Furst Tania, Piette Marie, Lechanteur Anna, Evrard Brigitte, Piel Géraldine
Laboratory of Pharmaceutical Technology and Biopharmacy, CIRM, University of Liège, Belgium.
Laboratory of Pharmaceutical Technology and Biopharmacy, CIRM, University of Liège, Belgium.
Eur J Pharm Biopharm. 2015 Sep;95(Pt A):128-35. doi: 10.1016/j.ejpb.2015.01.019. Epub 2015 Feb 4.
Vaginal delivery of active drugs has been largely studied for local and systemic applications. It is well known that vagina is a complex route, due to physiological and non-physiological changes. Therefore, in order to achieve a prolonged local effect, these variations have to be considered. The aim of this study was to formulate and to characterize a solid system, called sponges, obtained by lyophilization of cellulosic derivative (HEC 250M) hydrogels. These sponges have to meet particular criteria to be adapted for vaginal application: they have to adhere to the vaginal cavity and to be rehydrated by the small amount of vaginal fluids. Moreover, they have to be easily manipulated and to be stable. Three freezing temperatures have been tested to prepare sponges (-15°C, -25°C, -35°C). By SEM analyzes, it was observed that the pores into the sponges were smaller and numerous as the freezing temperature decreases. However, this temperature did not have any influence on the rehydration speed that was rather influenced by the HEC concentration. Viscosity and mucoadhesive strength of hydrogels and corresponding sponges were also measured. It appeared that these parameters are mainly dependent on the HEC concentration. These mucoadhesive sponges can be considered as potential drug delivery systems intended for vaginal application.
对于活性药物的阴道给药，人们已针对局部和全身应用进行了大量研究。众所周知，由于生理和非生理变化，阴道是一条复杂的给药途径。因此，为了实现长效局部作用，必须考虑这些变化。本研究的目的是制备并表征一种通过纤维素衍生物（HEC 250M）水凝胶冻干得到的固体系统，即海绵体。这些海绵体必须满足特定标准以适用于阴道给药：它们必须粘附于阴道腔，并能被少量阴道液再水化。此外，它们必须易于操作且稳定。已测试了三种冷冻温度来制备海绵体（-15°C、-25°C、-35°C）。通过扫描电子显微镜分析观察到，随着冷冻温度降低，海绵体内的孔隙变得更小且更多。然而，该温度对再水化速度没有任何影响，再水化速度主要受HEC浓度影响。还测量了水凝胶及相应海绵体的粘度和粘膜粘附强度。结果表明，这些参数主要取决于HEC浓度。这些粘膜粘附性海绵体可被视为用于阴道给药的潜在药物递送系统。
