Physicochemical and biological evaluation of 'click' synthesized vinyl epoxide-chitosan film for active food packaging.

Chitosan (Cs) being a natural biopolymer serves as an excellent template to construct active packaging materials for achieving sustainable development. In this study, Cs was chemically modified via epoxide ring opening click reaction using vinyl epoxide to obtain a novel chitosan vinyl epoxide (Cs-VE) derivative with hydroxyl and olefinic functional groups. The Cs-VE transparent film was fabricated through the eco-friendly solution casting technique.

Epigallocatechin-3-gallate Synergistically Inhibits the Proliferation of Lung Cancer Cells with Gemcitabine by Induction of Apoptosis Mediated by ROS Generation.

The present study focused on the formulation, characterization, and evaluation of solid lipid nanoparticles (SLNs) loaded with gemcitabine (GEM) and epigallocatechin-3-gallate (EGCG) for lung cancer treatment. A 2-level, 3-factor factorial design was used to optimize various process parameters in the preparation of SLNs. The average particle size and polydispersity index (PDI) of GEM-EGCG SLNs were found to be 122.

Evaluation of Gemcitabine and Epigallocatechin-3-Gallate Loaded Solid Lipid Nanoparticles on Benzopyrene Induced Lung Cancer Model Via Intranasal Route: Improved Pharmacokinetics and Safety Profile.

The objective of this study was to create a new treatment for lung cancer using solid lipid nanoparticles (SLNs) loaded with gemcitabine (GEM) and epigallocatechin-3-gallate (EGCG) that can be administered through the nose. We analyzed the formulation for its effectiveness in terms of micromeritics, drug release, and anti-cancer activity in the benzopyrene-induced Swiss albino mice lung cancer model. We also assessed the pharmacokinetics, biodistribution, biocompatibility, and hemocompatibility of GEM-EGCG SLNs.

Adapting Clinical Practice Guidelines for Chronic Kidney Disease: Blood Pressure Management and Kidney Replacement Therapy in Adults and Children in the Saudi Arabian Context Using the Grading of Recommendations Assessment, Development, and Evaluation-ADOLOPMENT Methodology.

This practice guideline was developed by the chronic kidney disease (CKD) Task Force, which was composed of clinical and methodological experts. The Saudi Arabian Ministry of Health and its health holding company commissioned this guideline project to support the realization of Vision 2030's health-care transformation pillar. The synthesis of these guidelines was guided by the Grading of Recommendations Assessment, Development, and Evaluation (GRADE)- ADOLOPMENT methodology.

Arylazo sulfones: multifaceted photochemical reagents and beyond.

The photochemical action of arylazo sulfones under visible light irradiation has recently gained considerable attention for the construction of carbon-carbon and carbon-heteroatom bonds in organic synthesis. The inherent dyedauxiliary group (-NSOR) embedded in the reagent is responsible for the absorption of visible light even in the absence of a photocatalyst, additive or oxidant, leading to the generation of three different radicals, . aryl (carbon-centred), sulfonyl (sulphur-centred) and diazenyl (nitrogen-centred) radicals, under different reaction conditions.

In Vivo Cancer Microenvironment Responsive Glycan Receptor-Targeted Nanoparticles for Gemcitabine Delivery to Benzo[a]pyrene-Induced Lung Cancer Model.

Targeted gemcitabine (GEB) loaded 5-N-acetyl-neuraminic acid (Neu5Ac) assembled chitosan nanoparticles (CA-NPs) were formulated by ionotropic gelation process and evaluated for physicochemical and morphological characterization, in vitro and in vivo studies in A-549 cells and lung cancer mice model, respectively. The mean diameter of GEB-CA-Neu5Ac-NPs determined by dynamic light scattering was 161.16 ± 7.

pH-influenced self-assembled stealth nanoscaffolds encapsulating memantine for treatment of Alzheimer's disease.

Alzheimer's disease (AD) is the most common neurological disorder characterized by the accumulation of β-amyloid peptides. The only medication used to treat moderate-to-severe AD progression is memantine. In this study, polyethylene glycol (PEG)-coated poly D, L-lactic-co-glycolic acid (PLGA) nanostructures were prepared, as their self-assembling ability helps to penetrate the drug at disease sites with altered pH range (5.

Dual targeting pH responsive chitosan nanoparticles for enhanced active cellular internalization of gemcitabine in non-small cell lung cancer.

Lung cancer (LC), related with the enhanced expression of epidermal growth factor receptor (EGFR) and sialic acid binding receptors (glycan) brought about the development of EGFR and glycan receptor specific anticancer therapeutics. The current study assessed the formulation, physiochemical characterization, in vitro and in vivo effects of sialic acid (SA) and cetuximab (Cxmab) decorated chitosan nanoparticles (CSN-NPs) loaded with gemcitabine (GMC) targeted to glycan and EGFR over-expressing non-small-cell lung-cancer (NSCLC) A-549 cells. Chitosan (CSN) was conjugated with sialic acid via EDC/NHS chemistry followed by gemcitabine loaded sialic acid conjugated chitosan nanoparticles (GMC-CSN-SA-NPs) were prepared by ionic gelation method decorated with Cxmab by electrostatic interaction.

'Click' synthesized calcium-chitosan-triazole nanocomplex from CaC as an efficient drug carrier, antimicrobial and antioxidant polymer.

A calcium-chitosan-triazole nanocomplex (Ca@CS-Tz) was synthesized via the robust copper catalyzed azide-alkyne cycloaddition using calcium carbide (CaC2) as an in-situ source of acetylene. The nanocomplex was characterized by various techniques and it was proved to be an efficient drug carrier with satisfactory antimicrobial and antioxidant properties. Quercetin loaded nanocomplex (encapsulation efficiency- 68.

Role of pro-inflammatory cytokines in Alzheimer's disease and neuroprotective effects of pegylated self-assembled nanoscaffolds.

Neurodegeneration and synaptic loss in Alzheimer's disease (AD) lead to impairment in memory functions. Neuroinflammation causes activation of microglia and astrocytes cells that locally and systemically produces inflammatory cytokines which can serve as early diagnostic markers or therapeutic targets in AD. Pro-inflammatory cytokines (Interleukins (IL-1β, IL-6 and IL-10) and tumor necrosis factor (TNF α)) levels were estimated in serum, cerebral tissue, hepatic tissue, and renal tissue in treatment groups of scopolamine-induced amnesia mice model using ELISA protocol.

Changing paradigms in the treatment of tuberculosis.

Tuberculosis, caused by Mycobacterium tuberculosis, is a disease long dealt with, but still remains the second leading cause of death world-wide. The current anti-tubercular chemotherapy primarily targets the microbial pathogenesis, which however, is failing due to the development of drug resistance. Moreover, with fewer new drugs reaching the market, there is a need to focus on alternate treatment approaches that could be used as stand-alone or adjunct therapy and the existing drugs, referred to as Track II chemotherapy.

Design, fabrication, optimization and characterization of memantine-loaded biodegradable PLGA nanoscaffolds for treatment of Alzheimer's disease.

This study aimed to design and develop nanoscaffolds for the controlled release of memantine by non-solvent-induced phase separation (N-TIPS) method. The development and optimization of nanoscaffolds was performed by Box-Behnken Design in which two independent formulation variables and one independent process variable: poly(lactic-co-glycolic acid) (PLGA) (), Pluronics F-127 (), and rotation speed () were used. The design provided 15 formulation designs which were prepared to determine the response: percentage porosity () and drug loading ().

New paradigm in combination therapy of siRNA with chemotherapeutic drugs for effective cancer therapy.

Chemotherapeutics drugs play a pivotal role in the treatment of cancer. However, many issues generate by chemotherapy drugs, including unfavorable harm to healthy cells and multidrug resistance (MDR), persist and have a negative impact on therapeutic outcomes. When compared to monotherapy, combination cancer therapy has many advantages, like improving efficacy through synergistic effects and overcoming drug resistance.

A photocatalyst-free visible-light-mediated solvent-switchable route to stilbenes/vinyl sulfones from β-nitrostyrenes and arylazo sulfones.

Photocatalyst-free visible-light-mediated reactions, based on the presence of a visible-light-absorbing functional group in the starting material itself in order to exclude the often costly, hazardous, degradable and difficult to remove or recover photoredox catalysts, have been gaining momentum recently. We have employed this approach to develop a denitrative photocatalyst-free visible-light-mediated protocol for the arylation/sulfonylation of β-nitrostyrenes employing arylazo sulfones (bench-stable photolabile compounds) in a switchable solvent-controlled manner. Arylazo sulfones served as the aryl and sulfonyl radical precursors under blue LED irradiation for the synthesis of trans-stilbenes and (E)-vinyl sulfones in CH3CN and dioxane/H2O 2 : 1, respectively.

Organic photoredox catalysis enabled cross-coupling of arenediazonium and sulfinate salts: synthesis of (un)symmetrical diaryl/alkyl aryl sulfones.

We disclose herein the first transition-metal- and external oxidant/reductant-free visible-light-mediated synthesis of (un)symmetrical diaryl/alkyl aryl sulfones from arenediazonium tetrafluoroborates and sodium sulfinates using eosin Y as an organic photoredox catalyst. The utilization of visible light as an inexpensive and ecosustainable energy source, operational simplicity, ambient temperature and clean reaction in aqueous acetonitrile are the salient features of the developed protocol. The desired sulfones were also synthesized via a one-pot, two-step process directly from anilines and sulfinate salts in good to excellent yields.

Polylactide-co-glycolide nanoparticles of antitubercular drugs: formulation, characterization and biodistribution studies.

Background: The present study was designed to prepare and characterize poly lactide-co-glycolide nanoparticles of antitubercular drugs (ATDs) for delivery through oral route to alveolar macrophages.

Methods: Nanoparticles were prepared by double emulsification solvent evaporation method. Ex vivo and in vivo drug accumulation studies were performed in alveolar macrophages, harvested by broncheoalveolar lavaging.

Aerobic oxysulfonylation of alkenes using thiophenols: an efficient one-pot route to β-ketosulfones.

We have developed a highly efficient synthetic route to β-ketosulfones via AgNO3 catalyzed oxysulfonylation of alkenes using thiophenols in the presence of air (O2) and K2S2O8 as eco-friendly oxidants. Thiophenols have been used as sulfonylation precursors for the first time in a dioxygen activation based radical process. Moreover, the protocol also offers a new and convenient method for the synthesis of β-hydroxysulfides at room temperature without the use of any initiator.

Intranasal curcumin and its evaluation in murine model of asthma.

Curcumin, a phytochemical present in turmeric, rhizome of Curcuma longa, has been shown to have a wide variety of pharmacological activities including anti-inflammatory, anti-allergic and anti-asthmatic properties. Curcumin is known for its low systemic bioavailability and rapid metabolization through oral route and has limited its applications. Over the recent decades, the interest in intranasal delivery as a non-invasive route for drugs has increased as target tissue for drug delivery since nasal mucosa offers numerous benefits.

Development and optimization of polymeric nanoparticles of antitubercular drugs using central composite factorial design.

Objective: The objective of the present study was to develop sustained release biodegradable polymeric nanoparticles (PNs) of two anti-tubercular drugs (ATDs), rifampicin (RIF) and isoniazid (INH) using circumscribed central composite factorial design (CCD) and evaluate in vivo uptake potential using rhodamine labeled PNs (RPNs).

Methods: CCD was employed to study the influence of independent formulation factors, drug:polymer ratio (D:P) and surfactant concentration (SC), on dependent physicochemical characteristics, particle size (PS), polydispersity index (PI) and percentage entrapment efficiency (%EE) of the drugs. Optimized PNs prepared using response surface methodology (RSM) were evaluated for in vitro kinetics at endosomal macrophage pH 5.

NHC-catalysed diastereoselective synthesis of multifunctionalised piperidines via cascade reaction of enals with azalactones.

NHC-catalysed azalactone ring-opening and piperidine ring-closing cascade with α,β-unsaturated aldehydes (enals) in a one-pot operation is reported. The present reaction cascade offers a convenient method for a highly diastereoselective synthesis of multifunctionalised piperidines in excellent yields under mild conditions.