Search Results - "Zakelj, Simon"
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A review of methods for solubility determination in biopharmaceutical drug characterization
Published in Drug development and industrial pharmacy (02-11-2019)“…The significance of thermodynamic solubility in biopharmaceutical compound or drug characterization as well as the importance of having methods that accurately…”
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Suitability of RPMI 2650 cell models for nasal drug permeability prediction
Published in European journal of pharmaceutics and biopharmaceutics (01-12-2019)“…[Display omitted] The RPMI 2650 cell line has been a subject of evaluation as a physiological and pharmacological model of the nasal epithelial barrier…”
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The Magic of Crystal Structure-Based Inhibitor Optimization: Development of a Butyrylcholinesterase Inhibitor with Picomolar Affinity and in Vivo Activity
Published in Journal of medicinal chemistry (11-01-2018)“…The enzymatic activity of butyrylcholinesterase (BChE) in the brain increases with the progression of Alzheimer’s disease, thus classifying BChE as a promising…”
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Suitability and functional characterization of two Calu-3 cell models for prediction of drug permeability across the airway epithelial barrier
Published in International journal of pharmaceutics (30-07-2020)“…[Display omitted] The Calu-3 cell line has been largely investigated as a physiological and pharmacological model of the airway epithelial barrier. Its…”
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Stereoselective Activity of 1‑Propargyl-4-styrylpiperidine-like Analogues That Can Discriminate between Monoamine Oxidase Isoforms A and B
Published in Journal of medicinal chemistry (13-02-2020)“…The resurgence of interest in monoamine oxidases (MAOs) has been fueled by recent correlations of this enzymatic activity with cardiovascular, neurological,…”
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Applicability of RPMI 2650 and Calu-3 Cell Models for Evaluation of Nasal Formulations
Published in Pharmaceutics (06-02-2022)“…The RPMI 2650 and Calu-3 cell lines have been previously evaluated as models of the nasal and airway epithelial barrier, and they have demonstrated the…”
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Treatment of canine cognitive dysfunction with novel butyrylcholinesterase inhibitor
Published in Scientific reports (13-09-2021)“…Canine cognitive dysfunction (CCD) is common in aged dogs and has many similarities with Alzheimer’s disease. Unfortunately, like Alzheimer’s disease, CCD…”
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Development of an in-vivo active reversible butyrylcholinesterase inhibitor
Published in Scientific reports (21-12-2016)“…Alzheimer’s disease (AD) is characterized by severe basal forebrain cholinergic deficit, which results in progressive and chronic deterioration of memory and…”
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How Azide Ion/Hydrazoic Acid Passes Through Biological Membranes: An Experimental and Computational Study
Published in The Protein Journal (01-06-2023)“…Hydrazoic acid (HN 3 ) and its deprotonated form azide ion (N 3 − ) (AHA) are toxic because they inhibit the cytochrome c oxidase complex IV (CoX IV) embedded…”
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10
The effect of lipid composition and liposome size on the release properties of liposomes-in-hydrogel
Published in International journal of pharmaceutics (01-11-2013)“…To study the release of liposome-associated drugs into hydrogels, we designed and synthesized two pH-sensitive rhodamine derivatives to use as model compounds…”
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Biopharmaceutical classification of desloratadine - not all drugs are classified the easy way
Published in Acta Pharmaceutica (01-06-2020)“…The biopharmaceutical classification of drugs was designed as a basis for bio-waivers - a mechanism with the double ethical benefit of delivering new drug…”
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Mechanical properties and drug permeability of the PA6 membranes prepared by immersion precipitation from PA6 – formic acid – water system
Published in Journal of membrane science (15-09-2018)“…The paper presents the effect of polymer solution composition on the morphology, mechanical properties and drug permeability of the asymmetric polyamide 6…”
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Indoles and 1-(3-(benzyloxy)benzyl)piperazines: Reversible and selective monoamine oxidase B inhibitors identified by screening an in-house compound library
Published in Bioorganic chemistry (01-02-2022)“…[Display omitted] •MAO-B inhibitors were identified in the screening of the in-house compound library.•Exploration of SARs led to selective micromolar…”
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Determination of permeability coefficients of ophthalmic drugs through different layers of porcine, rabbit and bovine eyes
Published in European journal of pharmaceutical sciences (30-08-2012)“…Comparison of permeability coefficients of lidocaine, ciprofloxacin, timolol and dexamethasone for the cornea and a multi-layer complex of porcine, bovine and…”
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8-Hydroxyquinolylnitrones as multifunctional ligands for the therapy of neurodegenerative diseases
Published in Acta pharmaceutica Sinica. B (01-05-2023)“…We describe the development of quinolylnitrones (QNs) as multifunctional ligands inhibiting cholinesterases (ChEs: acetylcholinesterase and…”
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Thematic issue on drug delivery for specific populations
Published in European journal of pharmaceutical sciences (30-07-2015)Get full text
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Decreasing acidity in a series of aldose reductase inhibitors: 2-Fluoro-4-(1H-pyrrol-1-yl)phenol as a scaffold for improved membrane permeation
Published in Bioorganic & medicinal chemistry (01-04-2014)“…Targeting long-term diabetic complications, as well as inflammatory pathologies, aldose reductase inhibitors (ARIs) have been gaining attention over the years…”
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In vitro interactions between aged garlic extract and drugs used for the treatment of cardiovascular and diabetic patients
Published in European journal of nutrition (01-09-2010)“…Background Disease preventing effects gained by garlic consumption have been recognized since early period of history, making commercially available garlic…”
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Correlative study of functional and structural regeneration of urothelium after chitosan-induced injury
Published in Histochemistry and cell biology (01-11-2013)“…High transepithelial electrical resistance (TEER) demonstrates a functional permeability barrier of the normal urothelium, which is maintained by a layer of…”
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Aged Garlic Extract Stimulates P-Glycoprotein and Multidrug Resistance Associated Protein 2 Mediated Effluxes
Published in Biological & Pharmaceutical Bulletin (01-04-2009)“…The growing concomitant consumption of drugs and herbal preparations such as garlic, and the numerous reports about the influence of herbal preparations on…”
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