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1. Optimization of Solid Lipid Nanoparticle Formulation for Cosmetic Application Using Design of Experiments, PART II: Physical Characterization and In Vitro Skin Permeation for Sesamol Skin Delivery.

Author

Cassayre, Margot, Oline, Auriane, Orneto, Caroline, Wafo, Emmanuel, Abou, Lydia, Altié, Alexandre, Claeys-Bruno, Magalie, Sauzet, Christophe, and Piccerelle, Philippe

Subjects
NANOPARTICLES, EXPERIMENTAL design, HAIR follicles, LIPIDS, ZETA potential
Abstract

Our research focuses on evaluating the preliminary stability of solid lipid nanoparticles (SLNs) in order to identify an optimal formulation for studying the skin penetration of SLNs loaded with sesamol, with a view to developing potential cosmetic applications. For this study, SLNs were prepared with varying lipid and surfactant compositions and produced through homogenization and ultrasonication. The particle size (PS), polydispersity index (PDI), zeta potential (ZP), and encapsulation efficiency (EE) were analyzed for the different formulations. We identified OP2Se as the optimal formulation for skin penetration assessment due to its stable PS, PDI, ZP, and EE over time, with a Turbiscan Stability Index (TSI) below 1 after a month, indicating favorable stability conditions. The in vitro skin permeation study compared sesamol-loaded SLNs with a control sesamol hydrogel, revealing controlled release characteristics ideal for localized skin effects without significant bloodstream penetration, attributed to the SLNs' 200 nm particle size. Further exploration could enhance skin retention and targeting, potentially extending penetration studies and reducing particle size to improve accumulation in hair follicles. Exploring SLN applications beyond sesamol, such as incorporating mineral filters for suncare, offers promising avenues, underscoring SLNs' versatility in cosmetic formulations and skincare applications. [ABSTRACT FROM AUTHOR]

Published
2024
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5. Chimie, dermo-cosmétique et beauté

Author

Patrice André, Jean-Marie Aubry, Sabine Berteina-Raboin, Claire Bouix-Peter, Sandra Del Bino, Philippe Humbert, Jacques Leclaire, Laurent Marrot, Christophe Masson, Isabelle Pélisson, Philippe Piccerelle, Philippe Walter and Patrice André, Jean-Marie Aubry, Sabine Berteina-Raboin, Claire Bouix-Peter, Sandra Del Bino, Philippe Humbert, Jacques Leclaire, Laurent Marrot, Christophe Masson, Isabelle Pélisson, Philippe Piccerelle, Philippe Walter

Published
2017

7. Lignosulfonate is an efficient SPF booster: Application to eco-friendly sunscreen formulations

Author

Lorquin, Faustine, Lorquin, Jean, Claeys-Bruno, Magalie, Rollet, Marion, Robin, Maxime, Di Giorgio, Carole, Piccerelle, Philippe, Institut méditerranéen de biodiversité et d'écologie marine et continentale (IMBE), Centre National de la Recherche Scientifique (CNRS)-Institut de recherche pour le développement [IRD] : UMR237-Aix Marseille Université (AMU)-Avignon Université (AU), Aix Marseille Université (AMU), Institut méditerranéen d'océanologie (MIO), Institut de Recherche pour le Développement (IRD)-Aix Marseille Université (AMU)-Institut national des sciences de l'Univers (INSU - CNRS)-Université de Toulon (UTLN)-Centre National de la Recherche Scientifique (CNRS), Avignon Université (AU)-Aix Marseille Université (AMU)-Institut de recherche pour le développement [IRD] : UMR237-Centre National de la Recherche Scientifique (CNRS), and Institut de Recherche pour le Développement (IRD)-Aix Marseille Université (AMU)-Institut national des sciences de l'Univers (INSU - CNRS)-Centre National de la Recherche Scientifique (CNRS)-Université de Toulon (UTLN)

Subjects
[SDV]Life Sciences [q-bio], [SDU.ENVI]Sciences of the Universe [physics]/Continental interfaces, environment, ComputingMilieux_MISCELLANEOUS
Abstract

International audience

Published
2021

8. Efficacy of a Biorevitalizing-Filler Solution on All Skin Aspects: 10 Years Approach through in Vitro Studies and Clinical Trials

Author

Robin, Sophie, Fanian, Férial, Courderot-Masuyer, Carol, Tordjman, Michel, Braccini, Frederic, Boisnic, Sylvie, Philippon, Valérie, Vincent, Anne Grand, Salomon, Catherine, Manfait, Michel, Humbert, Philippe, Piccerelle, Philippe, Bioexigence SAS, Besançon, France, Laboratoires Fill-Med, Paris, France, Aesthetic Doctor, Paris, France, Aesthetic Surgeon, Nice, France, Gredeco SARL, Paris, France, Laboratoires Multaler, Argenteuil, France, Reims University, Pharmaceutical Faculty, Reims, France, Université Bourgogne Franche-Comté [COMUE] (UBFC), Institut méditerranéen de biodiversité et d'écologie marine et continentale (IMBE), Avignon Université (AU)-Aix Marseille Université (AMU)-Institut de recherche pour le développement [IRD] : UMR237-Centre National de la Recherche Scientifique (CNRS), and University of Bourgogne-Franche Comté, Besançon, France

Subjects
Skin Biorevitalization, Skin Booster, Mesotherapy, [SDV]Life Sciences [q-bio], Skin Rejuvenation, Hyaluronic Acid, NCTF 135HA 
Abstract

International audience; Introduction: Skin aging is the result of many cellular dysfunctions over time particularly the fibroblasts and the keratinocytes. These dysfunctions could be decelerated by the preventive effects of some skin treatments such as Intradermal injections. NCTF 135HA  has a polycomponent formulation designed to improve the efficacy of non-cross linked hyaluronic acid (as a micro-filler) on fibroblasts function. Although NCTF 135HA has been used by aesthetic practitioners since 20 years, we have analyzed all in vitro, ex vivo and in vivo studies during past 10 years in order to summarized its anti-aging

Published
2021

11. Efficacy of a Biorevitalizing-Filler Solution on All Skin Aspects: 10 Years Approach through <i>in Vitro</i> Studies and Clinical Trials

Author

Robin, Sophie, primary, Fanian, Férial, additional, Courderot-Masuyer, Carol, additional, Tordjman, Michel, additional, Braccini, Frederic, additional, Boisnic, Sylvie, additional, Philippon, Valérie, additional, Vincent, Anne Grand, additional, Salomon, Catherine, additional, Manfait, Michel, additional, Humbert, Philippe, additional, and Piccerelle, Philippe, additional

Published
2021
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13. Synthesis and Evaluation of the Antibacterial Activities of 13-Substituted Berberine Derivatives

Author

Olleik, Hamza, primary, Yacoub, Taher, additional, Hoffer, Laurent, additional, Gnansounou, Senankpon Martial, additional, Benhaiem-Henry, Kehna, additional, Nicoletti, Cendrine, additional, Mekhalfi, Malika, additional, Pique, Valérie, additional, Perrier, Josette, additional, Hijazi, Akram, additional, Baydoun, Elias, additional, Raymond, Josette, additional, Piccerelle, Philippe, additional, Maresca, Marc, additional, and Robin, Maxime, additional

Published
2020
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14. GC-MS screening and evaluation of the anti-inflammatory and antioxidant activities of ethanolic leaves and stem barks extracts from Dialium guineense Willd, Parkia biglobosa (Jacq.) R. Br. ex Benth. and Tamarindus indica L

Author

Gnansounou, Senankpon, Iskandar, Samy, Abou, Lydia, Robin, Maxime, Di Giorgio, Carole, Dahouenon, Edwige, Piccerelle, Philippe, Sonhounhloue, Dominique, GNANSOUNOU, Martial Senankpon, University of Abomey Calavi (UAC), Aix-Marseille Université - Faculté de pharmacie (AMU PHARM), Aix Marseille Université (AMU), Institut méditerranéen de biodiversité et d'écologie marine et continentale (IMBE), Centre National de la Recherche Scientifique (CNRS)-Institut de recherche pour le développement [IRD] : UMR237-Aix Marseille Université (AMU)-Avignon Université (AU), Centre recherche en CardioVasculaire et Nutrition (C2VN), Institut National de la Recherche Agronomique (INRA)-Aix Marseille Université (AMU)-Institut National de la Santé et de la Recherche Médicale (INSERM), Université d’Abomey-Calavi = University of Abomey Calavi (UAC), Avignon Université (AU)-Aix Marseille Université (AMU)-Institut de recherche pour le développement [IRD] : UMR237-Centre National de la Recherche Scientifique (CNRS), and Centre recherche en CardioVasculaire et Nutrition = Center for CardioVascular and Nutrition research (C2VN)

Subjects
ethanolic extracts, stigmasterol, antioxidant, lupeol, sitosterol, [CHIM.THER] Chemical Sciences/Medicinal Chemistry, [CHIM.THER]Chemical Sciences/Medicinal Chemistry, GC-MS, complex mixtures, anti-inflammatory
Abstract

International audience; Inflammation has been shown to be greatly involved in the degenerative processes of human skin such as photo aging and atopy. Reduction of low-grade inflammatory reactions by topical products may be necessary in case of skin aggression, to obtain an optimal wound healing and restore the physiological balance of human skin. Present work evaluated the antioxidant, anti-inflammatory and phototoxic properties of ethanolic extracts from leaves and stem barks of Dialium guineense Willd., Parkia biglobosa (Jacq.) R. Br. Ex Benth. and Tamarindus indica L. The antioxidant power of the extracts, measured in vitro by the KRL method, showed that each gram of D. guineense bark extract, P. biglobosa leaves extract and T. indica bark and leaves extracts has an antioxidant capacity equivalent to 1585, 2092, 5071 and 2246 mg of Trolox respectively. Simultaneously with their actions on cell viability, the anti-inflammatory activity of the extracts was monitored measuring their effects on NO production by mouse macrophages submitted to LPS from E. coli to determine the anti-inflammatory ratio of each extract. The bark and leaves of D. guineense Willd., the leaves of P. biglobosa (Jacq.) R. Br. Ex Benth. and the bark of T. indica L. have anti-inflammatory ratios from 161 to 458.2, whereas Dexamethasone (positive control) has a ratio of 37.87. The in vitro 3T3 NRU test was used on mouse fibroblasts to determine the phototoxicity of the six extracts. Only D. guineense Willd. stem bark was photo-toxic with a photo-irritation factor greater than 5 (PIF = 8.39). Our study report some molecules such as lupeol, amaryn, sitosterol for the first time in the extracts and shows that the use of these plants in traditional medicine is justified.

Published
2019

15. Antioxidant, Anti-inflammatory and Neuroprotective Activities of a Plant Extract Derived from Traditional Chinese Medicine SuHeXiang Wan (AT000)

Author

Iskandar, Samy, Gnansounou, Senankpon, Robin, Maxime, Lorquin, Jean, Di Giorgio, Carole, Piccerelle, Philippe, Aix-Marseille Université - Faculté de pharmacie (AMU PHARM), Aix Marseille Université (AMU), Université d’Abomey-Calavi = University of Abomey Calavi (UAC), Biomécanique et Bioingénierie (BMBI), Université de Technologie de Compiègne (UTC)-Centre National de la Recherche Scientifique (CNRS), Institut méditerranéen d'océanologie (MIO), Institut de Recherche pour le Développement (IRD)-Aix Marseille Université (AMU)-Institut national des sciences de l'Univers (INSU - CNRS)-Université de Toulon (UTLN)-Centre National de la Recherche Scientifique (CNRS), Institut méditerranéen de biodiversité et d'écologie marine et continentale (IMBE), Avignon Université (AU)-Aix Marseille Université (AMU)-Institut de recherche pour le développement [IRD] : UMR237-Centre National de la Recherche Scientifique (CNRS), Faculté de Pharmacie, and University of Abomey Calavi (UAC)

Subjects
Inflammation, SuHeXiang Wan, Traditional Chinese medicine, Oxidative stress, [SCCO.NEUR]Cognitive science/Neuroscience, Amyloid beta, Alzheimer's disease, AT000
Abstract

International audience; In this paper, we present SuHeXiang Wan, a medicine used in traditional Chinese medicine for the treatment of epilepsy and convulsions. We investigated the antioxidant, anti-inflammatory and neuroprotective activities of the same treatment designated as AT000. The synergy of the two plants, Dryobalanops aromatica and Saussurea lappa, of which the use in alimentary supplements is considered controversial, was evaluated for the first time. The antioxidant activity of the extract was assessed by DPPH and ORAC tests while the anti-inflammatory activity was determined by measuring the capacity of macrophages to generate a strong inflammatory response when stimulated with antigens, inducing NO release. The extract efficacy on the attenuation of the Aβ25-35-induced learning deficits (spatial working memory: spontaneous alternation in the Y-maze and contextual long-term memory: passive avoidance test) was evaluated in vivo in mice seven days after the peptide administration. The impact on lipid peroxidation in the hippocampus, an index of oxidative Chemistry of Advanced Materials (CAM) Journal homepage: http://issrpublishing.com/cam/ Iskandar et al., Chemistry of Advanced Materials 3(2) (2018) 36-59 37 stress, was also evaluated. AT000 extract showed a strong antioxidant activity at 2 mg/mL, 10 mg/mL and 301774 Trolox equivalents according to the DPPH and ORAC tests respectively. The 21-days AT000 treatment dose-dependently alleviated Aβ25-35-induced deficits, with significant prevention at the highest dose tested (250 mg/Kg/day) on the spontaneous alternation, step-through latency and escape latency parameter. 21-days AT000 treatment dose-dependently attenuated also Aβ25-35-induced increase lipid peroxidation, with a significant and complete blockade at the highest doses tested. Synergistic experiments showed that the presence of Dryobalanops aromatica and Saussurea lappa is crucial to obtain a neuroprotective effect. According to these results, AT000 could be a candidate compound in the development of therapeutic drugs for the prevention and treatment of Alzheimer's disease.

Published
2018

16. In Vitro Cocktail Effects of PCB-DL (PCB118) and Bulky PCB (PCB153) with BaP on Adipogenesis and on Expression of Genes Involved in the Establishment of a Pro-Inflammatory State

Author

May, Phealay, Bremond, Patricia, Sauzet, Christophe, Piccerelle, Philippe, Grimaldi, Frédérique, Champion, Serge, Villard, Pierre-Henri, Institut méditerranéen de biodiversité et d'écologie marine et continentale (IMBE), Avignon Université (AU)-Aix Marseille Université (AMU)-Institut de recherche pour le développement [IRD] : UMR237-Centre National de la Recherche Scientifique (CNRS), Laboratoire de Galénique, Université de la Méditerranée - Aix-Marseille 2, Aix Marseille Université (AMU), Nutrition humaine et lipides : Biodisponibilité, métabolisme et régulation, Université de la Méditerranée - Aix-Marseille 2-Institut National de la Recherche Agronomique (INRA)-Université de Provence - Aix-Marseille 1-IFR125-Institut National de la Santé et de la Recherche Médicale (INSERM), Villard, Pierre-Henri, and Centre National de la Recherche Scientifique (CNRS)-Institut de recherche pour le développement [IRD] : UMR237-Aix Marseille Université (AMU)-Avignon Université (AU)

Subjects
Leptin, animal structures, adipocytes, polycyclic aromatic hydrocarbons, Down-Regulation, Response Elements, Article, adipogenesis, lcsh:Chemistry, Mice, polychlorobiphenyls (PCB), [SDV.BBM.GTP]Life Sciences [q-bio]/Biochemistry, Molecular Biology/Genomics [q-bio.GN], polycyclic compounds, Animals, lcsh:QH301-705.5, Glucose Transporter Type 4, Drug Synergism, 3T3 Cells, Polychlorinated Biphenyls, PPAR gamma, [SDV.TOX] Life Sciences [q-bio]/Toxicology, lcsh:Biology (General), lcsh:QD1-999, inflammation, [SDV.TOX]Life Sciences [q-bio]/Toxicology, Ah receptor, cocktail effect, Cytokines, [SDV.BBM.GTP] Life Sciences [q-bio]/Biochemistry, Molecular Biology/Genomics [q-bio.GN], Environmental Pollutants, benzo(a)pyrene, Drug Antagonism
Abstract

International audience; Objective: Highlight the in vitro effects of 3T3-L1 cell exposure to polychlorinated biphenyls (PCB118 and 153) or benzo(a)pyrene (BaP) alone or as a cocktail on adipogenesis (ADG) by focusing on changes in lipid metabolism and inflammatory-related genes expression (INFG) and ADG-related genes expression (ADGG).Results: Treatment from the early stage of cell differentiation by BaP alone or in combination with PCBs decreased the expression of some of the ADGG (PPARγ Glut-4, FAS, Lipin-1a, Leptin, and Adiponectin). BaP enhanced the INFG, especially MCP-1 and TNFα. Co-exposure to BaP and PCB153 showed a synergistic effect on TNFα and IL6 expression. Treatment with BaP and PCBs during only the maturation period up-regulated the INFG (IL6, TNFα, CXCL-10 & MCP-1). PCB118 alone also enhanced TNFα, CXCL-10, and PAI-1 expression. The change in MCP-1 protein expression was in agreement with that of the gene. Finally, the BaP-induced up-regulation of the xenobiotic responsive element (XRE)-controlled luciferase activity was impaired by PCB153 but not by PCB118.Conclusion: BaP and PCBs down-regulate a part of ADGG and enhance INFG. The direct regulatory effect of PCBs on both ADGG and INFG is usually rather lower than that of BaP and synergistic or antagonistic cocktail effects are clearly observed.

Published
2018

18. Thermodynamic study of the interaction between calcium and zoledronic acid by calorimetry

Author

Piccerelle, Philippe, Cau, Pierre, Lévy, Nicolas, Gallice, Philippe, Bergé-Lefranc, David, Larbi, Mohamed A. Mostefa Side, Sauzet, Christophe, Mostefa, Mohamed, Larbi, Side, Institut méditerranéen de biodiversité et d'écologie marine et continentale (IMBE), Centre National de la Recherche Scientifique (CNRS)-Institut de recherche pour le développement [IRD] : UMR237-Aix Marseille Université (AMU)-Avignon Université (AU), Génétique Médicale et Génomique Fonctionnelle (GMGF), Aix Marseille Université (AMU)-Assistance Publique - Hôpitaux de Marseille (APHM)- Hôpital de la Timone [CHU - APHM] (TIMONE)-Institut National de la Santé et de la Recherche Médicale (INSERM)-Centre National de la Recherche Scientifique (CNRS), Département de génétique médicale [Hôpital de la Timone - APHM], Institut National de la Santé et de la Recherche Médicale (INSERM)- Hôpital de la Timone [CHU - APHM] (TIMONE)-Assistance Publique - Hôpitaux de Marseille (APHM)-Aix Marseille Université (AMU), Avignon Université (AU)-Aix Marseille Université (AMU)-Institut de recherche pour le développement [IRD] : UMR237-Centre National de la Recherche Scientifique (CNRS), Aix Marseille Université (AMU)-Assistance Publique - Hôpitaux de Marseille (APHM)- Hôpital de la Timone [CHU - APHM] (TIMONE)-Institut National de la Santé et de la Recherche Médicale (INSERM), and Institut National de la Santé et de la Recherche Médicale (INSERM)-Aix Marseille Université (AMU)-Assistance Publique - Hôpitaux de Marseille (APHM)- Hôpital de la Timone [CHU - APHM] (TIMONE)-Centre National de la Recherche Scientifique (CNRS)

Subjects
0301 basic medicine, Chemistry, chemistry.chemical_element, Ionic bonding, Isothermal titration calorimetry, Calorimetry, Calcium, 010402 general chemistry, 01 natural sciences, Binding constant, Atomic and Molecular Physics, and Optics, 0104 chemical sciences, 03 medical and health sciences, 030104 developmental biology, Biochemistry, Biophysics, Molecule, General Materials Science, Physical and Theoretical Chemistry, [SDE.BE]Environmental Sciences/Biodiversity and Ecology, Mode of action, Calcium disorder
Abstract

International audience; Bisphosphonates (BPs) are widely used to treat calcium disorders because of their structural and functional similarities with the organic pyrophosphates present in plasma and urine. BPs are well known for their strong interactions with calcium, and they have been shown to bind to hydroxyapatite or bone; however, no model exists for studying in greater detail how BPs and particularly amino-bisphosphonates (N-BPs) such as zolendronate (Zol) bind to free calcium. The aim of this work was to determine the effect of pH on Ca2+/Zol complex formation using isothermal titration calorimetry (ITC) because these effects might have important implications for the future development of a solid dosage form. In this study, using a predictive model, we can observe, the existence of three Ca2+/Zol complexes. Knowledge of the binding constant for each complex is helpful for predicting the predominance of the different species at different Ca2+/Zol ratios. Binding is due to ionic interaction between Ca2+ and the negative charges formed by dissociated Zol as a function of the pKa. Ca2+ fixation induces a strong rearrangement of the surrounding water molecules and causes proton release or uptake. The pH-dependent affinity of calcium for each site based on the model used in this work is proposed in detail, which might facilitate the development of new bisphosphonates and enable further elucidation of their mode of action. (C) 2016 Elsevier Ltd. All rights reserved.

Published
2016

20. The Transcriptional Effects of PCB118 and PCB153 on the Liver, Adipose Tissue, Muscle and Colon of Mice: Highlighting of Glut4 and Lipin1 as Main Target Genes for PCB Induced Metabolic Disorders

Author

Mesnier, Aurélia, Champion, Serge, Louis, Laurence, Sauzet, Christophe, May, Phealay, Portugal, Henri, Benbrahim, Karim, Abraldes, Joelle, Alessi, Marie-Christine, Amiot-Carlin, Marie-Josephe, Peiretti, Franck, Piccerelle, Philippe, Nalbone, Gilles, Villard, Pierre-Henri, Institut méditerranéen de biodiversité et d'écologie marine et continentale ( IMBE ), Université d'Avignon et des Pays de Vaucluse ( UAPV ) -Aix Marseille Université ( AMU ) -Institut de recherche pour le développement [IRD] : UMR237-Centre National de la Recherche Scientifique ( CNRS ), Génétique Médicale et Génomique Fonctionnelle ( GMGF ), Aix Marseille Université ( AMU ) -Assistance Publique - Hôpitaux de Marseille ( APHM ) - Hôpital de la Timone [CHU - APHM] ( TIMONE ) -Institut National de la Santé et de la Recherche Médicale ( INSERM ) -Centre National de la Recherche Scientifique ( CNRS ), Nutrition, obésité et risque thrombotique ( NORT ), Institut National de la Recherche Agronomique ( INRA ) -Aix Marseille Université ( AMU ) -Institut National de la Santé et de la Recherche Médicale ( INSERM ), Institut méditerranéen de biodiversité et d'écologie marine et continentale (IMBE), Avignon Université (AU)-Aix Marseille Université (AMU)-Institut de recherche pour le développement [IRD] : UMR237-Centre National de la Recherche Scientifique (CNRS), Génétique Médicale et Génomique Fonctionnelle (GMGF), Aix Marseille Université (AMU)-Assistance Publique - Hôpitaux de Marseille (APHM)- Hôpital de la Timone [CHU - APHM] (TIMONE)-Institut National de la Santé et de la Recherche Médicale (INSERM)-Centre National de la Recherche Scientifique (CNRS), Laboratoire central, Hôpital Sainte-Marguerite [CHU - APHM] (Hôpitaux Sud ), Nutrition, obésité et risque thrombotique (NORT), Institut National de la Recherche Agronomique (INRA)-Aix Marseille Université (AMU)-Institut National de la Santé et de la Recherche Médicale (INSERM), Institut National de la Santé et de la Recherche Médicale (INSERM), Aix-Marseille Université - Faculté de pharmacie (AMU PHARM), Aix Marseille Université (AMU), Villard, Pierre-Henri, This work was supported by the PNRPE (Plan National de Recherche sur les Perturbateurs Endocriniens) from the 'Ministère de l'écologie, du développement durable et de l'énergie', Centre National de la Recherche Scientifique (CNRS)-Institut de recherche pour le développement [IRD] : UMR237-Aix Marseille Université (AMU)-Avignon Université (AU), Institut National de la Santé et de la Recherche Médicale (INSERM)-Aix Marseille Université (AMU)-Assistance Publique - Hôpitaux de Marseille (APHM)- Hôpital de la Timone [CHU - APHM] (TIMONE)-Centre National de la Recherche Scientifique (CNRS), and Aix Marseille Université (AMU)-Institut National de la Recherche Agronomique (INRA)-Institut National de la Santé et de la Recherche Médicale (INSERM)

Subjects
Blood Glucose, Male, EXPRESSION, Transcription, Genetic, Colon, Phosphatidate Phosphatase, lcsh:Medicine, Real-Time Polymerase Chain Reaction, Mice, Metabolic Diseases, [SDV.BBM.GTP]Life Sciences [q-bio]/Biochemistry, Molecular Biology/Genomics [q-bio.GN], POLYCHLORINATED-BIPHENYLS, [ SDV.MHEP ] Life Sciences [q-bio]/Human health and pathology, Animals, EXPOSURE, Muscle, Skeletal, lcsh:Science, Triglycerides, Oligonucleotide Array Sequence Analysis, [SDV.MHEP.EM] Life Sciences [q-bio]/Human health and pathology/Endocrinology and metabolism, LIPODYSTROPHY, [ SDV.BID ] Life Sciences [q-bio]/Biodiversity, INSULIN-RESISTANCE, Glucose Transporter Type 4, ADIPOCYTE DIFFERENTIATION, Dose-Response Relationship, Drug, [ SDV ] Life Sciences [q-bio], lcsh:R, DEATH, Nuclear Proteins, [SDV.MHEP.EM]Life Sciences [q-bio]/Human health and pathology/Endocrinology and metabolism, GAMMA, Polychlorinated Biphenyls, TRANSPORT, Mice, Inbred C57BL, [SDV.TOX] Life Sciences [q-bio]/Toxicology, Adipose Tissue, Liver, [SDV.TOX]Life Sciences [q-bio]/Toxicology, OBESITY, [SDV.BBM.GTP] Life Sciences [q-bio]/Biochemistry, Molecular Biology/Genomics [q-bio.GN], lcsh:Q, Research Article
Abstract

International audience; Epidemiological studies have associated environmental exposure to polychlorinated biphe-nyls (PCBs) with an increased risk of type 2 diabetes; however, little is known about the underlying mechanisms involved in the metabolic side-effects of PCB. Our study evaluated the transcriptional effects of a subchronic exposure (gavage at Day 0 and Day 15 with 10 or 100 μmol/Kg bw) to PCB118 (dioxin-like PCB), PCB153 (non-dioxin-like PCB), or an equi-molar mixture of PCB118 and PCB153 on various tissues (liver, visceral adipose tissue, muscle, and colon) in mice. Our results showed that a short-term exposure to PCB118 and/ or PCB153 enhanced circulating triglyceride levels but did not affect glycemia. Among the studied tissues, we did not observe any modification of the expression of inflammation-related genes, such as cytokines or chemokines. The main transcriptional effects were observed in visceral adipose and liver tissues. We found a downregulation of lipin1 and glut4 expression in these two target organs. In adipose tissue, we also showed a downregu-lation of Agpat2, Slc25a1, and Fasn. All of these genes are involved in lipid metabolism and insulin resistance. In muscles, we observed an induction of CnR1 and Foxo3 expression, which may be partly involved in PCB metabolic effects. In summary, our results suggest that lipin1 and glut4, notably in adipose tissue, are the main targeted genes in PCB-induced metabolic disorders, however, further studies are required to fully elucidate the mechanisms involved.

Published
2015

22. Innovations récentes en cosmétique anti-âge

Author

Cantecor, Bénédicte, Savelli, Marie-Pierre, Marti-Mestres, Gilberte, Bonniol, Vincent, Larbi, Mohamed A. Mostefa Side, Piccerelle, Philippe, Prenyl B SAS, Aix Marseille Université (AMU), Université de Montpellier (UM), Apprentissage, Didactique, Evaluation, Formation (ADEF), and Robert Chilcott, Keith R. Brain

Subjects
[SDV.BIO]Life Sciences [q-bio]/Biotechnology, [SDV.SP.PG]Life Sciences [q-bio]/Pharmaceutical sciences/Galenic pharmacology, [SDV.SPEE]Life Sciences [q-bio]/Santé publique et épidémiologie, [SDV.BC]Life Sciences [q-bio]/Cellular Biology, ComputingMilieux_MISCELLANEOUS
Abstract

International audience

Published
2013
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31. Self-assembled liquid crystalline nanoparticles as an ophthalmic drug delivery system. Part II: optimization of formulation variables using experimental design.

Author

Achouri, Djamila, Sergent, Michelle, Tonetto, Alain, Piccerelle, Philippe, Andrieu, Véronique, and Hornebecq, Virginie

Subjects
NANOMEDICINE, MOLECULAR self-assembly, LIQUID crystals, OPHTHALMIC drugs, DRUG delivery systems, EXPERIMENTAL design, EXCIPIENTS, KERATOCONUS, THERAPEUTICS
Abstract

In the field of keratoconus treatment, a lipid-based liquid crystal nanoparticles system has been developed to improve the preocular retention and ocular bioavailability of riboflavin, a water-soluble drug. The formulation of this ophthalmic drug delivery system was optimized by a simplex lattice experimental design. The delivery system is composed of three main components that are mono acyl glycerol (monoolein), poloxamer 407 and water and two secondary components that are riboflavin and glycerol (added to adjust the osmotic pressure). The amounts of these three main components were selected as the factors to systematically optimize the dependent variables that are the encapsulation efficiency and the particle size. In this way, 12 formulas describing experimental domain of interest were prepared. Results obtained using small angle X-rays scattering (SAXS) and cryo-transmission electron microscopy (cryo-TEM) evidenced the presence of nano-objects with either sponge or hexagonal inverted structure. In the zone of interest, the percentage of each component was determined to obtain both high encapsulation efficiency and small size of particles. Two optimized formulations were found: F7 and F1. They are very close in the ternary phase diagram as they contain 6.83% of poloxamer 407; 44.18% and 42.03% of monoolein; 46.29% and 48.44% of water for F7 and F11, respectively. These formulations displayed a good compromise between inputs and outputs investigated. [ABSTRACT FROM AUTHOR]

Published
2015
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32. Self-assembled liquid crystalline nanoparticles as an ophthalmic drug delivery system. Part I: influence of process parameters on their preparation studied by experimental design.

Author

Achouri, Djamila, Hornebecq, Virginie, Piccerelle, Philippe, Andrieu, Véronique, and Sergent, Michelle

Subjects
OPHTHALMIC drugs, DRUG delivery systems, EXPERIMENTAL design, LIQUID crystals, NANOPARTICLES, KERATOCONUS, ENCAPSULATION (Catalysis), THERAPEUTICS
Abstract

To develop self-assembled liquid crystalline nanoparticles as a drug delivery system for keratoconus treatment, a formulation containing riboflavin a water-soluble drug, two surfactants (poloxamer 407 and mono acyl glycerol - monoolein-) and water was optimized and prepared by emulsification and a homogenization process. A fractional factorial design was applied to estimate the main effects and interaction effects of five parameters on two responses, namely particle size and encapsulation efficiency. The five parameters are the temperature of the two phases, the duration of emulsification, the presence of heating during homogenization, the number of passes and pressure. The most influent parameters are the presence of heating during the homogenization and the pressure that led to the production of nanoparticles with an average size of 145 nm and an average encapsulation efficiency of 46%. [ABSTRACT FROM AUTHOR]

Published
2015
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33. Recent advances in ocular drug delivery.

Author

Achouri, Djamila, Alhanout, Kamel, Piccerelle, Philippe, and Andrieu, Véronique

Subjects
DRUG delivery systems, OCULAR pharmacology, PRODUCT elimination, PHARMACEUTICAL chemistry, DRUG development, BIOAVAILABILITY, COLLOIDS in medicine
Abstract

Amongst the various routes of drug delivery, the field of ocular drug delivery is one of the most interesting and challenging endeavors facing the pharmaceutical scientist. Recent research has focused on the characteristic advantages and limitations of the various drug delivery systems, and further research will be required before the ideal system can be developed. Administration of drugs to the ocular region with conventional delivery systems leads to short contact time of the formulations on the epithelium and fast elimination of drugs. This transient residence time involves poor bioavailability of drugs which can be explained by the tear production, non-productive absorption and impermeability of corneal epithelium. Anatomy of the eye is shortly presented and is connected with ophthalmic delivery and bioavailability of drugs. In the present update on ocular dosage forms, chemical delivery systems such as prodrugs, the use of cyclodextrins to increase solubility of various drugs, the concept of penetration enhancers and other ocular drug delivery systems such as polymeric gels, bioadhesive hydrogels, in-situ forming gels with temperature-, pH-, or osmotically induced gelation, combination of polymers and colloidal systems such as liposomes, niosomes, cubosomes, microemulsions, nanoemulsions and nanoparticles are discussed. Novel ophthalmic delivery systems propose the use of many excipients to increase the viscosity or the bioadhesion of the product. New formulations like gels or colloidal systems have been tested with numerous active substances by in vitro and in vivo studies. Sustained drug release and increase in drug bioavailability have been obtained, offering the promise of innovation in drug delivery systems for ocular administration. Combining different properties of pharmaceutical formulations appears to offer a genuine synergy in bioavailability and sustained release. Promising results are obtained with colloidal systems which present very comfortable conditions of use and prolonged action. [ABSTRACT FROM AUTHOR]

Published
2013
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34. In Vitro Cocktail Effects of PCB-DL (PCB118) and Bulky PCB (PCB153) with BaP on Adipogenesis and on Expression of Genes Involved in the Establishment of a Pro-Inflammatory State.

Author

May P, Bremond P, Sauzet C, Piccerelle P, Grimaldi F, Champion S, and Villard PH

Subjects
3T3 Cells, Animals, Cytokines genetics, Down-Regulation, Drug Antagonism, Drug Synergism, Glucose Transporter Type 4 genetics, Glucose Transporter Type 4 metabolism, Inflammation metabolism, Leptin genetics, Leptin metabolism, Mice, PPAR gamma genetics, PPAR gamma metabolism, Response Elements, Adipogenesis drug effects, Benzo(a)pyrene pharmacology, Cytokines metabolism, Environmental Pollutants pharmacology, Polychlorinated Biphenyls pharmacology
Abstract

(1) Objective: Highlight the in vitro effects of 3T3-L1 cell exposure to polychlorinated biphenyls (PCB118 and 153) or benzo(a)pyrene (BaP) alone or as a cocktail on adipogenesis (ADG) by focusing on changes in lipid metabolism and inflammatory-related genes expression (INFG) and ADG-related genes expression (ADGG); (2) Results: Treatment from the early stage of cell differentiation by BaP alone or in combination with PCBs decreased the expression of some of the ADGG ( PPARγ Glut-4 , FAS , Lipin-1a , Leptin , and Adiponectin ). BaP enhanced the INFG, especially MCP-1 and TNFα . Co-exposure to BaP and PCB153 showed a synergistic effect on TNFα and IL6 expression. Treatment with BaP and PCBs during only the maturation period up-regulated the INFG ( IL6 , TNFα , CXCL-10 & MCP-1 ). PCB118 alone also enhanced TNFα , CXCL-10 , and PAI-1 expression. The change in MCP-1 protein expression was in agreement with that of the gene. Finally, the BaP-induced up-regulation of the xenobiotic responsive element (XRE)-controlled luciferase activity was impaired by PCB153 but not by PCB118; (3) Conclusion: BaP and PCBs down-regulate a part of ADGG and enhance INFG. The direct regulatory effect of PCBs on both ADGG and INFG is usually rather lower than that of BaP and synergistic or antagonistic cocktail effects are clearly observed., Competing Interests: The authors declare no conflict of interest. The founding sponsors (PNRPE) had no role in the design of the study; in the collection, analyses, or interpretation of data; in the writing of the manuscript, and in the decision to publish the results.

Published
2018
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35. The Transcriptional Effects of PCB118 and PCB153 on the Liver, Adipose Tissue, Muscle and Colon of Mice: Highlighting of Glut4 and Lipin1 as Main Target Genes for PCB Induced Metabolic Disorders.

Author

Mesnier A, Champion S, Louis L, Sauzet C, May P, Portugal H, Benbrahim K, Abraldes J, Alessi MC, Amiot-Carlin MJ, Peiretti F, Piccerelle P, Nalbone G, and Villard PH

Subjects
Adipose Tissue metabolism, Animals, Blood Glucose drug effects, Colon metabolism, Dose-Response Relationship, Drug, Liver metabolism, Male, Mice, Mice, Inbred C57BL, Muscle, Skeletal metabolism, Oligonucleotide Array Sequence Analysis, Real-Time Polymerase Chain Reaction, Transcription, Genetic drug effects, Triglycerides blood, Adipose Tissue drug effects, Colon drug effects, Glucose Transporter Type 4 drug effects, Liver drug effects, Metabolic Diseases chemically induced, Muscle, Skeletal drug effects, Nuclear Proteins drug effects, Phosphatidate Phosphatase drug effects, Polychlorinated Biphenyls adverse effects
Abstract

Epidemiological studies have associated environmental exposure to polychlorinated biphenyls (PCBs) with an increased risk of type 2 diabetes; however, little is known about the underlying mechanisms involved in the metabolic side-effects of PCB. Our study evaluated the transcriptional effects of a subchronic exposure (gavage at Day 0 and Day 15 with 10 or 100 μmol/Kg bw) to PCB118 (dioxin-like PCB), PCB153 (non-dioxin-like PCB), or an equimolar mixture of PCB118 and PCB153 on various tissues (liver, visceral adipose tissue, muscle, and colon) in mice. Our results showed that a short-term exposure to PCB118 and/or PCB153 enhanced circulating triglyceride levels but did not affect glycemia. Among the studied tissues, we did not observe any modification of the expression of inflammation-related genes, such as cytokines or chemokines. The main transcriptional effects were observed in visceral adipose and liver tissues. We found a downregulation of lipin1 and glut4 expression in these two target organs. In adipose tissue, we also showed a downregulation of Agpat2, Slc25a1, and Fasn. All of these genes are involved in lipid metabolism and insulin resistance. In muscles, we observed an induction of CnR1 and Foxo3 expression, which may be partly involved in PCB metabolic effects. In summary, our results suggest that lipin1 and glut4, notably in adipose tissue, are the main targeted genes in PCB-induced metabolic disorders, however, further studies are required to fully elucidate the mechanisms involved.

Published
2015
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