Cimato Alejandra, Hoyos Obando Andres, Facorro Graciela, Martínez Sarrasague María
Cátedra de Física, Departamento de Fisicomatemática, Facultad de Farmacia y Bioquímica, Universidad de Buenos Aires, Buenos Aires, Argentina.
Cátedra de Física, Departamento de Fisicomatemática, Facultad de Farmacia y Bioquímica, Universidad de Buenos Aires, Buenos Aires, Argentina.
Respir Physiol Neurobiol. 2016 Nov;233:33-40. doi: 10.1016/j.resp.2016.07.009. Epub 2016 Jul 28.
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.
外源性肺表面活性物质（EPS）可作为糖皮质激素（GCs）的载体用于呼吸系统疾病的治疗。我们制备了含有牛EPS和一种GC（10wt%）的新型复方药物产品：倍氯米松（Be）、布地奈德（Bu）或氟替卡松（Flu），并研究了GCs对EPS表面活性和生物物理性质的作用。通过磷脂测定评估亚型比例；使用脉动气泡表面张力仪测定表面张力（ST），通过电子自旋共振（ESR）测定构象变化。GCs在EPS中的掺入率超过80%。它们均未导致表面活性剂解聚，仅在轻亚型中发现了Bu。Bu和Be对双层膜极性区域的流动性影响最小，但这些变化不足以使表面活性剂失活。Flu未显著改变任何生物物理性质或表面活性。这些新型EPS-GC复方产品可能是治疗肺部疾病的一种有前景的策略，因为所测试的GCs掺入并未对EPS功能产生有害影响。
