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12 protocols using gelucire 50 13

1

Dutasteride Solubility Enhancement with Cyclodextrins

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Dutasteride was purchased from Cipla Ltd (Mumbai, India). α-Cyclodextrin (α-CD), β-cyclodextrin (β-CD), γ-cyclodextrin (γ-CD) and hydroxypropyl-β-cyclodextrin (HP-β-CD) were obtained from Wacker Chemie AG (München, Germany). Polyvinylpyrrolidone K30 (PVP) (BASF, Germany), d-α-tocopheryl polyethylene glycol 1000 succinate (TPGS) (Isochem, France), stearoyl polyoxylglycerides (Gelucire 50/13) (Gattefosse, France), polyethyleneglycol (PEG400) (Yakuri Pure Chem, Japan) and polyethyleneoxide-polypropylene oxide copolymer (Poloxamer 407) (BASF, Germany) were used as solubilizers. Lactose (SuperTab 11SD) (DFE pharma, Japan), microcrystalline cellulose (Avicel PH102) (FMC, USA), crospovidone (Polyplasone XL) (Ashland, Netherland), magnesium stearate (Faci, Italy), Opadry® (Colorcon, Singapore) and ethylcellulose (Ethocel 10) (Colorcon, Korea) were used as excipients for the tablets. Avodart® soft capsules (GlaxoSmithKline, United Kingdom) were purchased from a local pharmacy.
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2

Ibuprofen Lipid-Based Formulation Development

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Ibuprofen (99.3% of purity, white crystalline powder) was purchased from Spectrum chemicals (New Brunswick, NJ, USA). All the lipid excipients Gelucire® 44/14, Gelucire® 48/16, Gelucire® 50/13, Transcutol® HP, and Maisine® CC were kindly gifted by Gattefosse (Paramus, NJ, USA). The solid adsorbent carriers Neusilin® US2 was gifted by Fuji chemical industries (Burlington, NJ, USA), Starch 1500® (partially pregelatinized maize starch) was donated by Colorcon (Harleysville, PA), and Avicel PH® 102 (microcrystalline cellulose) was donated by FMC Biopolymer (Philadelphia, PA, USA). All the disintegrants AC-DI-SOL®, Sodium starch glycolate, and Kollidon-CL® were donated by FMC Biopolymer (Philadelphia, PA, USA), Roquette (Geneva, IL, USA), and BASF (Ludwigshafen, Germany), respectively. The Slide-A-LyzerTM mini dialysis device with a molecular weight of 10 kDa was procured from ThermoFisher Scientific (Hampton, NH, USA). All other chemicals and solvents utilized in the current investigation are of analytical grade.
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3

Lipid-based Ophthalmic Drug Delivery

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AmB was purchased from Cayman Chemicals Pvt. Ltd. (Michigan, US). The solid lipids (Compritol™ 888 ATO, Precirol™ ATO 5, Geleol™, Dynasan™ 114, Dynasan™ 116, Gelucire™ 43/01, Gelucire™ 44/14, Gelucire™ 50/13) and liquid lipids (Labrafilm™, Maisine™, and Capryol 90™) were gift samples from Gattefossé (Weil and Rhein, Germany). mPEG-2K-DSPE(N-(Carbonyl-methoxypolyethylenglycol-2000)-1,2-distearoyl-sn-glycero-3-phosphoethanolamine- mPEG-2K-DSPE) was obtained from Lipoid GmbH (Germany). All other molecular weight mPEG-DSPE were obtained from Creative PEGWorks® (Chapel Hill, NC, USA). Surfactants, olive oil, Cremophor® EL, castor oil, oleic acid, and analytical grade solvents were procured from Fisher scientific (Massachusetts, US). Whole eyes of male albino New Zealand rabbits for the transcorneal study were procured from Pel-Freez® Biologicals (Rogers, AR, USA).
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4

Luliconazole Topical Formulation Development

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Luliconazole was obtained as a gift sample from Sun Pharmaceuticals, Gurgaon, India. Gelucire 50/13 and Precirol ATO 5 were obtained from Gattefosse, France (ex gratia). Tween 80, Kolliphor, Carbopol (grade 940) and Triethanolamine were obtained from Sigma Aldrich, India. All other chemicals and reagents used were of analytical grade and were used without further purifications.
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5

Development and Evaluation of Xarelto Formulations

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RXB (purity > 98.5%; Hanseo Chemical, Pyeongtaek, Korea) and Xarelto® tablets (20 mg, Bayer, Luverkusen, Germany) were purchased.
Polyvinylpyrrolidone-vinyl acetate 64 (PVP VA 64, Kollidone® VA 64), Soluplus® (Polyvinyl caprolactam-polyvinyl acetate-polyethylene glycol graft co-polymer), Cremophor® RH 40 (PEG-40 hydrogenated castor oil), polyvinylpyrrolidone K 90 (PVP 90), Solutol® HS 15 (Polyoxyl 15-hydroxystearate), and Kolliphor® 188 (Poloxamer 188) were obtained from BASF (Ludwigshafen, Germany). Polyvinylalcohol (PVA, MW 89,000–98,000) was purchased from Sigma (St. Louis, MO, USA), and polyethylene glycol (PEG) was purchased from Daejung (Seoul, Korea). Gelucire® 44/14 (Lauroyl polyoxy-32-glycerides) and Gelucire® 50/13 (Stearoyl macrogol-32 glycrides) were obtained from Gattefosse (Saint-Priest, France). Carboxymethyl cellulose (CMC) and hydroxypropyl cellulose (HPC) were purchased from Samchun (Pyeongtaek, Korea). Acetonitrile and methanol for HPLC were purchased from J.T. Baker (Seoul, Korea). All the other chemicals and reagents used were of analytical grade.
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6

Cellular Uptake of Protocatechuic Acid Ester

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Protocatechuic acid ethyl ester was purchased from Sigma Aldrich Chimica s.r.l. (Milan, Italy). Precirol® ATO 5 (glyceryl distearate) and Gelucire 50/13 were gifted by Gattefossé (Saint-Pries, France). Tween® 80 (polysorbate 80) was retrieved from Sigma Aldrich Co. (St. Louis, MO, USA). The chemical 1,2-dimyristoyl-sn-glycero-3-phosphocholine (DMPC) was purchased from Genzyme (Liestal, Switzerland).
The chemical 3-(4,5-dimethyl-2-thiazolyl)-2,5-diphenyl-2H-tetrazolium bromide (MTT), Dulbecco’s modified Eagle’s medium, fetal bovine serum, glucose, and penicillin–streptomycin, were obtained from Sigma Aldrich (Milan, Italy).
Human foreskin fibroblast (HFF-1) and human colorectal adenocarcinoma (CaCo-2) cells were bought from ATCC® SCRC-1041 TM (ATCC, Manassas, VA, USA). Purified water from Millipore-Q® Gradient A10TM ultra-pure water system (Millipore, Guyancourt, France) was produced as needed and employed for the duration of the studies.
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7

Lipid-based Nanoparticle Formulation Development

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VG was purchased from Megafine, Mumbai, India. Gelucire®50/13 (mp 50 °C) and Compritol®888 ATO (mp 70–77 °C) were purchased from Gattefossé, Saint-Priest, France. Carbomer®934 NF was purchased from PCCA, Houston, TX, USA. Hydrochloric acid and sodium chloride were purchased from Merck, Darmstadt, Germany. Ammonium dihydrogen phosphate was supplied from BDH, Poole Dorset, England. Potassium orthophosphate, ammonium formate, and formic acid were purchased from Merck, Germany.
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8

Formulation Development of Ramipril

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Drug (Ramipril), Tween 20, Span 80, and dimethyl sulfoxide (DMSO) were obtained as a gift sample from Emcure Pharmaceutical Limited Pune, India. Gelucire43/01, Gelucire 50/13, and Gelucire 48/16 were obtained as a gift sample from Gattefosse India Pvt. Ltd, Mumbai, India. All other chemicals used were of analytical grade.
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9

Lipid Nanosuspension for Dexamethasone Delivery

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The lipid components Gelucire® 50/13 (stearoyl macrogolglycerides,GATTEFOSSÉ GmbH, Bad Krozingen, Germany), Witepsol® S55 (solid triglycerides containing hydrogenated coco-glycerides, beeswax and ceteareth-25, CREMER OLEO GmbH & Co. KG, Hamburg, Germany), and Capryol® 90 (propylene glycol monocaprylate, Gattefossé GmbH, Bad Krozingen, Germany) were mixed in a ratio of 5:3:1 (w/ w) and melted at 60°C together with 0.5% (w/ w) PCA-labeled Dx. The 10% (w/ w) lipid nanosuspension was prepared from a nanoemulsion by pouring ultrapure water of the same temperature to the lipid melt and high-shear-homogenization for 5 minutes. Finally, the nanoemulsion was cooled to room temperature to solidify the lipid phase and thus, to obtain the lipid nanosuspension. The lipid nanosuspension was filtered through 0.7 µm glass fiber filters (Whatman® GF/F; Sigma-Aldrich Chemie GmbH, Steinheim, Germany) to eliminate precipitated drug crystals from the water phase.
Two different sizes of DxPCA loaded NLP were produced to study the effect of loading. Furthermore, DxPCA was incorporated into single lipid components of the NLP and in selected lipid combinations, with and without dispersion in water to associate the microenvironment of DxPCA in the NLP.
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10

Mucoadhesive Nanoparticle Formulation Development

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TA was obtained from TCI Europe N.V. (Zwijndrecht, Belgium). Poloxamer® 188 was purchased from Sigma-Aldrich (St Louis, MO, USA). Capryol® and Gelucire® 50/13 were gift samples from Gattefossé (Nanterre, France). Miglyol® was from Sasol (Hamburg, Germany). Eudragit® RS100 was obtained from Evonik (Essen, Germany). Lipoid® S75 was a gift sample from Lipoid®, Ludwigshafen, Germany. All other materials were of analytical grade. Mucin from porcine stomach (Type III, bound sialic acid 0.5%–1.5%, partially purified powder) was purchased from Sigma-Aldrich.
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