Efficacy and pharmacological assessment of novel -hydroxypyridinediones as hepatitis B virus ribonuclease H inhibitors.

We previously reported -hydroxypyridinedione (HPD) compounds with mid-nanomolar efficacy and selectivity indexes around 300 against hepatitis B virus (HBV) replication. However, they lack pharmacological evaluation. Here, we report anti-HBV efficacy, cytotoxicity, and pharmacological characterization of 29 novel HPDs within seven subgroups.

Nanoparticles use magnetoelectricity to target and eradicate cancer cells.

Unlabelled: This study presents the first in vivo and in vitro evidence of an externally controlled, predictive, MRI-based nanotheranostic agent capable of cancer cell specific targeting and killing via irreversible electroporation (IRE) in solid tumors. The rectangular-prism-shaped magnetoelectric nanoparticle is a smart nanoparticle that produces a local electric field in response to an externally applied magnetic field. When externally activated, MENPs are preferentially attracted to the highly conductive cancer cell membranes, which occurs in cancer cells because of dysregulated ion flux across their membranes.

Eucalyptus oil nanoemulsion for enhanced skin deposition of fluticasone propionate in psoriatic plaques: A combinatorial anti-inflammatory effect to suppress implicated cytokines.

Psoriasis is a chronic inflammatory skin disease that affects patients' quality of life. This study aimed to enhance the efficacy of topical application of fluticasone propionate (FP) using a eucalyptus oil-based nanoemulsion, an oil possessing anti-inflammatory activity and extracted from the leaves, fruits, and buds of Eucalyptus globulus or Eucalyptus maidenii, to improve the skin deposition of FP and aid its anti-inflammatory effect. Box-Behnken design was employed to optimize NE formulations, which were characterized for globule size, zeta potential, polydispersity index, rheological behavior, microscopic morphology, ex vivo skin permeation/deposition, and in vivo efficacy using imiquimod-induced psoriatic lesions.

Allostreptopyrroles A-E, β-alkylpyrrole derivatives from an actinomycete sp. RD068384.

Five new β-alkylpyrrole derivatives, allostreptopyrroles A-E (-), were isolated from the culture broth of RD068384. Their structures were elucidated by 1D and 2D NMR spectroscopic analyses, HRESIMS, and chemical derivatization. The absolute configurations of compounds and were predicted by comparison of experimental and calculated specific rotation data.

Recurrent attention U-Net for segmentation and quantification of breast arterial calcifications on synthesized 2D mammograms.

Breast arterial calcifications (BAC) are a type of calcification commonly observed on mammograms and are generally considered benign and not associated with breast cancer. However, there is accumulating observational evidence of an association between BAC and cardiovascular disease, the leading cause of death in women. We present a deep learning method that could assist radiologists in detecting and quantifying BAC in synthesized 2D mammograms.

Novel radioiodinated desvenlafaxine-loaded lipid nanocapsule for brain delivery.

Lipid nanocapsules (LNCs) are lipid nanocarriers developed for drug delivery enhancement. The antidepressant drug desvenlafaxine (DSV) was entrapped in LNC to improve its brain delivery. Different DSV-loaded LNCs formulae using different oils and surfactants were studied to obtain the optimum formula for further studies.

Radiation synthesis and chemical modifications of p(AAm-co-AAc) hydrogel for improving their adsorptive removal of metal ions from polluted water.

The research focuses on utilizing gamma irradiation to synthesize polyacrylic acid-co-polyacrylamide p(AAm-co-AAc) hydrogels. The effect of synthetic parameters on physicochemical features of p(AAm-co-AAc) hydrogls were examined, including acrylic acid (AAc): acrylamide (AAm) weight ratios, monomer concentration, and gamma irradiation dosage (kGy). At the optimum synthetic conditions (30 kGy and 75% AAc), different chemical modifications are explored to incorporate sulfonate, hydroxyl, carboxyl, cysteine, thiol, and amine functional groups within the bare hydrogel (Cpd 0) structure.

In vitro evaluation of tropolone absorption, metabolism, and clearance.

Tropolone compounds can inhibit hepatitis B virus (HBV) replication at sub-micromolar levels and are synergistic upon co-treatment with nucleos(t)ide analog drugs. However, only a few compounds within this chemotype have been screened for their pharmacological properties. Here, we chose 36 structurally diverse tropolones from six subclasses to characterize their in vitro pharmacological parameters.

Structure-emission relationship of some coumarin laser dyes and related molecules: Prediction of radiative energy dissipation and the intersystem crossing rate constants.

Dye lasers are commonly used in optical investigation because their solutions in organic solvents deliver tunable, coherent emissions. They exhibit intense fluorescence owing to some specific spectroscopic characteristics. One drawback of the laser dyes is that it shows excessive triplet-state losses (TSLs.

Polymeric Nanoparticles' Accumulation in Atopic Dermatitis: Clinical Comparison between Healthy, Non-Lesional, and Lesional Skin.

A major limitation in the current topical treatment strategies for inflammatory skin disorders is the inability to selectively target the inflamed site with minimal exposure of healthy skin. Atopic dermatitis is one of the most prevalent types of dermatitis. The use of polymeric nanoparticles for targeting inflamed skin has been recently proposed, and therefore the aim of this proof-of-concept clinical study was to investigate the skin penetration and deposition of polymeric biodegradable nanoparticles in the atopic dermatitis lesions and compare the data obtained to the deposition of the particles into the healthy skin or lesion-free skin of the atopic dermatitis patients.

Multimodal Spatiotemporal Deep Learning Framework to Predict Response of Breast Cancer to Neoadjuvant Systemic Therapy.

Current approaches to breast cancer therapy include neoadjuvant systemic therapy (NST). The efficacy of NST is measured by pathologic complete response (pCR). A patient who attains pCR has significantly enhanced disease-free survival progress.

The interplay of solvent-drug-protein interactions during albumin nanoparticles formulations for temozolomide delivery to brain cancer cells.

Objectives: Temozolomide (TMZ), the first line for glioma therapy, suffers from stability at physiological pH. TMZ was selected as a challenging model drug for loading into human serum albumin nanoparticles (HSA NPs). Our aim is to optimise the conditions for TMZ loading into HSA NPs while ensuring TMZ stability.

Combined application of biosponges and an antifibrotic agent for the treatment of volumetric muscle loss.

Volumetric muscle loss (VML) causes irrecoverable loss of muscle mass and strength and results in permanent disability. VML injury shows extensive fibrosis, which impedes functional tissue regeneration. Our lab has created a biosponge scaffold composed of extracellular matrix (ECM) proteins (i.

Can Essential Oils/Botanical Agents Smart-Nanoformulations Be the Winning Cards against Psoriasis?

Although psoriasis remains one of the most devastating inflammatory disorders due to its huge negative impact on patients' quality of life, new "green" treatment approaches still need to be fully explored. The purpose of this review article is to focus on the utilization of different essential oils and active constituents of herbal botanical origin for the treatment of psoriasis that proved efficacious via both in vitro and in vivo models. The applications of nanotechnology-based formulations which displayed great potential in augmenting the permeation and delivery of these agents is also addressed.

Boosting the In Vivo Transdermal Bioavailability of Asenapine Maleate Using Novel Lavender Oil-Based Lipid Nanocapsules for Management of Schizophrenia.

Lipid nanocapsules (LNCs) are promising for transdermal drug delivery due to their higher permeability-enhancing effects compared to polymeric nanoparticles. Lavender oil is an essential oil consisting of several terpenes (primarily linalool and linalyl acetate) known for their profound permeation-enhancing action. In the present work, we successfully encapsulated asenapine maleate (a second-generation antipsychotic that is highly metabolized by the liver, reducing its oral bioavailability) into biocompatible LNCs for transdermal application using a novel oily phase, i.

Lipoproteins as Drug Carriers for Cyclosporine A: Optimization of the Entrapment.

Lipoproteins are natural nanostructures responsible for the transport of cholesterol and other lipids in the blood. They are characterized by having a lipophilic core surrounded by an amphiphilic shell composed of phospholipids, cholesterol and one or more apolipoproteins. Being endogenous carriers makes them suitable for drug delivery purposes.

Skin targeting by chitosan/hyaluronate hybrid nanoparticles for the management of irritant contact dermatitis: In vivo therapeutic efficiency in mouse-ear dermatitis model.

Irritant contact dermatitis (ICD) is an inflammatory skin condition characterized by severe eczematous lesions. Nanoparticulate drug delivery is the most predominant way to improve dermal penetration and have gained remarkable recognition for targeted delivery of therapeutic payload and reduced off-target effects. Therefore, the current work aimed to fabricate polyelectrolyte complex nanoparticles (PENPs) containing two natural biodegradable polymers namely; chitosan (CS) and hyaluronic acid (HA) to deliver the non steroidal anti-inflammatory drug etoricoxib (ETX) to the deeper skin layers to alleviate any systemic toxicity and improve its therapeutic efficacy against ICD.

Viable production of hydrogen and methane from polluted water using eco-friendly plasmonic Pd-TiO nanocomposites.

Solar-to-fuel conversion is a novel clean energy approach that has gained the interest of many researchers. Solar-driven photocatalysts have become essential to providing valuable fuel gases such as methane and hydrogen. Solar energy has emerged as a renewable, abundant energy source that can efficiently drive photochemical reactions through plasmonic photocatalysis.

Effect of lifestyle-based lipid lowering interventions on the relationship between circulating levels of per-and polyfluoroalkyl substances and serum cholesterol.

Exposure to certain per-and polyfluoroalkyl substances (PFAS) has been shown to be positively associated with total and/or low-density lipoprotein cholesterol. Examining this association in lipid lowering interventions may provide additional evidence linking PFAS to cardiovascular risk. We examined the relationship of 6 PFAS with cholesterol in a 6-month lifestyle-based intervention.

Rapid removal of PFOA and PFOS via modified industrial solid waste: Mechanisms and influences of water matrices.

Emerging perfluoroalkyl and polyfluoroalkyl substances contaminate waters at trace concentrations, thus rapid and selective adsorbents are pivotal to mitigate the consequent energy-intensive and time-consuming issues in remediation. In this study, coal combustion residuals-fly ash was modified (FA-SCA) to overcome the universal trade-off between high adsorption capacity and fast kinetics. FA-SCA presented rapid adsorption (t = 2 min) of PFOX (perfluorooctanoic acid and perfluorooctanesulfonic acid, collectively), where the dynamic adsorption capacity (q = q/t) was 2-3 orders of magnitude higher than that of benchmark activated carbons and anion-exchange resins.

Magnetic-field-synchronized wireless modulation of neural activity by magnetoelectric nanoparticles.

The in vitro study demonstrates wirelessly controlled modulation of neural activity using magnetoelectric nanoparticles (MENPs), synchronized to magnetic field application with a sub-25-msec temporal response. Herein, MENPs are sub-30-nm CoFeO@BaTiO core-shell nanostructures. MENPs were added to E18 rat hippocampal cell cultures (0.

Stimulated generation of photobiogas by morphologically tuned nanostructured ZnO and ZnO/TiO.

The photocatalytic degradation (PCD) of ethanol in an inert atmosphere on catalysis was explored in a lab-scale experiment. A morphologically tuned nanostructured controlled ZnO and ZnO/TiO nanocomposites were synthesized using a simple hydrothermal process under the control of several functionally capping agents marking a milestone in photocatalysis. It is possible that this could be modified to produce photobiogas out of organic dye pollution.

Nanomedicine and nanobiotechnology applications of magnetoelectric nanoparticles.

Unlike any other nanoparticles known to date, magnetoelectric nanoparticles (MENPs) can generate relatively strong electric fields locally via the application of magnetic fields and, vice versa, have their magnetization change in response to an electric field from the microenvironment. Hence, MENPs can serve as a wireless two-way interface between man-made devices and physiological systems at the molecular level. With the recent development of room-temperature biocompatible MENPs, a number of novel potential medical applications have emerged.