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1. Chitosan nanoparticles/cellulose nanocrystals nanocomposites as a carrier system for the controlled release of repaglinide.

Author

Abo-Elseoud WS, Hassan ML, Sabaa MW, Basha M, Hassan EA, and Fadel SM

Subjects
Carbamates therapeutic use, Cellulose chemistry, Cellulose therapeutic use, Chitosan therapeutic use, Delayed-Action Preparations chemistry, Delayed-Action Preparations therapeutic use, Drug Carriers chemistry, Drug Carriers therapeutic use, Drug Delivery Systems, Drug Liberation, Humans, Hydrolysis, Nanocomposites chemistry, Nanocomposites therapeutic use, Nanoparticles therapeutic use, Piperidines therapeutic use, Spectroscopy, Fourier Transform Infrared, Carbamates chemistry, Chitosan chemistry, Hyperglycemia drug therapy, Nanoparticles chemistry, Piperidines chemistry
Abstract

The aim of the present work was to study the use of cellulose nanocrystals (CNC) and chitosan nanoparticles (CHNP) for developing controlled-release drug delivery system of the anti-hyperglycemic drug Repaglinide (RPG). CNC was isolated from palm fruit stalks by sulfuric acid hydrolysis; the dimensions of the isolated nanocrystals were 86-237 nm in length and 5-7 nm in width. Simple and economic method was used for the fabrication of controlled release drug delivery system from CNC and CHNP loaded with RPG drug via ionic gelation of chitosan in the presence of CNC and RPG. The prepared systems showed high drug encapsulation efficiency of about ~98%. Chemical modification of CNC by oxidation to introduce carboxylic groups on their surface (OXCNC) was also carried out for further controlling of RPG release. Particles size analysis showed that the average size of CHNP was about 197 nm while CHNP/CNC/RPG or CHNP/OXCNC/RPG nanoparticles showed average size of 215-310 nm. Compatibility studies by Fourier transform infrared (FTIR) spectroscopy showed no chemical reaction between RPG and the system's components used. By studying the drug release kinetic, all the prepared RPG formulations followed Higuchi model, indicating that the drug released by diffusion through the nanoparticles polymeric matrix., (Copyright © 2018 Elsevier B.V. All rights reserved.)

Published
2018
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2. Evaluation of anti-diabetic and anti-tumoral activities of bioactive compounds from Phoenix dactylifera L's leaf: In vitro and in vivo approach

Author

Mohamed Bouaziz, Mohamed Makni, Naziha Marrakchi, Bassem Khemakhem, M Chakroun, Hazem Ben Mabrouk, Noureddine Drira, Hanen El Abed, Hafedh Mejdoub, Faculté des Sciences de Sfax, Université de Sfax - University of Sfax, University of Gabes, Laboratoire des Venins et Biomolécules Thérapeutiques - Laboratory of Venoms and Therapeutic Biomolecules (LR11IPT08), Institut Pasteur de Tunis, Réseau International des Instituts Pasteur (RIIP)-Réseau International des Instituts Pasteur (RIIP), École Nationale d'Ingénieurs de Sfax | National School of Engineers of Sfax (ENIS), and The major part of this work was accomplished at the Faculty of Sciences of Sfax. The authors would like to thank Prof. Monique Simmonds from Jodrell Laboratory, Kew Gardens UK, for her help with LC–MS/MS analysis. Special thanks are also go to Pr. Hafedh Bejaoui, from the English department at the Faculty of Science of Sfax and to Sana Chakroun (Rudolf-Bultmann Str. 4. 35039 Marburg) for carefully proofreading and polishing the language of the present paper, to Zaineb Kammoun (Sfax Faculty of Science) for her invaluable assistance in this project.

Subjects
0301 basic medicine, Male, MESH: Polyphenols/pharmacology, MESH: Plant Extracts/pharmacology, [SDV]Life Sciences [q-bio], Flavonoid, Phytochemicals, Pharmacology, MESH: Hyperglycemia/complications, MESH: Plant Leaves/chemistry, Mice, Oral administration, Tandem Mass Spectrometry, inhibitors, MESH: Hypoglycemic Agents/pharmacology, MESH: Phytochemicals/pharmacology, MESH: Animals, α-Glucosidase and α-Amylase, Acarbose, chemistry.chemical_classification, Cell Death, MESH: Antineoplastic Agents/pharmacology, MESH: Polyphenols/therapeutic use, Phoeniceae, 04 agricultural and veterinary sciences, General Medicine, MESH: Hyperglycemia/drug therapy, Postprandial Period, 040401 food science, Postprandial, Biochemistry, MESH: Phytotherapy, MESH: Hypoglycemic Agents/therapeutic use, MESH: Postprandial Period, MESH: Antineoplastic Agents/therapeutic use, medicine.drug, LC–MS/MS analysis, MESH: Phoeniceae/chemistry, MESH: Cell Line, Tumor, MESH: Phytochemicals/therapeutic use, MESH: Diabetes Mellitus, Experimental/complications, MESH: Diabetes Mellitus, Experimental/drug therapy, Antineoplastic Agents, MESH: alpha-Amylases/metabolism, Diabetes Mellitus, Experimental, 03 medical and health sciences, 0404 agricultural biotechnology, In vivo, MESH: Enzyme Assays, Diabetes mellitus, Cell Line, Tumor, medicine, [SDV.BV]Life Sciences [q-bio]/Vegetal Biology, Animals, Humans, Hypoglycemic Agents, MTT assay, IC50, MESH: Mice, Enzyme Assays, MESH: Plant Extracts/therapeutic use, MESH: Humans, Cytotoxic activity, Plant Extracts, MESH: Tandem Mass Spectrometry, Polyphenols, alpha-Glucosidases, medicine.disease, IGR-39 cancer cell lines, MESH: Diabetes Mellitus, Type 2/drug therapy, Phoenix dactylifera L.’s leaves, MESH: Male, [SDV.BV.PEP]Life Sciences [q-bio]/Vegetal Biology/Phytopathology and phytopharmacy, MESH: Cell Death/drug effects, MESH: Diabetes Mellitus, Type 2/complications, Plant Leaves, 030104 developmental biology, Antidiabetic activity, chemistry, Diabetes Mellitus, Type 2, Hyperglycemia, alpha-Amylases, MESH: alpha-Glucosidases/metabolism, MESH: Chromatography, Liquid, Chromatography, Liquid, Phytotherapy
Abstract

International audience; Among various chronic disorders, cancer and diabetes mellitus are the most common disorders. This study was designed to evaluate the effectiveness of hydroalcoholic extract of Phoenix dactylifera L. leaves (HEPdL) in animal models of type II diabetes in vitro/in vivo and in a human melanoma-derived cell line (IGR-39). A liquid chromatography–tandem mass spectrometry (LC–MS/MS) analysis was also performed to determine the amount of phenolic and flavonoid compounds in this plant. The physicochemical results by LC–MS/MS analysis of HEPdL showed the presence of 10 phenolic compounds. The in vitro study showed that the extract exhibited a more specific and potent inhibitor of α-glucosidase than α-amylase with an IC50 value of 20 ± 1 μg/mL and 30 ± 0.8 μg/mL, respectively. More importantly, the in vivo study of the postprandial hyperglycemia activity with (20 mg/kg) of HEPdL showed a decrease in plasma glucose levels after 60 min in resemblance to the glucor (acarbose) (50 mg/kg) effect. The oral administration of HEPdL (20 mg/kg) in alloxan-induced diabetic mices for 28 days showed a more significant anti-diabetic activity than that of the drug (50 mg/kg). Moreover, cytotoxicity effects of HEPdL in IGR-39 cancer cell lines were tested by MTT assay. This extract was effective in inhibiting cancer cells growth (IGR-39) at dose 35 and 75 μg/mL. These results confirm ethnopharmacological significance of the plant and could be taken further for the development of an effective pharmaceutical drug against diabetes and cancer

Published
2016