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Lestrem, France

Krenzlin S.,University of Lille Nord de France | Krenzlin S.,French Institute of Health and Medical Research | Siepmann F.,University of Lille Nord de France | Siepmann F.,French Institute of Health and Medical Research | And 6 more authors.
Drug Development and Industrial Pharmacy | Year: 2011

Background: Colon specific drug delivery can significantly improve the efficacy of local treatments of inflammatory bowel diseases. Film coatings containing the starch derivative Nutriose have recently been reported to minimize 5-ASA release in media simulating the upper gastro intestinal tract (GIT), while releasing the drug in a time-controlled manner upon contact with feces from Crohn's Disease and Ulcerative Colitis patients. It was the aim of this study to prepare Nutriose-containing matrix pellets and mini tablets in order to avoid a film coating step. Methods: Highly dosed matrix pellets were prepared by extrusion-spheronization, highly dosed mini tablets by compression. Various types of lipids were added and drug release measured in 0.1 N HCl and phosphate buffer pH 6.8, optionally containing pepsin and pancreatin. Results: The type of added lipid and the preparation technique, in particular the curing conditions, significantly affected the resulting drug release kinetics. Glyceryl palmitostearate containing pellets and mini tablets showed the most promising results upon appropriate curing, minimizing premature drug release in media simulating the upper GIT. Conclusion: The proposed novel multiparticulates do not require a film coating step and show an interesting potential for site-specific drug delivery to the colon of inflammatory bowel disease patients. © 2011 Informa Healthcare USA, Inc. Source


Karrout Y.,Charles de Gaulle University - Lille 3 | Karrout Y.,French Institute of Health and Medical Research | Dubuquoy L.,French Institute of Health and Medical Research | Piveteau C.,Charles de Gaulle University - Lille 3 | And 24 more authors.
Journal of Controlled Release | Year: 2015

The first proof of concept in vivo for a new type of microbiota-sensitive film coatings allowing for colon targeting is presented. The efficacy of these polysaccharide barriers to optimize drug release for the treatment of inflammation is demonstrated in an experimental colitis model with Wister rats. 5-Aminosalicylic acid (5-ASA) pellets were prepared by extrusion-spheronization and coated with Nutriose:ethylcellulose (EC) 1:4 or peas starch:ethylcellulose 1:2 blends. The pellets were mixed with standard chow, and the daily drug dose was 150 mg/kg. For reasons of comparison, also commercially available Pentasa pellets and placebo pellets were studied. At day 3 after the beginning of the treatment, colitis was induced by intrarectal administration of trinitrobenzene sulfonic acid (TNBS). Animals were sacrificed on day 6. Macroscopic and histological evaluations of colitis were performed blindly. In addition, inflammatory markers were evaluated using ELISA and real-time PCR. Rats receiving TNBS and placebo pellets developed a severe colitis in the distal half of the colon. 5-ASA administered in the form of Pentasa pellets reduced macroscopic inflammation by only 5%. In contrast, the colon lesions were much less severe upon treatment with Nutriose:EC- and peas starch:EC-coated pellets: The macroscopic score was reduced by 25 and 24%, respectively. Decreases of 37 and 38% of the histological lesions confirmed the efficacy of these new colon targeting systems. Also, inflammatory markers (MPO, IL-1β mRNA, TNF mRNA) were significantly decreased in rats receiving Nutriose:EC- and peas starch:EC-coated pellets compared to Pentasa pellets. Furthermore, real-time PCR analysis indicated increased activation of the target receptor PPAR-γ and the HMGCS2 gene in rats upon administration of 5-ASA loaded Nutriose:EC- and peas starch:EC pellets compared to the commercial product. Also, HPLC-MS/MS analysis of plasma samples demonstrated that the level of the main metabolite of the drug (N-acetyl-5-ASA) was much lower upon administration of Nutriose:EC or peas starch:EC coated pellets compared to Pentasa pellets, indicating that undesired premature drug release in the upper gastrointestinal tract was more effectively hindered. In addition to the rat study, in vivo imaging of transgenic mice expressing the luciferase gene evidenced much more pronounced PPAR-γ activation upon 5-ASA administration in the form of Nutriose:EC-coated pellets versus Pentasa pellets. All these results clearly demonstrate the superiority of these microbiota-sensitive polysaccharide-based film coatings for colon targeting in vivo. © 2014 Elsevier B.V. All rights reserved. Source


Karrout Y.,University of Lille Nord de France | Karrout Y.,French Institute of Health and Medical Research | Neut C.,University of Lille Nord de France | Neut C.,French Institute of Health and Medical Research | And 12 more authors.
Journal of Applied Polymer Science | Year: 2011

Peas starch: ethylcellulose-based film coatings are proposed allowing for site-specific drug delivery to the colon of inflammatory bowel disease patients. The film coatings are poorly permeable for 5-aminosalicylic acid in media simulating the contents of the stomach and small intestine. Thus, they can minimize premature drug release in the upper gastrointestinal tract and subsequent absorption into the blood stream. However, once the colon is reached, drug release sets on and is time controlled. This can be attributed to the partial degradation of the peas starch by enzymes secreted by bacteria, which are preferentially present in the colon. Thus, the drug is released at the site of action, which is likely to minimize undesired side effects in the healthy part of the human body and to optimize the therapeutic efficacy of the treatment. A blend ratio of 1: 4 peas starch: ethylcellulose and a coating level of 15% (w/w) seem to be optimal for pellet coating. Importantly, the polymeric films can be expected to withstand the mechanical stress encountered in vivo because of the motility of the stomach and small intestine. Furthermore, the systems are long-term stable: drug release from coated pellets remains unaltered during 1-year open storage. © 2010 Wiley Periodicals, Inc. Source


Hidalgo-Lucas S.,ETAP Laboratory | Rozan P.,ETAP Laboratory | Guerin-Deremaux L.,ROQUETTE | Baert B.,ROQUETTE | And 3 more authors.
Journal of Medicinal Food | Year: 2016

Chlorella sp. is a green microalgae containing nutrients, vitamins, minerals, and chlorophyll. In some communities, Chlorella sp. is a traditional medicinal plant used for the management of inflammation-related diseases. In a rat model, ROQUETTE Chlorella sp. (RCs) benefits were investigated on visceral pain and associated inflammatory parameters related to cystitis both induced by cyclophosphamide (CYP). RCs was orally administered every day from day 1-16 (250 and 500 mg/kg body weight). Six hours after an intraperitoneal injection of 200 mg/kg body weight of CYP, body temperature, general behavior, food intake, and body weight were recorded. Twenty-four hours after CYP injection, rats were tested in two behavioral tests, an open field and the aversive light stimulus avoidance conditioning test, to evaluate the influence of pain on general activity and learning ability of rats. After euthanasia, bladders were weighed, their thickness was scored, and the urinary hemoglobin was measured. RCs orally administered at the two dosages significantly reduced visceral pain and associated inflammatory parameters related to cystitis both induced by CYP injection, and improved rat behavior. To conclude, RCs demonstrated beneficial effects against visceral pain and cystitis. © Copyright 2016, Mary Ann Liebert, Inc. and Korean Society of Food Science and Nutrition 2016. Source


Schnebelen-Berthier C.,Institute Pasteur Of Lille | Acar N.,French National Center for Scientific Research | Acar N.,French National Institute for Agricultural Research | Acar N.,University of Burgundy | And 12 more authors.
International Journal of Food Sciences and Nutrition | Year: 2015

Lutein and docosahexaenoic acid (DHA) are associated with the prevention of age-related macular degeneration (AMD). Since microalgae are potent natural sources of these nutrients, their nutritional value should be evaluated based on the bioavailability of lutein and DHA for the retina via the plasmatic compartment. In this study, quail were fed for 5 months either with a diet supplemented or deprived with microalgae rich in lutein and DHA. In the microalgae-fed group, the retinal concentrations of lutein and zeaxanthin gradually increased whereas in plasma, these compounds started to increase from the first month of supplementation. We also observed a significant increase in retinal and plasmatic levels of DHA in the microalgae-fed group. In conclusion, the plasmatic and retinal contents of lutein and DHA were significantly increased in quail fed with lutein- and DHA-rich microalgae. Food fortification with microalgae may be an innovative way to increase lutein and DHA consumption in humans. © 2015 Informa UK Ltd. Source

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