作者: Lucia Prota , Antonietta Santoro , Maurizio Bifulco , Rita P. Aquino , Teresa Mencherini
DOI: 10.1016/J.IJPHARM.2011.03.055
关键词: IκBα 、 Biological activity 、 Naringin 、 Molecular biology 、 Biochemistry 、 Amino acid 、 Cell growth 、 Proline 、 Chemistry 、 Cell culture 、 Leucine
摘要: Abstract The effect of different amino acids (AAs) on the aerosol performance N spray-dried powders was studied. Morphology, size distribution, density, dissolution rate were evaluated and correlated to process parameters. analyzed by both Single Stage Glass Impinger Andersen Cascade Impactor. Results indicated that containing 5% (w/w) leucine, proline or histidine dried from 3:7 ethanol/water feeds showed very satisfying aerodynamic properties with fine particle fraction > 60%. Both neat (raw spray-dried) N-leu1 dry-powder showing good tested in cystic fibrosis (CF) normal bronchial epithelial cells. Cell proliferation expression levels key enzymes NF-κB MAPK/ERK pathways, overactivated CF cell lines, evaluated. able significantly inhibit IKKα, IKKβ, as well direct inhibitor, IκBα. In addition N-Leu1 inhibited phosphorylation ERK1/2 kinase did not reduce observed for raw drug. Leucine co-spray-dried drug improved vitro pharmacological activity Naringin. optimized N-Leu formulation dry powder is potentially hyperinflammatory status associated CF.