A mean-field approach for modeling the propagation of perturbations in biochemical reaction networks.

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Often, the time evolution of a biochemical reaction network is crucial for determining the effects of combining multiple pharmaceuticals. Here we illustrate a mathematical framework for modeling the dominant temporal […]

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Pharmacokinetic and tissue distribution study of ZCY-15, a novel compound against Alzheimer’s disease, in rats byliquid chromatography-tandem mass spectrometry.

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ZCY-15, N-(3,5-dimethyladamatan-1-yl)-N-(3-methylphenyl) urea, is a candidate compound synthesized from the memantine structure and has been shown to be remarkably effective in treating Alzheimer’s disease. To elucidate the pharmacokinetics and tissue […]

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Nose-to-brain delivery of phenytoin and its hydrophilic prodrug fosphenytoin combined in a microemulsion – formulation development and in vivo pharmacokinetics.

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Phenytoin is a low aqueous solubility antiepileptic drug, but its phosphate ester prodrug fosphenytoin is soluble, although less permeable. In a previous study, the intranasal administration of aqueous-based formulations of […]

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Multi-organ Targeting of HIV-1 Viral Reservoirs with Etravirine Loaded Nanostructured Lipid Carrier: An In-vivo Proof of Concept.

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The inadequate bioavailability and toxicity potential of antiretroviral therapy limit their effectiveness in the complete eradication of HIV from viral reservoirs. The penetration of these drugs into the brain is […]

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Crystalline Sponge Affinity Screening: A Fast Tool for Soaking Condition Optimization without the Need of X-ray Diffraction Analysis.

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Structural elucidation of small molecules only available in low quantity (nanogram) is one of the big advantages of the crystalline sponge method. The optimization of various soaking parameters is crucial […]

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Development and verification of an endogenous PBPK model to inform hydrocortisone replacement dosing in children and adults with cortisol deficiency.

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The goal of hormone replacement is to mirror physiology. Hydrocortisone granules and modified release formulations are being developed to optimise cortisol replacement in the rare disease of adrenal insufficiency. To […]

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Development of Gliclazide ionic liquid and the transdermal patches: an effective and noninvasive sustained release formulation to achieve hypoglycemic effects.

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Ionic liquids (IL) technology provides a useful platform to achieve the topical delivery of therapeutic agents, because of its capability to improve skin permeability. While the majority of the researches […]

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Electrospun gold nanorods/graphene oxide loaded-core-shell nanofibers for local delivery of paclitaxel against lung cancer during photo-chemotherapy method.

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The combinations of photothermal therapy (PTT) and chemotherapy (CHT) have attracted increasing attention for cancer therapy. In the present study, paclitaxel as an anticancer drug and graphene oxide/gold nanorods (GO/Au […]

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Improved efficacy and safety of low doses of benznidazole-loaded multiparticulate delivery systems in experimental Chagas disease therapy.

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Benznidazole (BZ) is a first-line drug for the treatment of Chagas disease; however, it presents several disadvantages that could hamper its therapeutic success. Multiparticulate drug delivery systems (MDDS) are promising […]

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Interface-sensitized prodrug nanoaggregate as an effective in situ antitumor vaccine.

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In situ antitumor vaccines have been widely explored as an effective strategy to inhibit tumor growth by stimulating antitumor immune responses. Herein, we reported a simple and effective in situ […]

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Flow Structure and Particle Deposition Analyses for Optimization of a Pressurized Metered Dose Inhaler (pMDI) in a Model of Tracheobronchial Airway.

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Inhalation therapy plays an important role in management or treatment of respiratory diseases such asthma and chronic obstructive pulmonary diseases (COPDs). For decades, pressurized metered dose inhalers (pMDIs) have been […]

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QbD-driven development of dissolving microneedle patch loaded with Ultradeformable liposomes encapsulated Noopept: Exploring a patient friendly, once-daily option to manage Dementia.

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Noopept (NPT), a potent neuroprotective agent, suffers the problem of poor oral bioavailability (∼10 %) and thus demands exploration of ways of bioavailability improvement. Present work focuses on confronting this […]

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Continuous downstream processing of milled electrospun fibers to tablets monitored by near-infrared and Raman spectroscopy.

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Electrospinning is a technology for manufacture of nano- and micro-sized fibers, which can enhance the dissolution properties of poorly water-soluble drugs. Tableting of electrospun fibers have been demonstrated in several […]

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Formulation of olopatadine hydrochloride viscous eye drops – physicochemical, biopharmaceutical and efficacy assessment using in vitro and in vivo approaches.

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The aim of this work was the formulation and the comprehensive evaluation of the viscous eye drops using vehicles containing medium chain chitosan (0.5% w/v), hydroxypropyl guar gum (0.25% w/v) […]

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Nondestructive Investigation of the Agglomeration Process for Nanosuspensions via NMR Relaxation of Water Molecules.

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This study investigated an agglomeration of nanoparticles in a suspension using nuclear magnetic resonance (NMR) relaxation. The nanosuspension was prepared by wet bead milling using indomethacin and polyvinylpyrrolidone as an […]

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How does pressure affect the molecular dynamics, intramolecular interactions, and the relationship between structural (α) and secondary (JG-β) relaxation above and below the glass transition temperature in binary mixtures of H-bonded API – probucol and acetylated saccharides?

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In this paper, the molecular dynamics as well as inter- and intramolecular interactions in the homogenous solid dispersions (SDs) of active pharmaceutical ingredient – probucol (PRO) with acetylated glucose (acGLU), […]

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Comparative efficacy evaluation of different penetration enhancement strategies for dermal delivery of poorly soluble drugs – a case with sertaconazole nitrate.

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The aim of this study was to compare the efficacy of different approaches for enhancement of dermal availability of the highly lipophilic antifungal model drug – sertaconazole nitrate (SN). For […]

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Physiologically based modelling of tranexamic acid pharmacokinetics following intravenous, intramuscular, sub-cutaneous and oral administration in healthy volunteers.

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Tranexamic acid (TXA) is an antifibrinolytic drug that reduces surgical blood loss and death due to bleeding after trauma and post-partum haemorrhage. Treatment success is dependent on early intervention and […]

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Recent advances of dendrimers as multifunctional nano-carriers to combat breast cancer.

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Breast cancer (BC) is a highly heterogeneous malignant carcinoma that is the most frequently occurring cancer in women. The major types of BC are luminal A, basal-like, luminal B, human […]

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Revisiting Inorganic Nanoparticles as Promising Therapeutic Agents: A Paradigm Shift in Oncological Theranostics.

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Cancer remains a global health problem largely due to a lack of effective therapies. Major cancer management strategies include chemotherapy, surgical resection, and radiation. Unfortunately, these strategies have a number […]

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Combining modeling of drug uptake and release of cyclosporine in contact lenses to determine partition coefficient and diffusivity.

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Ophthalmic drug delivery via eye drops is inefficient because only about 1-5% of the drug permeates the cornea during the short residence time of a few minutes. Contact lenses are […]

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Atypical kinetics of cytochrome P450 2J2: epoxidation of arachidonic acid and reversible inhibition by xenobiotic inhibitors.

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Extrahepatic CYP2J2 metabolism of arachidonic acid (AA) to bioactive regioisomeric epoxyeicosatrienoic acids (EETs) is implicated in both physiological and pathological conditions. Here, we aimed to characterize atypical substrate inhibition kinetics […]

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Design and characterization of highly porous curcumin loaded freeze-dried wafers for wound healing.

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The goal of this research was to evaluate the beneficial effects of topical curcumin loaded freeze-dried wafers in wound healing. Curcumin wafers were fabricated by cross-linking of chitosan with beta […]

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A novel crystalline molecular salt of sulfamethoxazole and amantadine hybridizing antiviral-antibacterial dual drugs with optimal in vitro/vivo pharmaceutical properties.

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In order to exploit the advantages to the full of multidrug salification strategy in amending the pharmaceutical properties of drugs both in vitro and in vivo, and further to open […]

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Gamma sterilization and in vivo evaluation of cationic nanostructured lipid carriers as potential ocular delivery systems for antiglaucoma drugs.

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Solid lipid nanoparticles and nanostructured lipid carriers showed promising results for enhancement of ocular bioavailability of drugs with poor corneal permeability. One of these drugs is methazolamide, which is an […]

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Optimization of a floating poloxamer 407-based hydrogel using the Box-Behnken design: in vitro characterization and in vivo buoyancy evaluation for intravesical instillation.

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Intravesical instillation of a poloxamer 407 (PLX)-based hydrogel offers advantages such as thermo-sensitivity and sol-to-gel transition, but its utility is limited by urinary obstruction and insufficient bladder residence time. To […]

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The promising pro-healing role of the association of mesoglycan and lactoferrin on skin lesions.

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Skin wound repair represents an important topic for the therapeutic challenges. Many molecules are commonly used as active principles of topical devices to induce the correct tissue regeneration. Among these […]

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The impact of the intestinal microbiota and the mucosal permeability on three different antibiotic drugs.

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BackgroundThe totality of bacteria, protozoa, viruses and fungi that lives in the human body is called microbiota. Human microbiota specifically colonizes the skin, the respiratory and urinary tract, the urogenital […]

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Relationship between anti-fungal effects and lung exposure of PC945, a novel inhaled antifungal agent, in Aspergillus fumigatus infected mice: Pulmonary PK-PD analysis of anti-fungal PC945.

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PC945 is a novel antifungal agent, optimised for inhaled treatment. In this study, the relationship between antifungal effects of PC945 and its exposure in the lungs was investigated in Aspergillus […]

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Estriol dissolving microneedle patches for protection against ionizing radiation-induced injury.

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Estriol can be used to treat radiation-induced leukopenia by increasing peripheral blood leukocytes and therefore it plays an important role in radiation protection. However, only high-dose injectable suspensions are available […]

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