ABSTRACT
The hemolytic activity and the cytotoxicity of PEG-based solubilizing agents on Caco-2 monolayer were investigated. In vitro tests can predict the irritancy potential and the delayed toxicity of the surfactants. There were significant concentration dependent differences between the result of the MTT (3-(4,5-dimethylthiazol-2-yl))-2,5-diphenyltetrazolium bromide) test and the data of the hemolytic activity test. Our investigations show that safer and more applicable tensides can be selected in order to form a more biocompatible medicament.
Subject(s)
Cell Survival/drug effects , Hemolysis/drug effects , Polyethylene Glycols/pharmacology , Caco-2 Cells , Coloring Agents , Erythrocytes/drug effects , Excipients , Humans , In Vitro Techniques , Solvents , Tetrazolium Salts , ThiazolesABSTRACT
Inhalation is an attractive delivery route for systemic and local therapy. High local drug concentrations may permit non-invasive delivery, lower therapeutic doses, reduced systemic side-effects, and reduced metabolic degradation of the drug in the liver. In our earlier study, carrier-based microcomposites were prepared and investigated. The present study introduces studies of the cytotoxicity of meloxicam-containing microcomposites on monolayers of Calu-3 cells, in order to acquire information on its availability in pulmonary formulations. By relating cytotoxicity and drug dissolution, the appropriate amount of meloxicam for dry powder inhalation could be determined.