Cimato Alejandra, Facorro Graciela, Martínez Sarrasague Margarita
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. 2018 Jan;247:80-86. doi: 10.1016/j.resp.2017.09.011. Epub 2017 Sep 27.
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.
糖皮质激素（GCs）被用于治疗肺部疾病。将GCs掺入外源性肺表面活性剂（EPS）中可能是一种改善药物递送并避免副作用的替代管理方法。在这些药品的研发过程中，了解能够掺入的GCs的最大量以及GCs数量的增加是否会改变EPS的生物物理特性非常重要。对含有EPS以及倍氯米松、布地奈德或氟替卡松的制剂进行了分析（磷脂10mg/ml；GCs 1 - 2mg/ml）。通过电子顺磁共振光谱评估微观结构，通过紫外吸收、偏光显微镜测定掺入的GCs，并使用脉动气泡表面张力仪测定表面活性剂活性。我们发现GCs的掺入上限约为10wt%，未掺入的GCs以晶体形式留在水相中，而不会改变表面活性剂的生物物理特性。这一事实很重要，因为EPS能够携带的GCs比例越高，这种肺部GC系统的效率就越高。
