Purpose Supersaturated formulations have been widely explored for improving the oral bioavailability of drugs by using mesoporous silica (MS) to generate supersaturation via molecular adsorption; however, this is followed precipitation. Several precipitation inhibitors (PI) prevent and maintain drug in solution a longer period. However, combined approach MS PIs, impact Silica, loading high-molecular-weight neutral molecules such as Cyclosporine A (CsA) not yet explored. The present study...

As compared to standard medicinal compounds, hybrid molecules that contain multiple biologically active functional groups have greater affinity and efficiency. Hence based on this concept, we predicted a combination of thiazolidinediones 1,3,4-oxadiazoles may enhance α-amylase α-glucosidase inhibition activity. A series novel 3-((5-phenyl-1,3,4-oxadiazol-2-yl)methyl)thiazolidine-2,5-dione derivatives (5a-5j) were synthesized characterized using different spectroscopic techniques

<ns3:p>Background As lung cancer treatment has progressed, there been an increase in awareness of the short- and long-term adverse effects targeted therapies tyrosine kinase inhibitors, particularly cardiovascular toxicities. Methods The current study assessed potential drug interactions using interaction drug-interaction checkers (IBM Micromedex Drugs.com). Molecular docking was employed to further investigate involvement human ether-à-go-go-related gene (hERG) pregnane X receptor (PXR)...

Alzheimer's disease (AD) is a neurodegenerative disorder that has higher prevalence and incidence in people older than 60 years. The need for improved AD therapies unmet as the current are symptomatic with modest efficacy. Partial agonists of 5-HT4 receptor (5-HT4R) offer both disease-modifying treatments they shift amyloid-precursor-protein (APP) processing from amyloidogenic pathway to nonamyloidogenic by activating α-secretase enzyme. In addition, also treatment increasing levels...

Fungal keratitis is one of the leading causes ophthalmic mycosis affecting vision due to corneal scarring. Voriconazole (VRC) most preferred azole antifungal agent for treating ocular mycotic infections. Ocular drug delivery challenging shorter residence time formulation requiring frequent administration, poor patient compliance. The present study aimed at improving solubility, transcorneal permeation, and efficacy voriconazole via formation cyclodextrin-based ternary complexes incorporation...

Dietary polyphenols such as quercetin and curcumin have been extensively administered to patients with cancer in the form of herbal supplements. They may a synergistic anticancer effect; however, risk pharmacokinetic interactions selective CDK-4/6 inhibitors that are metabolized by CYP3A4 enzyme exists. Considering these aspects, current study examined effects on human ascertain CYP3A4-mediated herb-drug CDK inhibitors. In this study, using silico methods inhibition kinetics liver microsomes...

A key diterpene lactone of Andrographis paniculata, i.e., andrographolide (AG), exhibits a variety physiological properties, including hepatoprotection. The limited solubility, short half-life, and poor bioavailability limits the pharmacotherapeutic potential AG. Therefore, in this study we aimed to formulate optimize AG-loaded nanoliposomes (AGL) using Design Experiment (DOE) approach further modify surface liposomes with mannosylated chitosan enhance its oral bioavailability. Physical,...

Lichens are symbiotic organisms that have been traditionally used for treating different kinds of ailments. As there only a few reports on the antiviral activity lichens, we thought evaluating anti-Herpes simplex virus-1 (HSV-1) methanolic extract Roccella montagnei and their isolated compounds. Fractionation crude by column chromatography two pure Antiviral was assessed using CPE inhibition assay at non-cytotoxic concentrations Vero cells. Molecular docking dynamics studies were carried out...

Iron-based metal-organic frameworks (MIL (101)) have recently gained attention in materials science for biomedical applications. In the present work, MOF (MIL-101(Fe)) were coated with lactoferrin (Lf) conjugated hyaluronic acid (HA) and investigated its potential delivering 5-fluorouracil (5-FU), along assessing toxicity profile. The synthesised nanoparticles extensively characterised using spectroscopic, X-Ray, thermal electron microscopic techniques. 5-FU was loaded into MOFs,...

Abstract Drug-induced liver injury can be caused by any drugs, their metabolites, or natural products due to the inefficient functioning of drug-metabolizing enzymes, resulting in reactive oxygen species generation and leading oxidative stress-induced cell death. For protection against stress, our has various defense mechanisms. One mechanisms is NRF2 pathway, when activated, protects stress. Natural antioxidants such as Sesamol have reported pharmacological activity (hepatoprotective &amp;...

Palbociclib and ribociclib are substrates of efflux transporter P-glycoprotein which plays a key role in absorption transport these drugs. Proton pump inhibitors, when co-administered with them known to show inhibitory effect on P-glycoprotein.Therefore, this study aims investigate the proton inhibitors inhibition mediated palbociclib ribociclib.A combined approach molecular docking ex vivo everted gut sac model was implemented predict potential i.e., omeprazole, esomeprazole, lansoprazole,...

Abstract Objectives Cyclin-dependent kinase inhibitors are subject to rapid first-pass metabolism, and their oral absorption is hindered by intestinal CYP3A4 P-gp. The present study investigates the impact of dietary polyphenols on pharmacokinetics palbociclib ribociclib, considering potential as modulators Methods Therefore, inhibitory effects drug metabolism efflux these drugs were investigated using molecular docking; in vitro preclinical assay rat liver microsomes Caco-2 cell monolayers;...

BACE-1 is a transmembrane protein occurring in the endoplasmic reticulum that responsible for generation of beta amyloid (Aβ) by cleavage precursor (APP). Deposition and aggregation Aβ brain results onset Alzheimer’s disease (AD). The process drug discovery this area sluggish most developed molecules fail due to toxicity. Research related phytochemicals has taken pace associated low toxicity comparatively. development inhibitors proven be promising treatment strategy AD. In current study,...

Introduction: Tuberculosis is a major respiratory disease globally with higher prevalence in Asian and African countries than rest of the world. With larger population tuberculosis patients anticipated to be co-infected COVID-19 infection, an ongoing pandemic, identifying, preventing managing drug–drug interactions inevitable for maximizing patient benefits current repurposed antitubercular drugs. Methods: We assessed potential between drugs using drug interaction checker IBM Micromedex®....

Herpes simplex virus (HSV) infections affect a wide range of the global population. The emergence resistance to existing anti-HSV therapy highlights necessity for an innovative strategy. interaction HSV gD with its main host receptor nectin-1 is potential target new antiviral drugs. aim this study was develop peptide derived from targeting using

Numerous clinical concerns have been expressed regarding the potential worsening of cyclin-dependent kinase 4/6 inhibitor effects in breast cancer patients because co-administration proton pump inhibitors. Hence, this study evaluated inhibitors on pharmacokinetics palbociclib and ribociclib terms cytochrome P450 (CYP) 3A4 P-glycoprotein involvement.

Background and objective: Concurrent usage of proton pump inhibitors their effect on survival medication termination has been found in individuals receiving protein kinase inhibitor chemotherapy. To investigate the drug-drug interaction mechanism between CDK inhibitors, in-silico docking approach was designed by applying computer simulation modules to predict binding inhibitory potential. Method: The potential predicted utilising molecular techniques that employed Schrödinger algorithms...

Tuberculosis (TB) is an air-borne infectious disease and the leading cause of death among all diseases globally. The current treatment regimen for TB overtly long patient non-compliance often leads to drug resistant resulting in a need develop new drugs that will act via novel mechanisms. In this research work, we selected Mycobacterium membrane protein large (MmpL3) as target indole-2-carboximide our molecule interest further designing molecules. A homology model was prepared tuberculosis...

Abstract Alzheimer's disease (AD) is the most common cause of dementia and one major causes death worldwide. The ability some natural compounds, such as flavonoids, to cross blood-brain barrier decrease progression disorders has been described in literature. This study aimed identify potential product molecules acetylcholinesterase inhibitors using silico computational approaches. A pharmacophore model was developed based on 3D structure protein–ligand complex protein (PDB:4EY7) Phase...