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7 protocols using sodium taurocholate

1

Ridinilazole Activity Against C. difficile

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Ridinilazole was provided by Summit Therapeutics and re-suspended in DMSO (Sigma–Aldrich). C. difficile strain R20291 (BI/027/NAP1) was used for all the experiments. All cultures were grown in a vinyl anaerobic chamber (Coy Lab Products) at 37°C. Liquid microbiological cultures were grown in brain–heart infusion (BHI) medium (Hardy Diagnostics) supplemented with 0.1% sodium taurocholate (Alfa Aesar) during time–kill experiments. For colony recovery and counts, bacteria were grown on blood agar plates (Hardy Diagnostics). Metronidazole and vancomycin were purchased from commercial suppliers (Sigma–Aldrich). Caco-2 human gut epithelial cells were grown in Eagle's minimal essential medium (EMEM; ATCC 302003) for measurements of IL-8 release.
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2

In Vitro Dissolution of Oral Dosage Forms

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The selected commercial drug products were purchased from a public pharmacy (Table 1). Hard gelatin capsules size 4 (Capsula GmbH, Ratingen, Germany) were used for those formulations, which represented pellets or powders. Tablet formulations were dose proportionally cut with a knife to create the respective in vitro dose (Table 1). The buffer concentrate contained tri-potassium phosphate (Alfa Aesar, Kandel, Germany), tri-potassium citrate (Carl Roth, Karlsruhe, Germany), and sodium hydroxide (VWR Chemicals, Darmstadt, Germany). Sodium-taurocholate, lecithin and 1-decanol were purchased from Alfa Aesar (Kandel, Germany). The high performance liquid chromatography HPLC chemicals consisted of methanol (VWR Chemicals, Darmstadt, Germany), and demineralized water (Merck Milli-Q, Darmstadt, Germany). 0.1 N hydrochloric acid was purchased from VWR Chemicals (Darmstadt, Germany). The following drug substances were used: aprepitant (TCI Deutschland, Eschborn, Germany), celecoxib (Acros Organics, Thermo Fisher Scientific, Geel, Belgium), itraconazole (Acros Organics, Thermo Fisher Scientific, Geel, Belgium), nimodipine (Alphar aesar, Landau, Germany) and ritonavir (AbbVie Deutschland GmbH & Co. KG, Ludwigshafen, Germany).
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3

Celecoxib Solubility Enhancement via Polymer Blends

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Polyvinyl alcohol (PVA, Parteck MXP®) was kindly donated by Merck (Darmstadt, Germany). HPMCAS LG (hydroxypropylmethylcellulose acetate succinate) was provided by Shin-Etsu Chemical (Tokyo, Japan). Copovidone, Kolliphor P188 and Kolliphor P407 were donated by BASF (Ludwigshafen, Germany). HPC-SSL was obtained from Nisso Chemical Europe (Düsseldorf, Germany) and Eudragit L100-55 was obtained from Evonik (Darmstadt, Germany). Celecoxib (CXB) was obtained from Swapnroop Drugs & Pharmaceuticals (Aurangabad, India) (Figure 1). Lecithin and sodium taurocholate were purchased from Alfa Aesar (Haverhill, MA, USA). FaSSIF-V2 medium was prepared according to Denninger et al. [30 (link)], in henceforth will be referred to as FaSSIF.
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4

Ritonavir Amorphous Solid Dispersion Characterization

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Neat ritonavir and ritonavir-ASD were provided by AbbVie Germany, Ludwigshafen, Germany. The ritonavir-ASD was prepared as extrudate beads by hot melt extrusion on a co-rotating twin-screw extruder, and composed of ritonavir (15%), copovidone (74%), sorbitan monolaurate (10%), and colloidal silicon dioxide (1%). The purity of the ingredients was according to the compendial specifications (Ph.Eur./USP). The absence of API-related crystallinity in the ASD was confirmed by polarized light microscopy (Model DMLM, Leica Microsystems, Wetzlar, Germany). Tri-potassium phosphate (Alfa Aesar, Kandel, Germany), tri-potassium citrate (Carl Roth, Karlsruhe, Germany), and sodium hydroxide (VWR Chemicals, Darmstadt, Germany) were used for the buffer concentrate. Lecithin, 1-decanol, and sodium taurocholate were obtained from Alfa Aesar (Kandel, Germany). Glitter powder was purchased from Jofrika Cosmetics, Bergisch-Gladbach, Germany. The high performance liquid chromatography HPLC chemicals consisted of methanol (VWR Chemicals, Darmstadt, Germany), acetonitrile (VWR Chemicals, Darmstadt, Germany), and demineralized water (Merck Milli-Q, Darmstadt, Germany). Samples for HPLC were filtered through a 0.45 µm cellulose acetate syringe filter (VWR Chemicals, Darmstadt, Germany).
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5

Itraconazole Metabolite Quantification Protocol

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The model drug itraconazole (ITZ) was obtained from Sris Pharmaceuticals (Hyderabad, India). Hydroxy-itraconazole (OH-ITZ, 0.1 mg/ml methanol solution), the major active metabolite of ITZ in rats (Yoo et al., 2000 (link)) as well as in humans (Heykants et al., 1989 (link)), was obtained from Sigma-Aldrich (Taufkirchen, Germany). Ketoconazole (KTZ), the internal standard, was obtained from ThermoFisher (Kandel, Germany). Sporanox® 100 mg capsules were obtained from Janssen GmbH (Neuss, Germany). HPC-SL (MW = 100,000 g/mol; 73.5% Hydroxypropoxy groups), -SSL (MW = 40,000 g/mol; 73.7% Hydroxypropoxy groups) and -UL (MW = 20,000 g/mol; 70.1% Hydroxypropoxy groups) were kindly donated by Nippon Soda Co., Ltd. (Tokyo, Japan). Affinisol® HME15LV (HPMC) was donated from Dow Chemical Company, (Bomlitz, Germany). LC-MS grade water was obtained from Bernd Kraft GmbH (Duisburg, Germany). LC-MS grade acetonitrile (AcN), potassium citrate monohydrate (> 99%) were obtained from VWR Chemicals GmbH (Darmstadt, Germany). Lecithin, sodium taurocholate, 1-decanol and potassium phosphate were obtained from ThermoFisher (Kandel, Germany). Sodium hydroxide was obtained from Honeywell Fluka (Seelze, Germany). 0.1 N HCl solutions were obtained from VWR Chemicals (Fontenay-sous-Bois, France). Dimethyl sulfoxide (DMSO, > 99.9%) was obtained from Fisher Scientific (Geel, Belgium).
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6

Curcumin-Based Nanoformulation Development

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Curcumin (Cur) 97%, oleic acid 90%, stearic acid 97%, polysorbate 20 (tween 20), sodium taurocholate 96%, sodium glycocholate 97.5%, hydrogen peroxide 29%, and deionized water were procured from Alfa Aesar (Thermo Fisher Scientific, Dreieich, Germany), whereas linalool and geraniol were procured from Acros Organics (Thermo Fisher Scientific, Dreieich, Germany). Skweez (contains Imidacloprid 34%) insecticide was purchased locally from Semadak (Damanhur, El Beheira governorate Egypt). All chemical reagents were utilized without being purified, with the exception of Skweez insecticide, which was lyophilized to produce a powder.
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7

Formulation and Characterization of Lipid Nanocarriers

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CorA was provided by the Helmholtz Centre for Infection Research (Braunschweig, Germany). Polyvinylpyrrolidone (Kollidon® 30 LP) and vinylpyrrolidone-vinyl acetate copolymer (Kollidon® VA 64) were kindly provided by BASF SE (Ludwigshafen, Germany). Ethanol 99.8% and tri-potassium citrate were purchased from Carl Roth GmbH & Co. KG (Karlsruhe, Germany). Tri-potassium phosphate, lecithin, 1-decanol and sodium taurocholate were purchased from Thermo Fisher GmbH (Kandel, Germany). Sodium oleate was purchased from Sigma (Darmstadt, Germany). Glycerol mono-oleate was kindly provided by Gattefosseé SAS (Saint-Priest, France). In addition, 1-micron full-flow polyethylene filters were purchased from Cole-Parmer GmbH. Acetic acid was purchased by Sigma Aldrich Chemie GmbH (Steinheim, Germany). Sodium hydroxide was purchased from VWR International, LLC (Darmstadt, Germany). Water for injection was purchased from Fresenius Kabi Deutschland GmbH (Bad Homburg, Germany). LC-MS grade acetonitrile and water were purchased from Bernd Kraft GmbH (Duisburg, Germany), and LC-MS grade ammonium acetate from Merck KGaA (Darmstadt, Germany). Cell culture reagents were purchased from Sigma Aldrich (Taufkirchen, Germany).
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