Spray-dried microparticles of glutathione and S-nitrosoglutathione based on Eudragit® FS 30D polymer
| Autor: | Marie Socha, Stéphane Gibaud, Shefaat Ullah Shah, C. Sejil |
|---|---|
| Přispěvatelé: | Cibles thérapeutiques, formulation et expertise pré-clinique du médicament (CITHEFOR), Université de Lorraine (UL), Gomal University, Laboratoire de Chimie Physique Macromoléculaire (LCPM), Institut de Chimie du CNRS (INC)-Université de Lorraine (UL)-Centre National de la Recherche Scientifique (CNRS) |
| Jazyk: | angličtina |
| Rok vydání: | 2017 |
| Předmět: |
Gastro-resistant
Scanning electron microscope Analytical chemistry Oral route Pharmaceutical Science 02 engineering and technology Methacrylate 030226 pharmacology & pharmacy S-Nitrosoglutathione 03 medical and health sciences chemistry.chemical_compound 0302 clinical medicine Fourier transform infrared spectroscopy Pharmacology chemistry.chemical_classification Spray dried Chromatography Chemistry Glutathione Polymer Nitrosothiols [SDV.SP]Life Sciences [q-bio]/Pharmaceutical sciences 021001 nanoscience & nanotechnology Crohn's disease Methacrylates 0210 nano-technology Dispersion (chemistry) |
| Zdroj: | Annales Pharmaceutiques Françaises Annales Pharmaceutiques Françaises, Elsevier Masson, 2017, 75 (2), pp.95-104. ⟨10.1016/j.pharma.2016.09.001⟩ |
| ISSN: | 0003-4509 |
| DOI: | 10.1016/j.pharma.2016.09.001⟩ |
| Popis: | Summary Objective In recent years, S-nitrosoglutathione has been proposed for the treatment of Crohn's disease to prevent mucosal barrier failure. In this paper, we report the formulation of spray dried microparticles of glutathione and S-nitrosoglutathione based on Eudragit ® FS 30D polymer (i.e. colon-specific delivery system). Material and methods The influence of several spray-drying parameters (inlet temperature 80–150 °C, solvent flow 5–10 mL/min) was studied. The parameters that yielded the best formulations (inlet temperature 120 °C, outlet temperature 47 °C, solvent flow 5 mL/min and air flow 100%) were selected for further studies. Results Scanning electron microscopy revealed that the resulting microparticles were spherical in shape. The powder X-ray diffraction patterns of pure GSH and GSNO showed sharp peaks that were not present in the microparticles, confirming a molecular dispersion of the drugs by the polymer. The stability of the drugs in the microparticles was confirmed by Fourier transform infrared spectroscopy. Release studies in phosphate buffer solutions showed fast release at basic pH 7.4, sustained release at pH 6.8, but practically no release at the acidic pHs of 1.2, 3 and 6 for the pH-sensitive microparticles. The microparticles prevented the release of drugs at acidic pH while demonstrating fast release at basic pH 7.4; this suggests the suitability of these microparticles to be evaluated for specific colon targeting. Conclusion Using Eudragit ® FS 30D as a gastro-resistant rate-controlling polymer, S-nitrosoglutathion could be targeted to the colon for further studies in the treatment of inflammatory bowel diseases including Crohn's disease. |
| Databáze: | OpenAIRE |
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