Analysis of the structure and surfactant activity of novel formulations containing exogenous pulmonary surfactant and glucocorticoids.

ABSTRACT

Exogenous pulmonary surfactant (EPS) could be used as carrier of glucocorticoids (GCs) in therapy for respiratory diseases. We formulated novel combination drug products containing bovine EPS and one GC (10wt%) beclomethasone (Be), budesonide (Bu) or fluticasone (Flu), and studied the GCs action on the surface activity and biophysical properties of EPS. Subtype ratio was evaluated by phospholipid determination; surface tension (ST) with a pulsating bubble surfactometer and conformational changes by Electron Spin Resonance (ESR). GCs were incorporated into EPS in more than 80%. None of them generated disaggregation of surfactant, only Bu was found in the light subtype. Bu and Be caused minimal changes in fluidity on polar region of bilayers, but these changes were not enough to inactivate the surfactant. Flu did not significantly alter any biophysical properties or surface activity. These novel combination EPS-GC products might be a promising strategy in the therapy of pulmonary diseases as the incorporation of the GCs tested did not cause detrimental effects on EPS functionality.