Developing an exogenous pulmonary surfactant-glucocorticoids association: Effect of corticoid concentration on the biophysical properties of the surfactant

•The effects of GCs on dynamic and structural properties of EPS were studied.•The tested GCs did not caused detrimental effects on the EPS functionality.•GCs can be incorporated into membrane up to 10wt%.•Surfactant might be a promising strategy for the efficient transport of GCs. Glucocorticoids (G...

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Bibliographic Details
Published in:Respiratory physiology & neurobiology 2018-01, Vol.247, p.80-86
Main Authors: Cimato, Alejandra, Facorro, Graciela, Martínez Sarrasague, Margarita
Format: Article
Language:English
Subjects:
Animals
Beclomethasone
Beclomethasone - chemistry
Budesonide
Budesonide - chemistry
Cattle
Electron Spin Resonance Spectroscopy
ESR
Exogenous pulmonary surfactant
Fluticasone
Fluticasone - chemistry
Glucocorticoids
Glucocorticoids - chemistry
Membranes, Artificial
Microscopy, Polarization
Phospholipids - chemistry
Pulmonary Surfactants - chemistry
Surface Tension
Surface-Active Agents - chemistry
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Summary:•The effects of GCs on dynamic and structural properties of EPS were studied.•The tested GCs did not caused detrimental effects on the EPS functionality.•GCs can be incorporated into membrane up to 10wt%.•Surfactant might be a promising strategy for the efficient transport of GCs. Glucocorticoids (GCs) are used to treat lung disease. GCs incorporated in an exogenous pulmonary surfactant (EPS) could be an alternative management to improve drug delivery avoiding side effects. In the development of these pharmaceutical products, it is important to know the maximum amount of GC that can be incorporated and if increasing quantities of GCs alter EPS biophysical properties. Formulations containing EPS and beclomethasone, budesonide or fluticasone were analyzed (PL 10mg/ml; GC 1–2mg/ml). The microstructure was evaluated by electron paramagnetic resonance spectroscopy, GCs incorporated were determined by UV absorption and polarized light microscopy and surfactant activity with pulsating bubble surfactometer. We found that GCs have a ceiling of incorporation of around 10wt%, and that the GC not incorporated remains as crystals in the aqueous phase without altering the biophysical properties of the surfactant. This fact is important, because the greater the proportion of GC that EPS can carry, the better the efficiency of this pulmonary GC system.
ISSN:1569-9048
1878-1519
DOI:10.1016/j.resp.2017.09.011