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Kleptose

Manufactured by Roquette
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Sourced in France, Belgium

KLEPTOSE is a high purity beta-cyclodextrin product manufactured by Roquette. It is a white, crystalline powder and serves as a functional excipient for the pharmaceutical and nutraceutical industries.

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Lab products found in correlation

Bhi broth, by BD (2 mentions) Methocel k100m cr, by Colorcon (1 mentions) Kollidon va64, by BASF (1 mentions) Magnesium stearate, by Fagron (1 mentions) Methanol meoh, by Chem-Lab (1 mentions) Hydroxypropyl β cyclodextrin, by Roquette (1 mentions) Ethanol, by Labsynth (1 mentions) Hydrochloric acid (hcl), by Labsynth (1 mentions) Methanol, by Labsynth (1 mentions) Luminol, by Merck Group (1 mentions) Aerosil 200, by Evonik (1 mentions) Ldh liquiform, by Labtest (1 mentions) Triton x 100, by Vetec (1 mentions) Tween 80, by Thermo Fisher Scientific (1 mentions) Dimethyl sulfoxide (dmso), by Merck Group (1 mentions) Methylcellulose, by Merck Group (1 mentions) Olaparib, by AstraZeneca (1 mentions) Crysmeb, by Roquette (1 mentions)

9 protocols using kleptose

1

Development of Honey-Propolis Hydrogel

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All reagents used were of standard analytical grade. HM pectin from apple (HMP, Degree of esterification = 70–75%, Sigma-Aldrich, Darmstadt, Germany) was used as received. Manuka Honey (MGO 550+, Manuka Health, Auckland, New Zealand) and crude propolis (Propolis from Taygetus Mountain, Green Family-Ellinikon, Thessaloniki, Greece) were kept in the dark at 4 °C and warmed to room temperature prior to use. Beta cyclodextrin (kleptose®, Roquette, Zaventem, Belgium) was used as received.
Andriotis E.G., Eleftheriadis G.K., Karavasili C, & Fatouros D.G. (2020). Development of Bio-Active Patches Based on Pectin for the Treatment of Ulcers and Wounds Using 3D-Bioprinting Technology. Pharmaceutics, 12(1), 56.
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2

Tolcapone Formulation Development and Evaluation

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The active substance under study is tolcapone (batches: SOM0114599 and SOM0714600) (CCN Industries LTD via Porschem Pharm).
The excipients studied are Vivapur® 102 (JRS, Rosenberg, Germany), Avicel® PH 101 (FMC Corp, Brusseles, Belgium), Kleptose® (ROQUETTE, Roquette Frères, Lestrem, France), Kollidon® VA 64 (BASF, Ludwigshafen, Germany), Prosolv® HD90 (JRS, Rosenberg, Germany), Isomalt® 721 (GalenIQ, Manheim, Germany), Methocel® K100M CR (Colorcon, Dartford, UK), talc (Fagron, Terrassa, Spain), magnesium stearate (Fagron, Terrassa, Spain), and colloidal silicon dioxide (Fagron, Terrassa, Spain).
Nardi-Ricart A., Nofrerias-Roig I., Suñé-Pou M., Pérez-Lozano P., Miñarro-Carmona M., García-Montoya E., Ticó-Grau J.R., Insa Boronat R, & Suñé-Negre J.M. (2020). Formulation of Sustained Release Hydrophilic Matrix Tablets of Tolcapone with the Application of Sedem Diagram: Influence of Tolcapone’s Particle Size on Sustained Release. Pharmaceutics, 12(7), 674.
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3

Ropinirole HCl Cyclodextrin Complexation

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Ropinirole HCl was kindly supplied by Pharmathen SA, Greece. Sulfobutyl ether-βcyclodextrin (SBE-β-CD) and hydroxypropyl-β-cyclodextrin (HP-β-CD) KLEPTOSE ® were purchased from Roquette (Lestrem, France) Captisol ® (La Jolla, USA) with MW 2170 and 1400 g/mol respectively. Methanol (MeOH) was purchased from Chem-Lab NV (Belgium) and CH3COONH4 (MW 77.08) from Panreac Quimica SA (Spain).
Buffer pH 6.8 solution simulating saliva was prepared using NaCl (0.85 g), Na2HPO4 (0.20 g) and NaH2PO4. 2H2O (0.13 g) in 100 mL of distilled water. Phosphate buffered saline (PBS) pH 7.4, was prepared by dissolving NaCl (8.0g), KCl (0.20 g), Na2HPO4
(1.44 g), and KH2PO4 (0.24 g) in 1L of distilled water. Low molecular weight (LMW, 150 kDa, DD 95 -98 %) chitosan was obtained from Fluka UK. Methyl iodide and 1methyl-2-pyrrolidinone were obtained from Across Organics, Belgium. All chemicals and solvents were of analytical grade and all components of buffer solutions were purchased from Merck (Germany).
Kontogiannidou E., Andreadis D.A., Zografos A.L., Nazar H., Klepetsanis P., van der Merwe S.M, & Fatouros D.G. (2017). Ex vivo buccal drug delivery of ropinirole hydrochloride in the presence of permeation enhancers: the effect of charge. Pharmaceutical development and technology, 22(8).
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4

Piroxicam-Cyclodextrin Inclusion Complex

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Piroxicam (PX) and low molecular weight chitosan (LMW, 150 kDa, DD 95–98%) were obtained from Sigma Aldrich (Munich, Germany). β-cyclodextrin (β-CD), methylated-β-cyclodextrin (number of methyl groups per molecule (DS) = 0.57) and hydroxypropyl-β-cyclodextrin (average number of hydroxypropyl groups per anhydroglucose unit (MS) = 0.85) KLEPTOSE® were purchased from Roquette (Lestrem, France), with MW 1135, 1191 and 1376 g/mol, respectively. All chemicals and solvents were of analytical grade.
Simulating saliva buffer (pH 6.8) was prepared using sodium chloride (0.8 g), sodium phosphate dibasic (2.38 g), and potassium phosphate monobasic (0.19 g) in 1 L of distilled water. Phosphate buffer saline (PBS) pH 7.4 was prepared by dissolving sodium chloride (8.0 g), potassium chloride (0.20 g), sodium phosphate dibasic (1.44 g), and potassium phosphate monobasic (0.24 g) in 1 L of distilled water. All components of buffer solutions were purchased from Merck (Darmstadt, Germany).
Kontogiannidou E., Ferrari M., Deligianni A.D., Bouropoulos N., Andreadis D.A., Sorrenti M., Catenacci L., Nazari K., Arshad M.S., Chang M.W., Ahmad Z, & Fatouros D.G. (2019). In Vitro and Ex Vivo Evaluation of Tablets Containing Piroxicam-Cyclodextrin Complexes for Buccal Delivery. Pharmaceutics, 11(8), 398.
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5

Listeria Infection and FX11 Treatment

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Listeria monocytogenes (wild-type strain 10403S) were kindly provided by Dr. Eric G. Pamer (The University of Chicago, Department of Medicine, IL) and grown in brain-heart infusion (BHI) broth (Becton Dickinson, Sparks, MD), and 12 week old female WT and MYC cKO mice were infected by intravenous injection of 5000 bacteria per animal as previously described (Serbina et al., 2003 (link)). 3 days post infection, mouse spleens were homogenized in PBS containing 0.1% Triton X-100 to extract bacteria, and colony-forming units were measured by plating serial dilutions of homogenates on BHI plates overnight at 37°C. To analyze the effect of FX11 (EMD Millipore), 12 week old C57BL/6J female mice were randomized and treated with either vehicle or FX11 (2.5 mg/kg) i.p. on day −1 and day 0 and infected with Listeria monocytogenes. FX11 was prepared in 10% KLEPTOSE (Roquette Pharma) following the manufacturer’s instructions.
Bae S., Uk Park P.S., Lee Y., Mun S.H., Giannopoulou E., Fujii T., Lee K.P., Violante S.N., Cross J.R, & Park-Min K.H. (2021). MYC-mediated early glycolysis negatively regulates proinflammatory responses by controlling IRF4 in inflammatory macrophages. Cell reports, 35(11), 109264.
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6

Listeria Infection and FX11 Treatment

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Listeria monocytogenes (wild-type strain 10403S) were kindly provided by Dr. Eric G. Pamer (The University of Chicago, Department of Medicine, IL) and grown in brain-heart infusion (BHI) broth (Becton Dickinson, Sparks, MD), and 12 week old female WT and MYC cKO mice were infected by intravenous injection of 5000 bacteria per animal as previously described (Serbina et al., 2003 (link)). 3 days post infection, mouse spleens were homogenized in PBS containing 0.1% Triton X-100 to extract bacteria, and colony-forming units were measured by plating serial dilutions of homogenates on BHI plates overnight at 37°C. To analyze the effect of FX11 (EMD Millipore), 12 week old C57BL/6J female mice were randomized and treated with either vehicle or FX11 (2.5 mg/kg) i.p. on day −1 and day 0 and infected with Listeria monocytogenes. FX11 was prepared in 10% KLEPTOSE (Roquette Pharma) following the manufacturer’s instructions.
Bae S., Uk Park P.S., Lee Y., Mun S.H., Giannopoulou E., Fujii T., Lee K.P., Violante S.N., Cross J.R, & Park-Min K.H. (2021). MYC-mediated early glycolysis negatively regulates proinflammatory responses by controlling IRF4 in inflammatory macrophages. Cell reports, 35(11), 109264.
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7

Evaluation of Antioxidant Compounds

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The chemicals used in this study are as follows: methanol (A1085.01.BJ), aluminum chloride (C1036.01.AG), ethanol (A1084.01.BJ), and hydrochloric acid (A1028.01.BJ; Labsynth, Diadema, SP, Brazil); sodium tungstate-2-hydrate (230), triton X-100, and phosphomolybdic acid (443; Vetec Química Fina Ltda, Duque de Caxias, RJ, Brazil); gallic acid monohydrate (27645-250G-R), 1,1-diphenyl-2-picrylhydrazyl (DPPH•; D9132), luminol (5-amino-2,3-dihydro-1,4-phthalazinedione; A8511-5G), phorbol-12-myristate-13-acetate (PMA; P8139), and Trypan blue (T6146-25G; Sigma-Aldrich, St. Louis, MO, USA); gelatin (microbiological grade; 214320, Difco, Laboratories, Detroit, MN, USA); dimethyl sulfoxide (DMSO; 3317275) (Merck-Schuchardt, Hohenbrunn, DE); “Kit” to determine lactate dehydrogenase enzyme (LDH Liquiform; 86-2/30—Labtest Diagnostica, Lagoa Santa, MG, Brazil). Drying carriers used are colloidal silicon dioxide (Aerosil 200, Evonik Degussa, Hanau, Germany), maltodextrin (MOR-REX 1910, Corn Products do Brasil), β-cyclodextrin (Kleptose; Roquette, Lestrem, FR), and gum Arabic (Encapsia; NEXIRA do Brasil, São Paulo, SP, Brazil).
Fernandes M.R., Azzolini A.E., Martinez M.L., Souza C.R., Lucisano-Valim Y.M, & Oliveira W.P. (2014). Assessment of Antioxidant Activity of Spray Dried Extracts of Psidium guajava Leaves by DPPH and Chemiluminescence Inhibition in Human Neutrophils. BioMed Research International, 2014, 382891.
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8

Neratinib and Olaparib Preparation Protocols

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Neratinib was obtained from Puma Biotechnology (Los Angeles, CA) through an MTA. It was dissolved in dimethyl sulfoxide (Sigma-Aldrich, St. Louis, MO) as a 10mM stock solution for the in vitro experiment. For the in vivo experiments, sterile water with 0.5% methylcellulose (Sigma Life Science, St. Louis, MO) and 0.4% of Tween 80 (Fisher Bioreagents) was used to dissolve neratinib to a concentration of 4mg/mL to ensure a dose of 20mg/kg in mice with 100 μL oral gavage volume. Olaparib was obtained from AstraZeneca (Cambridge, United Kingdom). It was prepared in the same way as neratinib for the in vitro study. For the in vivo experiment, it was dissolved in 50% Kleptose (Roquette-Pharma) and sterile water to reach a concentration of 10mg/mL to ensure a dose of 50 mg/kg in mice in 100 μL oral gavage volume.
Saito S., Sasai M, & Yomo T. (1997). Evolution of the folding ability of proteins through functional selection. Proceedings of the National Academy of Sciences of the United States of America, 94(21), 11324-11328.
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9

Cyclodextrin and Squalene Protocol

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β-cyclodextrin (βCD, Kleptose®) and randomly methylated β-cyclodextrin (Me-βCD, Crysmeb) were purchased from Roquette Pharma (Lestrem, France), Figure 1. Squalene (98%) was obtained from Alfa Aesar™ (density = 0.858 g/mL).
Van NGUYEN A., DEINEKA V.I., VU A.T., LE T.D., TRAN-TRUNG H, & NGUYEN T.A. (2022). Inclusion complexes of squalene with beta-cyclodextrin and methyl-beta-cyclodextrin: preparation and characterization. Turkish Journal of Chemistry, 47(1), 294-306.
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