM), established by intracranial implantation of luciferase-expressing human glioblastoma U87MG cells.

Effects of the FcRn developmental pharmacology on the pharmacokinetics of therapeutic monoclonal IgG antibody in pediatric subjects using minimal physiologically-based pharmacokinetic modelling.

The aim of this study was to investigate neonatal Fc receptor (FcRn) concentration developmental pharmacology in adult and pediatric subjects using minimal physiologically-based pharmacokinetic (mPBPK) modelling. Three types of pharmacokinetic (PK) data for three agents (endogenous/exogenous native IgG, bevacizumab and palivizumab) were used. The adult group contained six subjects with weights from 50 to 100 kg.

Platycosides P and Q, two new triterpene saponins from Platycodon grandiflorum.

The EtOH extract of the roots of Platycodon grandiflorum afforded two new triterpene saponins platycoside P (1) and platycoside Q (2). Their structures were elucidated based on spectroscopic means and hydrolysis products. These compounds were evaluated for inhibitory activity against LPS-induced TNF-α production in RAW 246.

Dose proportionality and pharmacokinetics of dronedarone following intravenous and oral administration to rat.

The aim of this study was to investigate the pharmacokinetic properties of dronedarone by using noncompartmental analysis and modeling approaches after intravenous and oral administration of dronedarone to rats. Twenty-eight male Sprague-Dawley rats were randomly divided into four groups, and dronedarone was administered intravenously (1 mg/kg) and orally (5, 10 and 40 mg/kg) based on a parallel design. Blood samples were collected before and 0.

Highly stable gold nanoparticles green-synthesized by upcycling cartilage waste extract from yellow-nose skate (Dipturus chilensis) and evaluation of its cytotoxicity, haemocompatibility and antioxidant activity.

Skate (Dipturus chilensis) cartilage extract was utilized as a green reducing agent for the synthesis of spherical gold nanoparticles with an average size of 16.7 ± 0.2 nm.

N-acetylaminogalactosyl-decorated biodegradable PLGA-TPGS copolymer nanoparticles containing emodin for the active targeting therapy of liver cancer.

Primary liver cancer (PLC) is one of the most common malignant tumours and has the third highest mortality rate worldwide. An active liver-targeting drug delivery system via the asialoglycoprotein receptors expressed in the hepatic parenchyma cells of mammals has become a research focus for the treatment of PLC. N-acetylaminogalactosyl-poly(lactide-co-glycolide)-succinyl-D-α-tocopherol polyethylene glycol 1000 succinate (GalNAc-PLGA-sTPGS) was synthesized to achieve active liver-targeting properties.